Enzyme linked receptor
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This document discusses receptors and their downstream signaling pathways, including JAK-STAT and MAPK pathways. It defines receptors and describes different receptor types like G protein-coupled and enzyme-linked receptors. It then focuses on the JAK-STAT pathway, identifying its components like JAK kinases and STAT transcription factors, and drugs that target this pathway for conditions like rheumatoid arthritis. Finally, it examines the MAPK pathway, identifying the MAP kinase families involved in key cellular processes and examples of drugs that inhibit parts of this pathway.
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Tyrosine kinase receptors & Nuclear receptors
This document summarizes kinase receptors and nuclear receptors. Kinase receptors contain an extracellular ligand-binding domain connected by a transmembrane helix to an intracellular domain with kinase activity. They signal through phosphorylation cascades like MAPK. Nuclear receptors regulate gene transcription as ligand-activated transcription factors. They contain a ligand binding domain, DNA binding domain, and transcriptional regulation domain. Nuclear receptors form dimers and recruit cofactors to modify gene expression.
Enzyme linked receptors
Cell surface receptors transmit signals from outside the cell via signal transduction pathways. Receptors are divided into classes including ion channel-linked and enzyme-linked receptors. Enzyme-linked receptors contain intrinsic enzyme activity or associate with intracellular enzymes. Upon ligand binding, a conformational change activates the enzyme, initiating signaling cascades. Tyrosine kinase receptors have intrinsic kinase activity that phosphorylates tyrosines, creating docking sites and activating downstream pathways such as MAPK cascades. Mutations in these receptors and associated kinases can cause cancers and developmental disorders.
Nuclear Receptors
Nuclear receptors are a family of transcription factors that regulate gene expression in response to small lipophilic compounds like steroid hormones and lipids. They have a conserved structure of six domains including a ligand binding domain that activates gene expression when a ligand is present. Nuclear receptors function by binding to DNA as monomers or dimers and recruiting other proteins to regulate transcription. They are classified into three classes based on their ligand, subcellular localization, and mechanism of action.
G protein coupled receptors
G-protein coupled receptors (GPCRs) are the largest family of membrane receptors that are linked to intracellular effector proteins via G-protein activation. There are several classes of GPCRs classified based on sequence homology. All GPCRs have seven transmembrane domains and signal through heterotrimeric G proteins. When a ligand binds a GPCR, it activates an associated G protein which then regulates downstream effectors like adenylyl cyclase or phospholipase C. These pathways mediate many physiological processes such as vision, smell, immune response, and neuronal signaling.
JAK STAT SIGNALLING PATHWAY
The JAK-STAT signaling pathway transmits signals from extracellular chemical signals to the cell nucleus, which leads to DNA transcription and cellular activity. It consists of receptors, Janus kinases (JAKs), and signal transducers and activators of transcription (STATs). When ligands bind to receptors, JAKs phosphorylate themselves and STATs, causing STAT dimers to enter the nucleus and promote transcription. Disrupted JAK-STAT signaling can cause immune deficiency and cancer. Drugs targeting JAK-STAT are used to reduce immune response and treat disorders like cancer and rheumatoid arthritis.
Jak stat signalling pathway
The document summarizes the JAK-STAT signaling pathway. It discusses how the pathway consists of receptors, Janus kinases (JAKs), and Signal Transducers and Activators of Transcription (STATs). When a ligand binds to a receptor, it activates associated JAKs which phosphorylate STATs. Phosphorylated STATs form dimers and translocate to the nucleus to regulate gene transcription. The pathway is negatively regulated by phosphatases, suppressors of cytokine signaling, and protein inhibitors of activated STATs. Experiments using STAT knockout cells and mice have helped elucidate the specific roles and regulation of the pathway.
Types of receptors
This document discusses the different types of receptors:
1) Ligand-gated ion channels directly open ion channels in response to neurotransmitters.
2) G-protein coupled receptors activate intracellular second messenger systems through G-proteins.
3) Kinase-linked receptors activate intracellular protein kinases.
4) Nuclear receptors regulate gene transcription by binding to DNA response elements as dimers.
Jak stat
The JAK-STAT signaling pathway transmits signals from extracellular chemicals to the nucleus, activating transcription of target genes. It consists of a cell surface receptor, associated Janus kinases (JAKs), and signal transducers and activators of transcription (STATs). When a ligand binds the receptor, JAKs phosphorylate STATs, which form dimers and translocate to the nucleus to regulate gene expression. The Ras/MAPK pathway similarly relays signals from cell surface receptors via Ras, Raf, MEK, and MAPK proteins to influence transcription. Both pathways are tightly regulated and important for processes like cell growth, differentiation, and apoptosis, with dysregulation contributing to diseases.
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Tyrosine kinase receptors & Nuclear receptors
This document summarizes kinase receptors and nuclear receptors. Kinase receptors contain an extracellular ligand-binding domain connected by a transmembrane helix to an intracellular domain with kinase activity. They signal through phosphorylation cascades like MAPK. Nuclear receptors regulate gene transcription as ligand-activated transcription factors. They contain a ligand binding domain, DNA binding domain, and transcriptional regulation domain. Nuclear receptors form dimers and recruit cofactors to modify gene expression.
