Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors
MetadataShow full item record
There 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 SAS
European Journal of Medicinal Chemistry
Showing items related by title, author, creator and subject.
Gill, Balraj Singh; Navgeet; Mehra, Richa; Kumar, Vicky; Kumar, Sanjeev (Springer New York LLC, 2018)Cancer is a multifactorial disease, causing behavioral and metabolic alterations, leading to uncontrolled cell proliferation with collateral weakening of immune system. Crucial balance between cell proliferation and cell ...
Kumar, Bhupinder; Singh, Sandeep; Skvortsova, Ira; Kumar, Vinod (Bentham Science Publishers B.V., 2017)Cancer is a multifactorial disease and its genesis and progression are extremely complex. The biggest problem in the anticancer drug development is acquiring of multidrug resistance and relapse. Classical chemotherapeutics ...
Khetarpal, Preeti; Das, Satrupa; Panigrahi, Inusha; Munshi, Anjana (Springer Verlag, 2016)Primordial dwarfism is a group of genetic disorders which include Seckel Syndrome, Silver?Russell Syndrome, Microcephalic Osteodysplastic Primordial Dwarfism types I/III, II and Meier?Gorlin Syndrome. This genetic disorder ...