Inhibition of Nonfunctional Ras

Ruth Nussinov; Hyunbum Jang; Attila Gursoy; Ozlem Keskin; Vadim Gaponenko

doi:10.1016/j.chembiol.2020.12.012

Inhibition of Nonfunctional Ras

Ruth Nussinov^*, Hyunbum Jang, Attila Gursoy, Ozlem Keskin, Vadim Gaponenko^*

^*Corresponding author for this work

Human Molecular Genetics Biochemistry

Research output: Contribution to journal › Review article › peer-review

24 Scopus citations

Abstract

Nussinov et al. describe that the mechanism of mutational activation of kinases differs from Ras. Drug action should relate to the mechanism of activation, not to whether the protein is in active or inactive state. However, allosterically blocking the functional site will work for the inactive kinase and active Ras.

Original language	English
Pages (from-to)	121-133
Number of pages	13
Journal	Cell Chemical Biology
Volume	28
Issue number	2
DOIs	https://doi.org/10.1016/j.chembiol.2020.12.012
State	Published - 18 Feb 2021

Funding

Funders	Funder number
National Institutes of Health	HHSN261200800001E
U.S. Department of Health and Human Services
National Cancer Institute	ZIABC010441
NIH Clinical Center
Government of South Australia

Keywords

K-Ras4B
KRAS
dimer
drug discovery
energy landscape
inhibitor
kinases

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.chembiol.2020.12.012

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abstract = "Nussinov et al. describe that the mechanism of mutational activation of kinases differs from Ras. Drug action should relate to the mechanism of activation, not to whether the protein is in active or inactive state. However, allosterically blocking the functional site will work for the inactive kinase and active Ras.",

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author = "Ruth Nussinov and Hyunbum Jang and Attila Gursoy and Ozlem Keskin and Vadim Gaponenko",

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KW - energy landscape

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Inhibition of Nonfunctional Ras

Abstract

Funding

Keywords

UN SDGs

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