Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules-Reference-Cited by-同舟云学术

Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules

Published:2024 Issue: Volume: Page:
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Acharya Baku¹,Saha Debasmita¹²,Armstrong Daniel¹,Jabali Baha'a¹,Hanafi Maha¹³,Herrera-Rueda Alan¹,Lakkaniga Naga Rajiv⁴,Frett Brendan¹^ORCID

Affiliation:

1. Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR, USA

2. Conrad Prebys Centre for Chemical Genomics, Sanford Burnham Prebys Medical Discovery Institute, San Diego, CA, USA

3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11526, Egypt

4. Department of Chemistry and Chemical Biology, Indian Institute of Technology (Indian School of Mines), Dhanbad, India

Abstract

The development of macrocycles has emerged as an innovative approach to improve kinase inhibitor selectivity, as well as pharmacokinetic and pharmacodynamic properties.

Funder

National Institutes of Health

University of Arkansas for Medical Sciences

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2024/MD/D3MD00457K

Reference92 articles.

1. Raf kinases in cancer–roles and therapeutic opportunities

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3. Mutational Analysis of the Tyrosine Kinome in Colorectal Cancers

4. Driver mutations in the mitogen‐activated protein kinase pathway: the seeds of good and evil

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