Enzyme linked receptors
Cell surface receptors transmit signals from outside the cell via signal transduction pathways. Receptors are divided into classes including ion channel-linked and enzyme-linked receptors. Enzyme-linked receptors contain intrinsic enzyme activity or associate with intracellular enzymes. Upon ligand binding, a conformational change activates the enzyme, initiating signaling cascades. Tyrosine kinase receptors have intrinsic kinase activity that phosphorylates tyrosines, creating docking sites and activating downstream pathways such as MAPK cascades. Mutations in these receptors and associated kinases can cause cancers and developmental disorders.
Nuclear Receptors
Nuclear receptors are a family of transcription factors that regulate gene expression in response to small lipophilic compounds like steroid hormones and lipids. They have a conserved structure of six domains including a ligand binding domain that activates gene expression when a ligand is present. Nuclear receptors function by binding to DNA as monomers or dimers and recruiting other proteins to regulate transcription. They are classified into three classes based on their ligand, subcellular localization, and mechanism of action.
G protein coupled receptors
G-protein coupled receptors (GPCRs) are the largest family of membrane receptors that are linked to intracellular effector proteins via G-protein activation. There are several classes of GPCRs classified based on sequence homology. All GPCRs have seven transmembrane domains and signal through heterotrimeric G proteins. When a ligand binds a GPCR, it activates an associated G protein which then regulates downstream effectors like adenylyl cyclase or phospholipase C. These pathways mediate many physiological processes such as vision, smell, immune response, and neuronal signaling.
JAK STAT SIGNALLING PATHWAY
The JAK-STAT signaling pathway transmits signals from extracellular chemical signals to the cell nucleus, which leads to DNA transcription and cellular activity. It consists of receptors, Janus kinases (JAKs), and signal transducers and activators of transcription (STATs). When ligands bind to receptors, JAKs phosphorylate themselves and STATs, causing STAT dimers to enter the nucleus and promote transcription. Disrupted JAK-STAT signaling can cause immune deficiency and cancer. Drugs targeting JAK-STAT are used to reduce immune response and treat disorders like cancer and rheumatoid arthritis.
Jak stat signalling pathway
The document summarizes the JAK-STAT signaling pathway. It discusses how the pathway consists of receptors, Janus kinases (JAKs), and Signal Transducers and Activators of Transcription (STATs). When a ligand binds to a receptor, it activates associated JAKs which phosphorylate STATs. Phosphorylated STATs form dimers and translocate to the nucleus to regulate gene transcription. The pathway is negatively regulated by phosphatases, suppressors of cytokine signaling, and protein inhibitors of activated STATs. Experiments using STAT knockout cells and mice have helped elucidate the specific roles and regulation of the pathway.
Types of receptors
This document discusses the different types of receptors:
1) Ligand-gated ion channels directly open ion channels in response to neurotransmitters.
2) G-protein coupled receptors activate intracellular second messenger systems through G-proteins.
3) Kinase-linked receptors activate intracellular protein kinases.
4) Nuclear receptors regulate gene transcription by binding to DNA response elements as dimers.
Jak stat
The JAK-STAT signaling pathway transmits signals from extracellular chemicals to the nucleus, activating transcription of target genes. It consists of a cell surface receptor, associated Janus kinases (JAKs), and signal transducers and activators of transcription (STATs). When a ligand binds the receptor, JAKs phosphorylate STATs, which form dimers and translocate to the nucleus to regulate gene expression. The Ras/MAPK pathway similarly relays signals from cell surface receptors via Ras, Raf, MEK, and MAPK proteins to influence transcription. Both pathways are tightly regulated and important for processes like cell growth, differentiation, and apoptosis, with dysregulation contributing to diseases.
Receptors
Introduction - receptor
Drug – receptor interactions
Ligand gated ion channel receptors
G – protein coupled receptors
Kinase liked receptors
Nuclear receptors
Comparison of receptor types
Conclusion
References
Ion channel RECEPTOR
The document summarizes ion channels and ion channel receptors. It discusses several key points:
1) Ion channels transport specific ions across cell membranes and generate electrical signals. Voltage-gated and ligand-gated ion channels open and close in response to changes in membrane potential or ligand binding.
2) Common types of ion channels include voltage-gated sodium, potassium, and calcium channels, as well as ligand-gated channels like GABA, glycine, and glutamate receptors.
3) Ion channels play important physiological roles in nerve impulse conduction, muscle contraction, and other processes. Dysfunctions can lead to channelopathies and medical conditions. Many drugs target ion channels.
Ion channels
Transmembrane ion channels are protein pores that regulate the passage of ions across cell membranes. There are two main types - voltage-gated ion channels, which open and close in response to changes in membrane potential, and ligand-gated ion channels, which open when certain chemical messengers bind to them. Key voltage-gated channels include sodium, calcium, and potassium channels. Major ligand-gated channels are nicotinic acetylcholine receptors, GABAA receptors, glutamate receptors, and ATP-sensitive potassium channels. The discovery and study of ion channels over time has provided crucial insights into nerve signaling and other cellular processes.
