Nucleotidase
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The document summarizes the development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold. It discusses the function of ectonucleotidases in hydrolyzing extracellular nucleotides. It then describes the synthesis and optimization of anthraquinone derivatives as inhibitors of ecto-5'-nucleotidase through structure-activity relationships. The most potent compounds showed submicromolar inhibition selectively for ecto-5'-nucleotidase over other ectonucleotidases and P2 receptors, indicating potential for cancer treatment.
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![Function of ectoNucleotidases Extracellular Nucleotide Triphosphates -Diphosphates -Monophosphates [ATP,AMP,UDP,UMP,GMP] Source of Extracellular nucleotides ,[object Object]](data:image/gif;base64,R0lGODlhAQABAIAAAAAAAP///yH5BAEAAAAALAAAAAABAAEAAAIBRAA7)
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Peptide nucleic acid
This document provides an overview of peptide nucleic acids (PNA), including their history, structure, properties, applications, and advantages over DNA and RNA. Some key points:
1. PNA was invented in 1991 as a synthetic DNA analogue where the phosphodiester backbone is replaced with a pseudopeptide backbone. This makes PNA more stable and allows it to bind more strongly to DNA/RNA.
2. PNA has a higher melting temperature when binding to DNA/RNA compared to DNA-DNA binding due to its uncharged backbone. It is also resistant to degradation by enzymes.
3. PNA can be used for applications like antisense therapy, molecular beacons, DNA microarrays
Recombinant protein
The document discusses recombinant proteins, including their production through recombinant DNA technology. It describes how genes can be isolated and inserted into expression vectors, which are then transferred into host cells to produce the recombinant protein. Various methods are covered, including molecular cloning and polymerase chain reaction. Examples of recombinant proteins discussed include insulin, interferons, hormones, and monoclonal antibodies that are used for medical applications.
Recombinant protein
The document discusses recombinant proteins, including their production through recombinant DNA technology. It describes how genes can be isolated and inserted into expression vectors, which are then transferred into host cells to produce the recombinant protein. Various methods are covered, including molecular cloning and polymerase chain reaction. Examples of recombinant proteins discussed include insulin, interferons, hormones, and monoclonal antibodies that are used for medical applications.
CAMP poster
1) The document discusses a method for the synthesis of naphthylisoquinoline alkaloids via thiolate demethylation and benzylation. Demethylation of 1-chloro-3, 5-dimethoxybenzene provides a precursor for the secondary benzylation step.
2) Experiments tested different thiolates for the demethylation reaction, finding sodium methylthiolate (Entry 5) was most successful, yielding the desired product in 78% by NMR.
3) The benzylation reaction achieved 11% yield but product separation posed challenges. Reaction conditions for both demethylation and benzylation are still being optimized to maximize yields.
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Nucleotidase
- 1. Development of Potent & Selective Inhibitors of ecto -5ʹ-Nucleotidase Based on an Anthraquinone Scaffold KORA UPENDRA REDDY 2010H146037H 18 April 2011 1
- 6. Damaged/dying cellsNucleosides 18 April 2011 2
- 7. Families of ectonucleotidases Ectonucleoside triphosphate diphosphohydrolases (E-NTPDase). Ectonucleotide pyrophosphate/phosphodiesterases (E-NPPS). Alkaline phosphatases. Ecto-5ʹ -nucleotidase. 18 April 2011 3
- 11. immune response
- 16. differentiation
- 18. A2a
- 19. A2b
- 20. A318 April 2011 4
- 21. 18 April 2011 5
- 22. 18 April 2011 6
- 23. 18 April 2011 7
- 24. Ectonucleotidase role in Tumor growth 18 April 2011 8 LPC=lysophosphotidyl choline LPA=lysophosphotidic acid
- 25. eN Inhibitors 18 April 2011 9
- 27. copper powder
- 28. microwave irradiation at 100-120 ͦ C
- 29. time =5 to 24 min18 April 2011 10
- 30. 18 April 2011 11
- 31. 18 April 2011 12 SAR
- 32. Lead molecule 18 April 2011 13
- 33. Molecular modeling 18 April 2011 14
- 35. High substrate concentrations were used because of low sensitivity
- 36. Quantifying product: Adenosine
- 37. Ki values calculated by using IC-50 values18 April 2011 15
- 38. Selectivity 18 April 2011 16
- 40. Intercalate into DNA
- 41. Inhibit DNA topoisomerase II complex
- 42. Form reactive oxygen speciesLacking phenolic basic side chains found to be non toxic 18 April 2011 17
- 44. Most potent compounds proved to be selective versus other ectonucleotidases & P2 receptors
- 45. Treatment for cancers
- 46. Anthraquinone scaffold appears to be privileged structure of nucleotide binding protein targets18 April 2011 18