A molecular perspective for the use of type IV tyrosine kinase inhibitors as anticancer therapeutics

Copyright © 2021 Elsevier Ltd. All rights reserved..

Tyrosine kinases are enzymes that can transfer a phosphate group from ATP to a specific protein tyrosine, serine or threonine residue within a cell, operating as a switch that can turn 'on' and 'off' causing different physiological alterations in the body. Mutated kinases have been shown to display an equilibrium shift toward the activated state. Types I-III have been studied intensively leading to drugs like imatinib (type II), cobimetinib (type III), among others. It is the same scenario for types V-VII; however, there is a lacuna in information regarding type IV inhibitors, although recently some advances have surfaced. This review aims to accumulate the knowledge gained so far about type IV inhibitors.

Medienart:

E-Artikel

Erscheinungsjahr:

2022

Erschienen:

2022

Enthalten in:

Zur Gesamtaufnahme - volume:27

Enthalten in:

Drug discovery today - 27(2022), 3 vom: 15. März, Seite 808-821

Sprache:

Englisch

Beteiligte Personen:

Das, Rudradip [VerfasserIn]
Choithramani, Asmita [VerfasserIn]
Shard, Amit [VerfasserIn]

Links:

Volltext

Themen:

42HK56048U
8A1O1M485B
Allosteric site
Cancer
EC 2.7.10.1
Imatinib Mesylate
Journal Article
Phosphorylation
Protein Kinase Inhibitors
Protein-Tyrosine Kinases
Review
Type IV inhibitor
Tyrosine
Tyrosine kinase

Anmerkungen:

Date Completed 20.04.2022

Date Revised 20.04.2022

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1016/j.drudis.2021.12.009

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM334562384