Map kinase and jak stat pathway
The document discusses the MAP kinase pathway and JAK-STAT pathway. It describes that the MAP kinase pathway involves signal transmission from activated RAS through a protein kinase cascade to MAP kinase, which then activates transcription factors in the nucleus. It also explains that the JAK-STAT pathway involves cytokine receptors activating associated JAK kinases, which phosphorylate and activate STAT proteins that dimerize and move to the nucleus to regulate gene expression. Both pathways play important roles in signal transduction and regulating gene transcription in cells.
Ion channels
Ion channels are membrane proteins that allow ions to pass through their pore, regulating ion flow and electrical signals. There are two main types of gated ion channels: ligand-gated channels, which open when neurotransmitters bind, and voltage-gated channels, which open in response to changes in membrane potential. Ligand-gated channels allow sodium influx upon acetylcholine binding, depolarizing the membrane and triggering action potentials. Voltage-gated channels maintain the resting potential and enable action potential propagation along axons by selectively transporting sodium, potassium, calcium, and chloride ions in response to changes in voltage.
GPCR
G protein coupled receptors (GPCRs) are a large family of cell membrane receptors that are linked to intracellular effector proteins. All GPCRs have seven transmembrane alpha helical segments. The receptors activate intracellular signaling pathways upon binding of an agonist ligand. This leads to the exchange of GDP for GTP on associated G proteins, which then activate downstream effectors to induce cellular responses. The major effector pathways activated by GPCRs are adenylyl cyclase/cAMP, phospholipase C/IP3-DAG, and ion channel regulation.
Types of receptors
Types of Receptors
Receptors are protein molecules in the target cell or on its surface that bind ligands. There are two types of receptors: internal receptors and cell-surface receptors.
Secondary messengers system
This document discusses second messengers, which are intracellular molecules that amplify and spread signals from receptors on the cell surface. It describes four main classes of second messengers - cyclic nucleotides, membrane lipid derivatives, calcium ions, and gases like nitric oxide. Specifically, it examines the cAMP, cGMP, IP3/DAG, and calcium-mediated signaling pathways, outlining the ligands, effectors, and downstream effects of each messenger. It also provides details on nitric oxide and calcium signaling within cells.
G protein coupled receptors
Dr. Pavani discusses G protein-coupled receptors (GPCRs), which are integral membrane proteins that sense molecules outside the cell and activate internal signal transduction pathways and cellular responses. There are over 800 GPCRs in humans that detect a wide range of ligands and are involved in many physiological processes. GPCRs work by coupling to G proteins, which activate various intracellular effectors like adenylyl cyclase, phospholipase C, and ion channels. Dysregulation of GPCR signaling can lead to many human diseases. Martin Rodbell and Alfred Gilman were awarded the 1994 Nobel Prize in Physiology or Medicine for their discoveries related to G proteins and GPCR signal transduction.
Mapk pathways
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Receptors
- There are 4 main types of receptors: ligand-gated ion channels, G-protein coupled receptors, kinase-linked receptors, and nuclear receptors.
- Ligand-gated ion channels directly open ion channels, G-protein receptors signal through G-proteins, kinase receptors signal through phosphorylation, and nuclear receptors regulate gene transcription as transcription factors.
- Receptors recognize a wide range of ligands and allow cells to respond to changes in their internal or external environment through second messenger signaling pathways.
Prostaglandin, leukotriene, and thromboxane
Eicosanoids are signaling molecules derived from polyunsaturated fatty acids like arachidonic acid. They are involved in complex control over inflammation, immunity, and the central nervous system. Eicosanoids are synthesized through the enzymatic oxidation of fatty acids by cyclooxygenase and lipoxygenase enzymes. They have short half-lives and act locally through autocrine and paracrine signaling. Examples of important eicosanoids include prostaglandins, thromboxanes, and leukotrienes.
Receptors and receptors classification
Definition
Classification and description of each class.
Description of individual receptor.
Forces affecting the drug receptor binding.
Binding of drug receptor affect drug action.
Agonist and antagonist.
Disease due to malfunctioning of receptors.
New drug design based on structure of receptors
Receptor as target for drug discovery.
Drug action not mediated by receptor.
Cell signaling
Cell signaling / Signal Transduction / Transmembrane signaling.
It is the process by which cells communicate with their environment and respond to external stimuli.
When a signaling molecule(ligand) binds to its receptor, it alters the shape or activity of the receptor, triggering a change inside of the cell such as alteration in the activity of a gene / cell division. Thus the original Intercellular Signal is converted into an Intracellular Signal that triggers as a response.
Receptors types
The document summarizes the main types of protein targets for drug action in mammalian cells. It discusses four main types:
1) Receptors, which are membrane proteins that sense chemical messengers like hormones and transmitters. They include ligand-gated ion channels, G-protein coupled receptors, kinase-linked receptors, and nuclear receptors.
2) Ion channels, which are membrane proteins that allow ions to pass through. They include ligand-gated ion channels and voltage-gated channels.
3) Enzymes, which are targets of drugs that act as competitive or irreversible inhibitors.
