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Sampurna Chakrabarti and Malcolm M. Slaughter characterized the effects of Ginkgolide B (GB) as an antagonist of alpha 3 glycine receptors. They expressed homomeric alpha 3 glycine receptors in HEK 293 cells and used whole-cell patch clamping to record GB's effects. They found that GB can pharmacologically differentiate alpha 3 glycine receptors and has more than one binding site, both inside and outside the pore. GB blockade of alpha 3 glycine receptors is voltage sensitive and recovers faster in the unliganded state compared to the liganded state. In summary, GB serves as a tool to selectively study alpha 3 glycine receptors and helps understand their role in the visual
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Gifasp for Expo “La cultura della protezione e della sostenibilità”. Report
Business initiatives to user stories implementation reality
Business initiatives to user stories implementation reality
Similar to BrockportPresentationSHORT
PHd defense presentation Final RIVES
The document discusses the functional interaction between mGlu1a and GABAB receptors. It first provides background on G protein-coupled receptors and their importance as drug targets. It then reviews evidence that mGlu1a and GABAB receptors physically interact in cortical neurons and Purkinje cells based on co-localization and co-immunoprecipitation studies. The study aims to further investigate the physical interaction between the receptors and the mechanism underlying their functional cross-talk using biophysical techniques like BRET, TR-FRET, and cell-surface co-immunoprecipitation. Preliminary data suggests mGlu1a and GABAB do not form complexes at the cell surface but may oligomerize intracellularly.
Zack Brittingham Poster draft 121014 Updated-2
GBA activity was assessed in cell lines with and without GBA knockout. Activity decreased in a dose-dependent manner with CBE treatment but not ambroxol or isofagomine after short incubation. Mutant B lymphocytes and fibroblasts generally had lower GBA levels and activity than controls, with some donor variability. Treatment of A53T transgenic mouse neurons with ambroxol and isofagomine decreased α-synuclein levels, indicating potential as chaperones to increase GBA activity and reduce α-synuclein aggregates.
Poster Presentation GABA
The document summarizes research investigating the role of GABA in visual processing in the retina. It finds that:
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2) Experiments on isolated catfish horizontal cells found that applying GABA sometimes caused an increase in extracellular acidity and sometimes an alkalization, likely through GABA receptors and transporters on the cells.
3) It is proposed that GABA regulation of pH involves cell depolarization opening calcium channels, increasing intracellular calcium and triggering a calcium pump that moves protons out of the cell.
GABA-ACs Chem Bio
1. The document reports on the mechanism of inactivation of GABA aminotransferase (GABA-AT) by (E)- and (Z)-(1S,3S)-3-amino-4-fluoromethylenyl-1-cyclopentanoic acid (1 and 2).
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3. This confirms the importance of Arg445 in the active site of GABA-AT for ligand interaction and enzyme inactivation, informing the design of new GABA-AT in
GABA-AT_2
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2. Both inactivators produce a metabolite that disrupts the Glu270-Arg445 salt bridge in GABA-AT, allowing interaction between the metabolite's formyl group and Arg445.
3. This confirms the importance of Arg445 in the active site of GABA-AT for ligand interaction and enzyme inactivation, informing the design of new GABA-AT in
Receptors
This document discusses different types of receptors. It describes G-protein coupled receptors (GPCRs) in detail, including that they are the largest group of receptors, mediate many physiological processes, and are targets for around 45% of drugs. It provides examples of specific GPCRs like muscarinic, adrenergic, histamine, dopamine, opioid, and serotonin receptors and discusses their functions. The document also briefly summarizes ligand-gated ion channels, enzymatic receptors, and nuclear receptors. In summary, it provides an overview of the main receptor types, with a focus on GPCRs, their examples, signaling pathways, and physiological roles.
GABA-AT_3
1) The document describes the design and testing of new GABA analogues that could inactivate the enzyme GABA-aminotransferase (GABA-AT) by a ring-opening mechanism.
2) Compound 17 was found to be the most potent inactivator of GABA-AT, being 8 times more effective than the current drug vigabatrin.
3) X-ray crystallography studies showed that compound 17 inactivates GABA-AT via a new mechanism, forming a buckled five-membered ring bound to the active site without covalently modifying amino acids.
