Accelerating the Validation of Endogenous On-Target Engagement and In Cellulo Kinetic Assessment for Covalent Inhibitors of KRAS<sup>G12C</sup> in Early Drug Discovery-Reference-Cited by-同舟云学术

Accelerating the Validation of Endogenous On-Target Engagement and In Cellulo Kinetic Assessment for Covalent Inhibitors of KRAS^G12C in Early Drug Discovery

Published:2022-07-26 Issue:8 Volume:17 Page:2366-2376
ISSN:1554-8929
Container-title:ACS Chemical Biology
language:en
Short-container-title:ACS Chem. Biol.

Author:

Kantae Vasudev¹,Polanski Radoslaw¹,Lewis Hilary J.²^ORCID,Haider Afreen¹,Barratt Derek¹,Srinivasan Bharath¹^ORCID

Affiliation:

1. Mechanistic and Structural Biology, Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, U.K.

2. Oncology R&D, AstraZeneca, Cambridge CB21 6GH, U.K.

Publisher

American Chemical Society (ACS)

Subject

Molecular Medicine,General Medicine,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acschembio.2c00483

Reference31 articles.

1. Fragment-based covalent ligand discovery

2. Osimertinib (AZD9291)—a science-driven, collaborative approach to rapid drug design and development

3. Amgen overcomes historically undruggable target, with FDA nod for first KRAS inhibitor

4. High-Throughput Mass Spectrometric Analysis of Covalent Protein-Inhibitor Adducts for the Discovery of Irreversible Inhibitors

5. A Perspective on the Kinetics of Covalent and Irreversible Inhibition

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