4) Carrier molecules called transporters, which transport ions and molecules across cell membranes using carrier proteins
MAPK pathway,
MAPK Signaling pathway (Mitogen-activated protein kinase), how the pathway helps in regulation of mitosis, It's activation and inactivation inside the cell, roles of MAPK pathway in cancerous cell, different classes of MAP kinase in human
Intercellular and intracellular cell signaling pathway
This document summarizes intercellular and intracellular signaling pathways. It describes four types of intercellular signaling: autocrine, paracrine, endocrine, and juxtacrine. Intracellular signaling pathways involve signal transduction after a ligand binds to a cell surface receptor. Examples of intracellular pathways discussed are G protein-coupled receptors, enzyme-linked receptors, ligand-gated ion channels, and second messenger pathways like cyclic AMP. The document provides details on the mechanisms and key steps in several of these signaling pathways.
Cyclic amp pathway
Earl Wilbur Sutherland Jr. discovered cyclic AMP (cAMP) as a second messenger that allows hormones like epinephrine to trigger physiological responses in cells. cAMP is produced from ATP by adenylate cyclase in response to hormone binding and activates protein kinase A. Protein kinase A then phosphorylates other proteins to initiate downstream cellular effects. The actions of cAMP are terminated by phosphodiesterase breaking it down and by dephosphorylation of proteins. cAMP mediates many important processes like glycogen breakdown and gene transcription.
Receptor
This document defines receptors and classifies them as either internal or cell surface receptors. It describes the three main types of cell surface receptors: ion channel-linked receptors, G-protein-linked receptors, and enzyme-linked receptors. It also discusses the forces affecting drug-receptor binding, how binding affects drug action, and the differences between agonists and antagonists. Additionally, it covers how receptor malfunctions can cause diseases and how understanding receptor structure enables new drug design by targeting receptors.
Cell signalling
This document discusses intracellular and extracellular cell signaling. It defines cell signaling as communication between cells using chemical signals or ligands. Extracellular signaling occurs between cells and can be contact-dependent, paracrine, synaptic, or endocrine. Intracellular signaling involves signal transduction across the cell membrane and secondary messengers that activate intracellular signaling pathways involving protein phosphorylation or GTP-binding proteins. Key signaling pathways include G-protein coupled receptors and receptor tyrosine kinases that activate intracellular cascades to regulate processes like gene expression, cell growth, and metabolism.
Cell signaling
Cell signaling is a complex system of communication that coordinates basic cellular activities and cell actions. It involves signaling molecules that produce responses in target cells through receptor binding. There are three main types of signaling: endocrine, paracrine, and autocrine. Upon receptor activation, various intracellular signal transduction pathways are initiated using second messengers like cAMP, IP3, Ca2+, which activate downstream effector mechanisms to elicit cellular responses. The key pathways include G protein-coupled receptor pathways, tyrosine kinase receptor pathways like Ras/Raf pathway and Jak/Stat pathway. Understanding cell signaling is crucial for treating diseases and engineering tissues.
JAK-STAT Signalling Pathway
This document presents information about the JAK-STAT signaling pathway. It begins with an introduction to the pathway, explaining that it communicates chemical signals from outside the cell to the nucleus and involves the JAK and STAT proteins. It then discusses the key components of the pathway - the JAK kinases that phosphorylate STAT proteins, and the STAT transcription factors. The document outlines the steps of the JAK-STAT signaling cascade, from cytokine binding to STAT phosphorylation and nuclear translocation. It also briefly discusses negative regulation of the pathway and its clinical significance in immune function and cancer. Finally, it provides examples of drugs that target the JAK-STAT pathway for conditions like rheumatoid arthritis.
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Receptors
Introduction - receptor
Drug – receptor interactions
Ligand gated ion channel receptors
G – protein coupled receptors
Kinase liked receptors
Nuclear receptors
Comparison of receptor types
Conclusion
References
Ion channel RECEPTOR
The document summarizes ion channels and ion channel receptors. It discusses several key points:
1) Ion channels transport specific ions across cell membranes and generate electrical signals. Voltage-gated and ligand-gated ion channels open and close in response to changes in membrane potential or ligand binding.
2) Common types of ion channels include voltage-gated sodium, potassium, and calcium channels, as well as ligand-gated channels like GABA, glycine, and glutamate receptors.
3) Ion channels play important physiological roles in nerve impulse conduction, muscle contraction, and other processes. Dysfunctions can lead to channelopathies and medical conditions. Many drugs target ion channels.
Ion channels
Transmembrane ion channels are protein pores that regulate the passage of ions across cell membranes. There are two main types - voltage-gated ion channels, which open and close in response to changes in membrane potential, and ligand-gated ion channels, which open when certain chemical messengers bind to them. Key voltage-gated channels include sodium, calcium, and potassium channels. Major ligand-gated channels are nicotinic acetylcholine receptors, GABAA receptors, glutamate receptors, and ATP-sensitive potassium channels. The discovery and study of ion channels over time has provided crucial insights into nerve signaling and other cellular processes.
Map kinase and jak stat pathway
The document discusses the MAP kinase pathway and JAK-STAT pathway. It describes that the MAP kinase pathway involves signal transmission from activated RAS through a protein kinase cascade to MAP kinase, which then activates transcription factors in the nucleus. It also explains that the JAK-STAT pathway involves cytokine receptors activating associated JAK kinases, which phosphorylate and activate STAT proteins that dimerize and move to the nucleus to regulate gene expression. Both pathways play important roles in signal transduction and regulating gene transcription in cells.
