Hitting KRAS When It’s Down

KRAS, one of the most prevalent oncogenes and sought-after anticancer targets, has eluded chemists for decades until an irreversible covalent strategy targeting a specific mutation (G12C) paved the way for the first KRAS inhibitors to reach the clinic. MRTX849 is one such clinical candidate with pro...

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Detalles Bibliográficos
Autores principales: Gabizon, Ronen, London, Nir
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7467708/
https://www.ncbi.nlm.nih.gov/pubmed/32568546
http://dx.doi.org/10.1021/acs.jmedchem.0c00785
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author Gabizon, Ronen
London, Nir
author_facet Gabizon, Ronen
London, Nir
author_sort Gabizon, Ronen
collection PubMed
description KRAS, one of the most prevalent oncogenes and sought-after anticancer targets, has eluded chemists for decades until an irreversible covalent strategy targeting a specific mutation (G12C) paved the way for the first KRAS inhibitors to reach the clinic. MRTX849 is one such clinical candidate with promising initial results in patients harboring the mutation. The impressive optimization story of MRTX849 highlights challenges and solutions in the development of covalent drugs, including the use of an α-fluoroacrylamide electrophile.
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spelling pubmed-74677082020-09-03 Hitting KRAS When It’s Down Gabizon, Ronen London, Nir J Med Chem KRAS, one of the most prevalent oncogenes and sought-after anticancer targets, has eluded chemists for decades until an irreversible covalent strategy targeting a specific mutation (G12C) paved the way for the first KRAS inhibitors to reach the clinic. MRTX849 is one such clinical candidate with promising initial results in patients harboring the mutation. The impressive optimization story of MRTX849 highlights challenges and solutions in the development of covalent drugs, including the use of an α-fluoroacrylamide electrophile. American Chemical Society 2020-06-22 2020-07-09 /pmc/articles/PMC7467708/ /pubmed/32568546 http://dx.doi.org/10.1021/acs.jmedchem.0c00785 Text en Copyright © 2020 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Gabizon, Ronen
London, Nir
Hitting KRAS When It’s Down
title Hitting KRAS When It’s Down
title_full Hitting KRAS When It’s Down
title_fullStr Hitting KRAS When It’s Down
title_full_unstemmed Hitting KRAS When It’s Down
title_short Hitting KRAS When It’s Down
title_sort hitting kras when it’s down
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7467708/
https://www.ncbi.nlm.nih.gov/pubmed/32568546
http://dx.doi.org/10.1021/acs.jmedchem.0c00785
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