High-throughput screening assays for cyclooxygenase-2 and 5-lipoxygenase, the targets for inflammatory disorders.

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dc.contributor.authorKumar, K Anil
dc.contributor.authorReddy, T Chandramohan
dc.contributor.authorReddy, Gorla V
dc.contributor.authorReddy, D Bharat Kumar
dc.contributor.authorMahipal, S V K
dc.contributor.authorSinha, Sudhir
dc.contributor.authorGaikwad, Anil N
dc.contributor.authorReddanna, P
dc.date.accessioned2011-11-16T05:52:07Z
dc.date.available2011-11-16T05:52:07Z
dc.date.issued2011-08
dc.description.abstractHigh-throughput screening (HTS) involves testing of compound libraries against validated drug targets using quantitative bioassays to identify ‘hit’ molecules that modulate the activity of target, which forms the starting point of a drug discovery effort. Eicosanoids formed via cyclooxygenase (COX) and lipoxygenase (LOX) pathways are major players in various inflammatory disorders. As the conventional non-steroidal anti-inflammatory drugs (NSAIDs) that inhibit both the constitutive (COX-1) and the inducible (COX-2) isoforms have gastric and renal side effects and the recently developed COX-2 selective anti-inflammatory drugs (COXIBs) have cardiac side effects, efforts are being made to develop more potent and safer anti-inflammatory drugs. Current assay methods for these enzymes, such as oxygraphic, radioisotopic, spectrophotometric etc. are not compatible for screening of large number of compounds as in drug discovery programs. In the present study, HTS-compatible assays for COX-1, COX-2 and 5-LOX were developed for screening of compound libraries with the view to identify potential anti-inflammatory drug candidates. A spectrophotometric assay involving co-oxidation of tetramethyl-p-phenylene diamine (TMPD) during the reduction of prostaglandin G2 (PGG2) to PGH2 was adopted and standardized for screening of compounds against COX-1 and COX-2. Similarly, the HTS-compatible FOX (ferrous oxidation-xylenol orange) based spectrophotometric assay involving the formation of Fe3+/xylenol orange complex showing absorption in the visible range was developed for screening of compounds against 5-LOX.en_US
dc.identifier.citationKumar K Anil, Reddy T Chandramohan, Reddy Gorla V, Reddy D Bharat Kumar, Mahipal S V K, Sinha Sudhir, Gaikwad Anil N, Reddanna P. High-throughput screening assays for cyclooxygenase-2 and 5-lipoxygenase, the targets for inflammatory disorders. Indian Journal of Biochemistry & Biophysics. 2011 Aug; 48(4): 256-261.en_US
dc.identifier.urihttps://imsear.searo.who.int/handle/123456789/135326
dc.language.isoenen_US
dc.source.urihttps://nopr.niscair.res.in/bitstream/123456789/12700/1/IJBB%2048%284%29%20256-261.pdfen_US
dc.subjectHigh-throughput screeningen_US
dc.subjectCyclooxygenaseen_US
dc.subjectLipoxygenaseen_US
dc.subjectNSAIDsen_US
dc.subjectCOXIBsen_US
dc.subjectCLOXIBsen_US
dc.subject.meshAnimals
dc.subject.meshArachidonate 5-Lipoxygenase --metabolism
dc.subject.meshCyclooxygenase 2 --metabolism
dc.subject.meshCyclooxygenase 2 Inhibitors --pharmacology
dc.subject.meshCyclooxygenase 2 Inhibitors --therapeutic use
dc.subject.meshInflammation --drug therapy
dc.subject.meshInflammation --enzymology
dc.subject.meshInhibitory Concentration 50
dc.subject.meshLipoxygenase Inhibitors --pharmacology
dc.subject.meshLipoxygenase Inhibitors --therapeutic use
dc.subject.meshSpodoptera
dc.titleHigh-throughput screening assays for cyclooxygenase-2 and 5-lipoxygenase, the targets for inflammatory disorders.en_US
dc.typeArticleen_US
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