Ion channels
Ion channels are membrane proteins that allow ions to pass through their pore, regulating ion flow and electrical signals. There are two main types of gated ion channels: ligand-gated channels, which open when neurotransmitters bind, and voltage-gated channels, which open in response to changes in membrane potential. Ligand-gated channels allow sodium influx upon acetylcholine binding, depolarizing the membrane and triggering action potentials. Voltage-gated channels maintain the resting potential and enable action potential propagation along axons by selectively transporting sodium, potassium, calcium, and chloride ions in response to changes in voltage.
GPCR
G protein coupled receptors (GPCRs) are a large family of cell membrane receptors that are linked to intracellular effector proteins. All GPCRs have seven transmembrane alpha helical segments. The receptors activate intracellular signaling pathways upon binding of an agonist ligand. This leads to the exchange of GDP for GTP on associated G proteins, which then activate downstream effectors to induce cellular responses. The major effector pathways activated by GPCRs are adenylyl cyclase/cAMP, phospholipase C/IP3-DAG, and ion channel regulation.
Types of receptors
Types of Receptors
Receptors are protein molecules in the target cell or on its surface that bind ligands. There are two types of receptors: internal receptors and cell-surface receptors.
Secondary messengers system
This document discusses second messengers, which are intracellular molecules that amplify and spread signals from receptors on the cell surface. It describes four main classes of second messengers - cyclic nucleotides, membrane lipid derivatives, calcium ions, and gases like nitric oxide. Specifically, it examines the cAMP, cGMP, IP3/DAG, and calcium-mediated signaling pathways, outlining the ligands, effectors, and downstream effects of each messenger. It also provides details on nitric oxide and calcium signaling within cells.
G protein coupled receptors
Dr. Pavani discusses G protein-coupled receptors (GPCRs), which are integral membrane proteins that sense molecules outside the cell and activate internal signal transduction pathways and cellular responses. There are over 800 GPCRs in humans that detect a wide range of ligands and are involved in many physiological processes. GPCRs work by coupling to G proteins, which activate various intracellular effectors like adenylyl cyclase, phospholipase C, and ion channels. Dysregulation of GPCR signaling can lead to many human diseases. Martin Rodbell and Alfred Gilman were awarded the 1994 Nobel Prize in Physiology or Medicine for their discoveries related to G proteins and GPCR signal transduction.
Mapk pathways
MAP KINASES PATHWAY..Regulation and signalling with a note on mammalian derived protein kinases with a note on JNK/p38/PI3 kinase pathways
Receptors
- There are 4 main types of receptors: ligand-gated ion channels, G-protein coupled receptors, kinase-linked receptors, and nuclear receptors.
- Ligand-gated ion channels directly open ion channels, G-protein receptors signal through G-proteins, kinase receptors signal through phosphorylation, and nuclear receptors regulate gene transcription as transcription factors.
- Receptors recognize a wide range of ligands and allow cells to respond to changes in their internal or external environment through second messenger signaling pathways.
Prostaglandin, leukotriene, and thromboxane
Eicosanoids are signaling molecules derived from polyunsaturated fatty acids like arachidonic acid. They are involved in complex control over inflammation, immunity, and the central nervous system. Eicosanoids are synthesized through the enzymatic oxidation of fatty acids by cyclooxygenase and lipoxygenase enzymes. They have short half-lives and act locally through autocrine and paracrine signaling. Examples of important eicosanoids include prostaglandins, thromboxanes, and leukotrienes.
Receptors and receptors classification
Definition
Classification and description of each class.
Description of individual receptor.
Forces affecting the drug receptor binding.
Binding of drug receptor affect drug action.
Agonist and antagonist.
Disease due to malfunctioning of receptors.
New drug design based on structure of receptors
Receptor as target for drug discovery.
Drug action not mediated by receptor.
Cell signaling
Cell signaling / Signal Transduction / Transmembrane signaling.
It is the process by which cells communicate with their environment and respond to external stimuli.
When a signaling molecule(ligand) binds to its receptor, it alters the shape or activity of the receptor, triggering a change inside of the cell such as alteration in the activity of a gene / cell division. Thus the original Intercellular Signal is converted into an Intracellular Signal that triggers as a response.
Receptors types
The document summarizes the main types of protein targets for drug action in mammalian cells. It discusses four main types:
1) Receptors, which are membrane proteins that sense chemical messengers like hormones and transmitters. They include ligand-gated ion channels, G-protein coupled receptors, kinase-linked receptors, and nuclear receptors.
2) Ion channels, which are membrane proteins that allow ions to pass through. They include ligand-gated ion channels and voltage-gated channels.
3) Enzymes, which are targets of drugs that act as competitive or irreversible inhibitors.
