IMR Press / FBL / Volume 25 / Issue 8 / DOI: 10.2741/4864

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Orthosteric and allosteric modulation of human kinases: A mechanistic view
Show Less
1 Amity Institute of Biotechnology, Amity University Uttar Pradesh, Noida, Uttar Pradesh, India
Send correspondence to: Puniti Mathur, Amity Institute of Biotechnology, Amity University Uttar Pradesh, Noida, Uttar Pradesh, India, Tel: 0120-439-2204, Fax: 0120-439-2947, E-mail:
Front. Biosci. (Landmark Ed) 2020, 25(8), 1462–1487;
Published: 1 March 2020
(This article belongs to the Special Issue Structural genomics of human kinome)

Human kinases represent a large family of enzymes with their primary function being the phosphorylation of various biomolecules. Kinases along with G-Protein Coupled Receptors (GPCRs) represent two of the most common protein targets in drug discovery. Kinases are classified by the substrate they phosphorylate namely, protein kinases, carbohydrate kinases and lipid kinases. These different classes have unique mechanism of action but show considerable overlap in their structural assembly and sequence of chemical modifications. Compounds can modulate kinase activity by interacting with the enzyme’s ATP binding site (orthosteric site) or the allosteric site. These modulators have been classified as Types I, II, III and IV depending on their mode of binding. Inclusion of atypical kinases and pseudokinases in the targetable kinome along with the recent approval of kinase-based therapeutics provides an impetus to the ever-growing field of kinase modulation. This review attempts to summarize the identification, historical stance, catalytic structure and subsequent development of kinases as significant drug targets with an emphasis on their catalytic machinery and modulation.

Kinase modulation
Kinase Drugs
Kinase review
Kinase mechanism
Figure 1
Back to top