Peptidomimetic Design of CDK Inhibitors Targeting theRecruitment Site of the Cyclin Subunit

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Peptidomimetic Design of CDK Inhibitors Targeting theRecruitment Site of the Cyclin Subunit

Anti-Cancer Agents in Medicinal Chemistry, 3(1): 57-69.

Author(s): David P. Lane and Peter M Fischer.

Affiliation: Cyclacel Limited, James Lindsay Place, Dundee DD1 5JJ, Scotland, UK.


The recognition of cyclin-dependent kinase (CDK) / cyclin complexes by various cell-cycle regulatory proteins, including certain tumour suppressors and transcription factors, occurs at least in part through a protein-protein interaction with a binding groove on the cyclin subunit. Since CDK function is generally deregulated in tumour cells, blocking of this recruitment site prevents recognition and subsequent phosphorylation of CDK substrates and offers a therapeutic approach towards restoration of checkpoint control in transformed cells. Here we discuss the finding that peptides derived from such cyclin-interacting proteins, and rendered permeable through conjugation to cellular delivery vectors, can apparently induce tumour cells to undergo apoptosis selectively. We review the current status of 3D-structural information available on cyclin-peptide interactions and we summarise our extensive peptide structure-activity relationship studies in light of this information. We also show how a combination of molecular modelling and introduction into synthetic peptides of peptidomimetic elements, such as non-natural amino acid residues and conformational constraints, is being used hopefully to arrive at drug candidates capable of modulating CDK function in a selective mechanism-based approach rather than through ATP antagonism.


Peptidomimetic, CDK Inhibitors, Cyclin, protein-protein interaction.

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Article Details

Volume: 3
Issue Number: 1
First Page: 57
Last Page: 69
Page Count: 13
DOI: 10.2174/1568011033353506
Global Biotechnology Congress 2017Drug Discovery and Therapy World Congress 2017

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