4) Carrier molecules called transporters, which transport ions and molecules across cell membranes using carrier proteins
MAPK pathway,
MAPK Signaling pathway (Mitogen-activated protein kinase), how the pathway helps in regulation of mitosis, It's activation and inactivation inside the cell, roles of MAPK pathway in cancerous cell, different classes of MAP kinase in human
Intercellular and intracellular cell signaling pathway
This document summarizes intercellular and intracellular signaling pathways. It describes four types of intercellular signaling: autocrine, paracrine, endocrine, and juxtacrine. Intracellular signaling pathways involve signal transduction after a ligand binds to a cell surface receptor. Examples of intracellular pathways discussed are G protein-coupled receptors, enzyme-linked receptors, ligand-gated ion channels, and second messenger pathways like cyclic AMP. The document provides details on the mechanisms and key steps in several of these signaling pathways.
Cyclic amp pathway
Earl Wilbur Sutherland Jr. discovered cyclic AMP (cAMP) as a second messenger that allows hormones like epinephrine to trigger physiological responses in cells. cAMP is produced from ATP by adenylate cyclase in response to hormone binding and activates protein kinase A. Protein kinase A then phosphorylates other proteins to initiate downstream cellular effects. The actions of cAMP are terminated by phosphodiesterase breaking it down and by dephosphorylation of proteins. cAMP mediates many important processes like glycogen breakdown and gene transcription.
Receptor
This document defines receptors and classifies them as either internal or cell surface receptors. It describes the three main types of cell surface receptors: ion channel-linked receptors, G-protein-linked receptors, and enzyme-linked receptors. It also discusses the forces affecting drug-receptor binding, how binding affects drug action, and the differences between agonists and antagonists. Additionally, it covers how receptor malfunctions can cause diseases and how understanding receptor structure enables new drug design by targeting receptors.
Cell signalling
This document discusses intracellular and extracellular cell signaling. It defines cell signaling as communication between cells using chemical signals or ligands. Extracellular signaling occurs between cells and can be contact-dependent, paracrine, synaptic, or endocrine. Intracellular signaling involves signal transduction across the cell membrane and secondary messengers that activate intracellular signaling pathways involving protein phosphorylation or GTP-binding proteins. Key signaling pathways include G-protein coupled receptors and receptor tyrosine kinases that activate intracellular cascades to regulate processes like gene expression, cell growth, and metabolism.
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Intercellular and intracellular cell signaling pathway
Intercellular and intracellular cell signaling pathway
Similar to Enzyme linked receptor
Cell signaling
Cell signaling is a complex system of communication that coordinates basic cellular activities and cell actions. It involves signaling molecules that produce responses in target cells through receptor binding. There are three main types of signaling: endocrine, paracrine, and autocrine. Upon receptor activation, various intracellular signal transduction pathways are initiated using second messengers like cAMP, IP3, Ca2+, which activate downstream effector mechanisms to elicit cellular responses. The key pathways include G protein-coupled receptor pathways, tyrosine kinase receptor pathways like Ras/Raf pathway and Jak/Stat pathway. Understanding cell signaling is crucial for treating diseases and engineering tissues.
JAK-STAT Signalling Pathway
This document presents information about the JAK-STAT signaling pathway. It begins with an introduction to the pathway, explaining that it communicates chemical signals from outside the cell to the nucleus and involves the JAK and STAT proteins. It then discusses the key components of the pathway - the JAK kinases that phosphorylate STAT proteins, and the STAT transcription factors. The document outlines the steps of the JAK-STAT signaling cascade, from cytokine binding to STAT phosphorylation and nuclear translocation. It also briefly discusses negative regulation of the pathway and its clinical significance in immune function and cancer. Finally, it provides examples of drugs that target the JAK-STAT pathway for conditions like rheumatoid arthritis.
Cell signalling through MAP-Kinase and JAK STAT pathway.pptx
Cell signaling is a complex process by which cells communicate with each other to regulate various cellular activities, including growth, differentiation, metabolism, and apoptosis (cell death). Signaling molecules, such as hormones, growth factors, and neurotransmitters, bind to specific receptors on the cell surface or inside the cell, initiating a cascade of events that ultimately lead to a cellular response. There are several signaling pathways involved in cell signaling, including the Ras-MAPK pathway and the JAK-STAT pathway.
Both the Ras-MAPK pathway and the JAK-STAT pathway are critical for normal cellular function, and dysregulation of these pathways can lead to various diseases, including cancer and inflammatory disorders.
JAK STAT.pptx
The JAK-STAT pathway transmits signals from extracellular chemical messengers through three main components: cell surface receptors, Janus kinases (JAKs), and signal transducers and activators of transcription (STATs). Upon ligand binding, receptor-associated JAKs become activated and phosphorylate STATs, allowing them to form dimers and translocate to the nucleus to regulate gene expression. The pathway is negatively regulated by phosphatases, suppressors of cytokine signaling, and protein inhibitors of activated STAT. Disrupted JAK-STAT signaling can cause immune deficiency, inflammation, and cancer. Drugs targeting the pathway are used to treat transplant rejection, myeloproliferative disorders, rheumatoid arthritis, and atopic
Cell signaling by ved prakash
Cell signaling is part of any communication process that governs basic activities of cells and coordinates all cell actions. The ability of cells to perceive and correctly respond to their microenvironment is the basis of development, tissue repair, and immunity, as well as normal tissue homeostasis
Jak stat signalling
Cytokines signal through the JAK-STAT pathway. JAK kinases are associated with cytokine receptors and activate upon cytokine binding. Activated JAKs phosphorylate the receptor and STAT proteins in the cytoplasm. Phosphorylated STATs dimerize and translocate to the nucleus to regulate gene expression. This confers specificity to cytokine responses. Drugs that target the JAK-STAT pathway include cytokine receptor blockers and JAK inhibitors, which are used to treat conditions like transplant rejection and rheumatoid arthritis.
