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Abstract

Modern Approaches in Drug Designing

Cyclin Dependent Kinase Inhibitors as Drug Targets for Cancer-A Reviewmacological Molecule Modify Strategy- New Algorithm

  • Open or CloseM Krishnaveni*

    Department of Biochemistry, Periyar University, India

    *Corresponding author: M Krishnaveni, Assistant Professor, Department of Biochemistry, Periyar University, Salem-636 011, India

Submission: September 18, 2017; Published: October 11, 2017

DOI: 10.31031/MADD.2017.01.000503

ISSN: 2576-9170
Volume1 Issue1

Abstract

Cyclin dependent kinases are proline directed serine / threonine protein kinases comprising of catalytic CDK subunit and active cyclin subunit. Till now around 25 different cyclins and 13 different cyclin dependent kinases are reported but only 7 CDK’s play a major role in the progression of cell cycle. Usually throughout cell cycle, cyclin levels vary and CDK remains constant. Complete activation of cyclin dependent kinases takes place by the phosphorylation of threonine residue close to kinase active site. Cyclin dependent kinases phosphorylate various substrates that are required for the progression of cell cycle. The eukaryotic cell growth and cell division are regulated at late G1, G2/M, metaphase to anaphase transition (check points). The first two check points are controlled by cyclin dependent kinases and are specific for each phase like CDK 4, 6 controls late G1 and S phase by CDK2 and CDK 1, while G2/M and last by anaphase promoting complex. Cyclin D interaction with CDK 4 regulates S phase initially, apart from this CDK 4/6 regulation at transcriptional level controls late G1 phase. Loss of cell cycle control, hyper-activation of cyclin dependent kinases due to mutation causes cancer. So, inhibitions of cyclin dependent kinases are targets in cancer therapy. The inhibitors of cyclin dependent kinases are ATP-competitive, ATP-noncompetitive (including some small mimetic peptides for p21, p27 and p57), Allosteric inhibitors. Let us have a look on some of the inhibitors in this review.

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