Title:Recent Trends in Rationally Designed Molecules as Kinase Inhibitors
Volume: 30
Issue: 13
Author(s): Parteek Prasher*, Mousmee Sharma, Yinghan Chan, Sachin Kumar Singh, Krishnan Anand, Harish Dureja, Niraj Kumar Jha, Gaurav Gupta, Flavia Zacconi, Dinesh K. Chellappan and Kamal Dua*
Affiliation:
- Department of Chemistry, University of Petroleum & Energy Studies, Dehradun 248007, India
- Discipline of Pharmacy, Graduate School of Health, University of Technology
Sydney, NSW 2007, Australia
Keywords:
Kinases, cancer, pharmacophore, inhibitors, GPCR kinase, VEGFR-2, RAF-kinase, MAP kinase, cyclic dependent kinase.
Abstract: Protein kinases modulate the structure and function of proteins by adding phosphate
groups to threonine, tyrosine, and serine residues. The phosphorylation process mediated
by the kinases regulates several physiological processes, while their overexpression results
in the development of chronic diseases, including cancer. Targeting of receptor tyrosine
kinase pathways results in the inhibition of angiogenesis and cell proliferation that validates
kinases as a key target in the management of aggressive cancers. As such, the identification
of protein kinase inhibitors revolutionized the contemporary anticancer therapy by
inducing a paradigm shift in the management of disease pathogenesis. Contemporary drug
design programs focus on a broad range of kinase targets for the development of novel
pharmacophores to manage the overexpression of kinases and their pathophysiology in cancer
pathogenesis. In this review, we present the emerging trends in the development of rationally
designed molecular inhibitors of kinases over the last five years (2016-2021) and
their incipient role in the development of impending anticancer pharmaceuticals.