JAK STAT Pathway.pptx
This document provides an overview of the Janus Kinase/Signal Transducers and Activators of Transcription (JAK/STAT) signaling pathway. It discusses how the pathway is activated when ligands bind to cell surface receptors, causing receptor dimerization and activation of associated JAK kinases. The JAKs then phosphorylate and activate STAT proteins, which dimerize and translocate to the nucleus to regulate gene transcription. Negative regulation of the pathway involves proteins that deactivate JAKs and STATs. The pathway is essential for processes like immunity, cell proliferation and death, and is involved in diseases when mutated.
Regulation of JAK STAT Pathway
1. The JAK-STAT pathway involves cytokine binding to receptors which activates JAK proteins, leading to phosphorylation of STAT proteins. Phosphorylated STATs form dimers and translocate to the nucleus to initiate gene transcription.
2. The pathway is regulated by PIAS, PTPs, and SOCS proteins. PIAS can add SUMO groups or recruit HDACs to inhibit STATs. PTPs remove phosphates to inhibit signaling. SOCS proteins form complexes that ubiquitinate proteins like JAKs and receptors to target them for degradation.
3. In rheumatoid arthritis, overactive JAK-STAT signaling leads to excessive inflammation. Approved drugs tofacitinib, ruxolit
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Signaling Pathways
The document summarizes several important signaling pathways involved in regulating gene expression, including the TGF-β, JAK-STAT, and Ras-MAPK pathways. The TGF-β pathway involves TGF-β ligands binding to serine/threonine kinase receptors, activating R-Smad transcription factors. The JAK-STAT pathway involves cytokine receptors associating with JAK kinases; ligand binding activates JAKs to phosphorylate and activate STAT transcription factors. The Ras-MAPK pathway involves receptor tyrosine kinases activating the Ras GTPase, which activates a kinase cascade culminating in MAPK activation of gene transcription.
Signal transduction
This document discusses signal transduction in cells. It explains that membrane proteins in bacterial cells detect environmental changes and generate signals to trigger responses. In multicellular organisms, cells exchange various signals, such as plant cells responding to growth hormones and sunlight. The document then provides details on the specific and sensitive nature of signal transduction pathways, including different types of receptors and some important signal transduction pathways like G protein-coupled receptors and receptor tyrosine kinases. It also discusses two-component regulatory systems in bacteria and plants.
CELL SIGNALING AND PATHWAYS INVOLVED IN CELL SIGNALING AND SOLID TUMORS.
Have Details about the various signaling pathways and signaling molecules and their role in solid tumors.
Stat3 protein in psoriasis by yousry
The document summarizes the Signal Transducer and Activator of Transcription (STAT) protein family, with a focus on STAT3 and its role in psoriasis. It describes how STAT proteins are activated downstream of cytokine and growth factor receptors via phosphorylation by Janus kinases (JAKs). STAT3 in particular is activated by cytokines like IL-6 and plays roles in processes like acute phase response, cell growth, and embryonic development. Aberrant STAT3 activation has been implicated in conditions like psoriasis and cancer.
Peroxisomes in dermatology.ppt
Peroxisomes are intracellular organelles found in mammalian cells including keratinocytes. They contain enzymes that produce hydrogen peroxide and help break down fatty acids, hormones, and other molecules. Peroxisomes proliferate in response to peroxisome proliferator activator receptors (PPARs) which are nuclear receptors that bind to peroxisome proliferator response elements in DNA and modulate gene expression involved in lipid metabolism and peroxisome biogenesis. PPARs have roles in skin homeostasis, inflammation, proliferation, and lipid metabolism and are targets for modulating peroxisome functions.
Peroxisomes in dermatology
Peroxisomes are intracellular organelles that contain enzymes involved in various metabolic processes like lipid metabolism. They contain oxidases rather than hydrolases. Peroxisome biogenesis involves the recruitment of lipids and proteins. Peroxisome proliferator-activated receptors (PPARs) are transcription factors that regulate peroxisome functions. PPARs have roles in skin homeostasis, inflammation, differentiation, wound healing and diseases like psoriasis. Activation of PPARs modulates these processes by regulating gene expression.
CELL SIGNALING
The document discusses three types of cell signaling:
1) Autocrine signaling occurs when a cell produces a messenger that stimulates receptors on its own surface.
2) Paracrine signaling involves messenger molecules that travel short distances to stimulate nearby cells.
3) Endocrine signaling uses messenger molecules that travel long distances through the bloodstream to target distant cells.
4183 abcdefghijklmnofqrstuvwxyz12345.ppt
Cells within multicellular organisms communicate via secreted molecules or direct contact. These signals integrate and coordinate cell functions. Cells signal locally through diffusible molecules or contact between nearby cells. They also signal over long distances using hormones transported in body fluids. Signaling involves reception of the signal, transduction through intracellular pathways, and cellular responses. Key pathways include receptor tyrosine kinases, MAPK pathways, JAK/STAT, and PI3K/Akt pathways. Signaling controls processes like cell growth, differentiation, and responses to stimuli.
