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Review Article

Recent Trends in Rationally Designed Molecules as Kinase Inhibitors

[ Vol. 30 , Issue. 13 ]


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*   Pages 1529 - 1567 ( 39 )


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.


Kinases, cancer, pharmacophore, inhibitors, GPCR kinase, VEGFR-2, RAF-kinase, MAP kinase, cyclic dependent kinase.


Department of Chemistry, University of Petroleum & Energy Studies, Dehradun 248007, Department of Chemistry, Uttaranchal University, Dehradun 248007, School of Pharmacy, International Medical University, Bukit Jalil 57000, Kuala Lumpur, School of Pharmacy and Pharmaceutical Science, Lovely Professional University, Department of Chemical Pathology, School of Pathology, Faculty of Health Sciences and National Health Laboratory Service, University of the Free State, Bloemfontein, Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak 124001, Department of Biotechnology, School of Engineering and Technology (SET), Sharda University, Greater Noida, 201310, UP, School of Pharmacy, Suresh Gyan Vihar University, Jaipur, Rajasthan, Departamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Av. Vicuña Mackenna 4860, Macul, Santiago 7820436, Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil 57000, Kuala Lumpur, Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, NSW 2007

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