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.
Gaba ppt
This document discusses GABA (gamma-aminobutyric acid), the primary inhibitory neurotransmitter in the mammalian central nervous system. It outlines GABA's mechanism of action via GABA-A and GABA-B receptors, synthesis, functions in relieving anxiety and improving mood, and relationship to health conditions like insomnia, depression, seizures, and panic disorders when deficient. The conclusion states that GABA functions to inhibit nerve impulses by blocking them, preventing nerve cells from firing too often or easily.
Molecular Pharmacology-Receptor Desensitization
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GABA.pptx
This document discusses GABA, the major inhibitory neurotransmitter in the mammalian central nervous system. It covers GABA's synthesis, receptors (GABA-A and GABA-B), and role in neuropsychiatric conditions like anxiety disorders, mood disorders, schizophrenia, and epilepsy. Specifically, it notes that GABA serves an important regulatory role by reducing neuronal activity in areas like the amygdala and cortico-striatal-thalamo-cortical loop. Dysfunction of GABA signaling has been linked to these conditions.
Gaba seminar
The document summarizes information about neurotransmitters, with a focus on GABA. It discusses the three main types of GABA receptors:
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3) GABA-C receptors, which are newly discovered transmitter-gated chloride channels that are insensitive to typical GABA receptor modulators.
The document also reviews the mechanisms of action, structures, and pharmacology of the different G
General Pharmacodynamics
This document discusses pharmacodynamics, which is how drugs act on the body through their mechanisms of action and effects. It provides details on the molecular aspects of specific drug action, including the main targets such as DNA, microbial organelles, and target macroproteins like receptors, ion channels, enzymes, and carrier molecules. Drugs can act through specific binding to these targets or through non-specific effects. The summary describes the four main types of receptors - ionotropic, G-protein coupled, tyrosine kinase-linked, and nuclear receptors - and how they mediate drug effects through different intracellular signaling pathways and timescales. Dose-response relationships and factors affecting drug concentration at the site of action are also introduced.
ILQ and LQ Poster (1)
This study investigated the effects of beta-estradiol and plant-derived estrogen receptor beta agonists liquiritigenin and isoliquiritigenin on glioblastoma cell proliferation. Individually, the compounds showed weak inhibition of cell growth. However, combinations of beta-estradiol with either liquiritigenin or isoliquiritigenin strongly inhibited cell growth, indicating a synergistic effect. These findings suggest that combinations of these compounds could be useful in clinical applications for glioblastoma.
GABAB receptor-mediated selective peripheral analgesia by the non-proteinogen...
1) The document examines the hypothesis that the amino acid isovaline produces peripheral analgesia through GABAB receptors without affecting the central nervous system.
2) Experiments in mice found that isovaline, like the GABAB agonists baclofen and GABA, reduced pain-related behavior induced by prostaglandin E2 injection into the paw in a GABAB receptor-dependent manner, but unlike baclofen, isovaline did not produce sedation or hypothermia indicating a lack of central effects.
3) Immunohistochemistry revealed co-localization of GABAB1 and GABAB2 receptor subunits on fine nerve endings and keratinocytes in skin
Similar to BrockportPresentationSHORT (16)
GABAB receptor-mediated selective peripheral analgesia by the non-proteinogen...
GABAB receptor-mediated selective peripheral analgesia by the non-proteinogen...
BrockportPresentationSHORT
- 1. Sampurna Chakrabarti, Malcolm M. Slaughter (Faculty mentor) University at Buffalo, Dept. of Biology and Dept. of Psychology University at Buffalo, Dept. of Physiology and Biophysics Characterization of Ginkgolide B as an Antagonist of Alpha 3 Glycine Receptors
- 2. Terminology Receptors- Protein molecules in plasma membrane responsible for chemical signaling. Glycine Receptors (GlyRs)-Ionotropic receptor, inhibitory neurotransmission, 5 subunits : 2 alpha (1-4) and 3 beta. Antagonists- Ligands that diminish the effects of Glycine Ginkgolide B (GB)
- 3. Ginkgolide B (GB) Extracted from roots and barks of Ginkgo biloba Platelet Activating Factor Treating cardiovascular diseases, migraine attacks Antagonist of GABA Receptors and alpha1, alpha2 GlyRs
- 4. The Big Question Why are there so many Glycine Receptor subunits in the retina and how are they different?
