Therapeutic Targeting the Allosteric Cysteinome of RAS and Kinase Families

• Published in: Journal of molecular biology Vol. 434; no. 17; p. 167626
• Main Authors: Li, Lianbo, Meyer, Cynthia, Zhou, Zhi-Wei, Elmezayen, Ammar, Westover, Kenneth
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier Ltd 15.09.2022
• Subjects: allosteric inhibitor; cancer therapy; chemistry; covalent inhibitor; cysteine; cysteinome; drug development; drugs; humans; kinase inhibitor; KRAS inhibitor; ligands; molecular biology; kinase inhibitor; cysteinome; allosteric inhibitor; KRAS inhibitor; covalent inhibitor

[Display omitted] •Allosteric inhibitors have many theoretical advantages including superior selectivity, the ability to modulate allosteric biological processes, and the ability to fine-tune biological responses.•Allosteric KRAS G12C inhibitor development showed that covalent chemistry can convert...