Eicosanoids: lipid mediators of inflammation in transplantation
This document summarizes research on eicosanoids, lipid mediators derived from arachidonic acid that play important roles in inflammation and immunity. It focuses on the roles of prostanoids and leukotrienes in organ transplantation. Prostanoids like prostaglandin E2 and prostacyclin generally have immunosuppressive effects, while thromboxane A2 enhances immune responses. Studies in animals and some human trials suggest these eicosanoids can influence transplant rejection and outcomes. Future research on specific receptors for these lipids may lead to new pharmacological approaches for controlling inflammation and promoting graft acceptance.
Receptors and signaling pathway dr nipa
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2. It describes two main types of receptors - extracellular/transmembrane receptors like G protein-coupled receptors and ion channel receptors, and intracellular/cytoplasmic receptors like nuclear receptors.
3. The key transmembrane signaling pathways discussed are the G protein pathway and its second messenger systems of cAMP, IP3/DAG, and ion channels. It also covers receptor enzyme pathways like receptor tyrosine kinases and Jak-STAT receptors.
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Enzyme linked receptor
- 1. Presented by Shakshi Sharma M. Pharm : Pharmacology (Ist semester) Department of Pharmacology ISF college of Pharmacy, Moga
- 2. Receptor Types of Receptor Enzyme linked receptor and their structure Cellular response JAK-STAT pathway Drugs targeted in JSAK-STAT pathway Physiological role of JAK-STAT pathway MAP kinase and their types Drugs targeted in MAP kinase Physiological role of MAP kinase signaling
- 3. The concept of receptor was introduced by John Newport Langley and Paul Ehrlich in 20th century. Receptor is defined as a macromolecule or binding site located on the surface or inside the effector cell that serves to recognize the signal/molecule/drug and initiate the response to it, but itself has no other function.
- 4. 1. G- protein coupled receptor- e.g., Ach- Muscarinic and Adrenergic receptors. 2. Ion channel receptor- e.g., Ach- Nicotine, GABA, Glutamate. 3. Transmembrane enzyme linked receptor- e.g., Insulin. 4. Receptors regulating gene expression- e.g., Steroids, Thyroxin.
- 5. These are also known as Catalytic Receptor, is a transmembrane receptor, where the binding of an extracellular ligand causes enzymatic activity on the intracellular side. Example:- Insulin, Epidermal growth factor (EGF), Nerve growth factor (NGF) receptors.
- 7. 7 Ligand Receptor Get autophosphorylate Activate ligand which futher regulates various pathways PI3-K /Akt pathway RAS/MAPK pathway JAK/STAT pathway Binds to
- 8. The JAK/STAT signaling pathway transmits information from extracellular chemical signals to the nucleus resulting in DNA transcription and expression of genes involved in immunity, proliferation, differentiation, apoptosis, and oncogenesis.
- 9. JAK- Family of cytoplamic non-receptor tyrosine kinases which get activated after the binding of a cytokine to the cell- surface cytokine receptor. STAT- Family of transcription factors that become activated when one of the tyrosine residues is phosphorylated by JAK. STAT3- Dimers then translocate from the cytoplasm into the nucleus-bind to Interferon-Stimulated Response Elements. Cellular responses to dozens of cytokines and growth factors are mediated by the evolutionarily conserved.
- 11. TOFACITINIB – JAK-STAT inhibitor, used in Rheumatoid arthritis. RUXOLITINIB – JAK inhibitor, used in myeloproliferative disorder. PYRIMETHAMINE – STAT3 inhibitor, used in chronic lymphocytic leukaemia. TOFACITINIB - JAK inhibitor, used in rheumatoid arthritis.
- 12. Modulates development and physiology of white adipose tissue. STAT proteins regulate adipocyte differentiation. Adipose tissue immune cells produce JAK-STAT activator.
- 13. It is an enzyme that translocates the signals to the nucleus and activates many transcriptional factors by phosphorylating many different proteins that regulate expression of important cell cycle and differentiation specific proteins.
- 14. MAP kinases are serine/threonine-specific protein kinases that respond to extracellular stimuli (mitogens, osmotic stress, heat shock, and pro- inflammatory cytokines) and regulate various cellular activities, such as gene expression, mitosis, differentiation, proliferation, cell survival/apoptosis. MAP kinases are activated within the protein kinase cascades called MAPK cascade/MAPK signaling toolkit.
- 16. 1. c-Jun NH2-terminal kinases (JNKs)- this phosphorylates Jun. 1. p38 MAPK- regulates cell death (apoptosis) and inflammatory cytokine expression (may be important in arthritis). 1. Extracellular signal-related kinases (ERKs)- crucial in cell division, memory and learning (abnormal ERKs may lead to Alzheimers). • JNKs and p38 are also called SAPK (Stress activated protein kinase) which gets activated on any stress. It help the cells to survive under any condition.
- 17. BRAF inhibitor:- Venurafenib, Dabarafenib Kinase inhibitor:- Sorafenib RTK inhibitor:- Gefitinib, Erlotinib