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Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors

dc.contributor.authorKalra, Sourav
dc.contributor.authorJoshi, Gaurav
dc.contributor.authorMunshi, Anjana
dc.contributor.authorKumar, Raj
dc.date.accessioned2017-01-15T16:09:10Z
dc.date.available2017-01-15T16:09:10Z
dc.date.issued2017
dc.identifier.citationKalra, S., Joshi, G., Munshi, A., & Kumar, R. (2017). Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. European Journal of Medicinal Chemistry, 142, 424-458. doi: 10.1016/j.ejmech.2017.08.071en_US
dc.identifier.issn2235234
dc.identifier.urihttp://kr.cup.edu.in/handle/32116/388
dc.description.abstractThere are around 20 Cyclin-dependent kinases (CDKs) known till date, and various research groups have reported their role in different types of cancer. The X-ray structures of some CDKs especially CDK2 was exploited in the past few years, and several inhibitors have been found, e.g., flavopiridol, indirubicin, roscovitine, etc., but due to the specificity issues of these inhibitors (binding to all CDKs), these were called as pan inhibitors. The revolutionary outcome of palbociclib in 2015 as CDK4/6 inhibitor added a new charm to the specific inhibitor design for CDKs. Computer-aided drug design (CADD) tools added a benefit to the design and development of new CDK inhibitors by studying the binding pattern of the inhibitors to the ATP binding domain of CDKs. Herein, we have attempted a comparative analysis of structural differences between several CDKs ATP binding sites and their inhibitor specificity by depicting the important ligand-receptor interactions for a particular CDK to be targeted. This perspective provides futuristic implications in the design of inhibitors considering the spatial features and structural insights of the specific CDK. ? 2017 Elsevier Masson SASen_US
dc.language.isoen_USen_US
dc.publisherElsevier Masson SASen_US
dc.subjectCyclin dependent kinaseen_US
dc.subjectCyclin dependent kinase 1en_US
dc.subjectCyclin dependent kinase 12en_US
dc.subjectCyclin dependent kinase 13en_US
dc.subjectCyclin dependent kinase 16en_US
dc.subjectCyclin dependent kinase 2en_US
dc.subjectCyclin dependent kinase 4en_US
dc.subjectCyclin dependent kinase 5en_US
dc.subjectCyclin dependent kinase 6en_US
dc.subjectCyclin dependent kinase 7en_US
dc.subjectCyclin dependent kinase 8en_US
dc.subjectCyclin dependent kinase 9en_US
dc.subjectCyclindependent kinase inhibitoren_US
dc.subjectLiganden_US
dc.subjectUnclassified drugen_US
dc.subjectCyclin dependent kinaseen_US
dc.subjectProtein kinase inhibitoren_US
dc.subjectComparative studyen_US
dc.subjectDrug bindingen_US
dc.subjectDrug designen_US
dc.subjectDrug structureen_US
dc.titleStructural insights of cyclin dependent kinases: Implications in design of selective inhibitorsen_US
dc.typeReviewen_US
dc.identifier.doi10.1016/j.ejmech.2017.08.071
dc.identifier.urlhttps://www.sciencedirect.com/science/article/pii/S0223523417306827?via%3Dihub
dc.title.journalEuropean Journal of Medicinal Chemistry


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