- 5. Goals Characterize Ginkgolide B (GB) block on homomeric alpha 3 Glycine Receptors (GlyRs) Identify binding site/s of the antagonist Highlight unique properties of alpha 3 GlyRs
- 6. Methods Expressed alpha 3 GlyRs in HEK 293 cell by transfection Identified transfected cells by GFP using fluorescence microscopy Recorded via whole cell patch clamping Micropipette tip in HEK 293 cells
- 7. Experimental Design Gly (establish baseline) – 2 s GB only (10s) GB + Gly (10 s) Wash (variable time) Wash (variable time) Gly (test for suppression) Gly (test for suppression) LigandedUnliganded
- 8. GB as pore blocker in Alpha 2 GlyRs 30%
- 9. GB blocks homomeric alpha 3 GlyRs in unliganded state -10 mV -50 mV 200 pA
- 10. Conclusion I GB can pharmacologically differentiate alpha 3 GlyRs
- 11. Voltage Sensitivity of GB In Alpha 3 GlyR
- 12. Alpha 3 GB block– Unliganded vs Liganded -10 mV
- 13. Recovery Rates in Liganded vs Unliganded states p<0.001, n=5 at -10 mV
- 14. Alpha 3 GB block– Unliganded vs Liganded -50 mV
- 15. Conclusion II GB has more than one binding site both inside and outside the pore Pore + Outside = Liganded Slow recovery Outside only = Unliganded Fast recovery
- 16. Summary GB can serve as a tool to selectively isolate alpha 3 GlyRs and can help us understand their role in the visual system
- 17. Next Step Cite Directed Mutagenesis
- 18. References 1. Durisic, Nela, et al. "Stoichiometry of the Human Glycine Receptor Revealed by Direct Subunit Counting." The Journal of Neuroscience 32.37 (2012): 12915-20. Print. 2. Hawthorne, Rebecca, et al. "Molecular Determinants of Ginkgolide Binding in the Glycine Receptor Pore." Journal of Neurochemistry 98.2 (2006): 395-407. Print. 3. Heads, Judith A., et al. "Structure-Activity Analysis of Ginkgolide Binding in the Glycine Receptor Pore." Journal of Neurochemistry 105.4 (2008): 1418-27. Print. 4. Huang, Shelley H., et al. "Ginkgolides, Diterpene Trilactones of Ginkgo Biloba, as Antagonists at Recombinant Α1β2γ2l Gabaa Receptors." European Journal of Pharmacology 494.2–3 (2004): 131-38. Print
Editor's Notes
- Our lab is interested in the neurobiology of the retina and seeks to understand what each receptor and their subunit play in visual pathways. For this project we are trying to answer the question why are there 5 GlyR subunits and what funcs they perform.
- We approach this proble
- Insert implication after this
- Another way of looking at the binding sites of GB in a3 is to see if it is voltage sensitive. Voltage sensitivity simply means the behavior of the drug changes when the internal voltage fo the cell is changed. If GB is able to detect change in voltage it means that it binds somewhere near the pore. We see here that at -10 mV GB acts a lot better than at -50 mV. This bar graph shows that there is a statistical significance between points 1 and 3 when the drug just starts acting and 2 and 4 which is a fixed interval later. This result suggest that a3, in addition to having a out-of-pore binding site, also has a binding site near the pore.
- To further look at the unique properties of a3 we look at the recovery rate from liganded and unliganded GB application. If you look at the gly current after 15 s wash you can see that in unliganded state it is as big as the control current, or fully recovered. But in liganded state, it is still 40% suppressed.
- This bar graph highlghts the result that recovery from liganded state is slower than unliganded state after 5, 10 and 15 s wash time.
- This is showing the same experiment now at -50 mV. The rate of recovery from liganded state is still slower but the difference between the two rates are less apparent.
- From the results we propose that GB has two binding sites one inside and the other outside the pore. The pore binding site is accessible only during liganded state so the recovery from liganded state is slower. Again at -50 mV GB doesn’t block the pore binding site well, so the liganded recovery from -50 mV is faster than at -10 mV.