Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling-Reference-Cited by-同舟云学术

Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling

Published:2021 Issue:48 Volume:12 Page:15975-15987
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Lim Shuhui¹,Boyer Nicolas²^ORCID,Boo Nicole¹,Huang Chunhui²,Venkatachalam Gireedhar¹,Angela Juang Yu-Chi¹,Garrigou Michael²,Kaan Hung Yi Kristal¹,Duggal Ruchia²,Peh Khong Ming¹^ORCID,Sadruddin Ahmad¹,Gopal Pooja¹,Yuen Tsz Ying³,Ng Simon³,Kannan Srinivasaraghavan³^ORCID,Brown Christopher J.³,Verma Chandra S.³^ORCID,Orth Peter⁴^ORCID,Peier Andrea⁴,Ge Lan⁴,Yu Xiang⁵,Bhatt Bhavana⁵,Chen Feifei⁵,Wang Erjia⁵,Li Nianyu Jason⁵,Gonzales Raymond J.⁵,Stoeck Alexander²,Henry Brian¹,Sawyer Tomi K.²,Lane David P.³,Johannes Charles W.³^ORCID,Biswas Kaustav²^ORCID,Partridge Anthony W.¹^ORCID

Affiliation:

1. MSD International, Singapore 138665, Singapore

2. Merck & Co., Inc., Boston, Massachusetts 02115, USA

3. Agency for Science, Technology and Research (A*STAR), Singapore 138665, Singapore

4. Merck & Co., Inc., Kenilworth, New Jersey 07033, USA

5. Merck & Co., Inc., West Point, Pennsylvania, 19486, USA

Abstract

Targeting undruggable intracellular proteins with peptides: novel on-target macrocyclic peptide inhibitors of KRAS with broad inhibition of proliferation of multiple KRAS-dependent cancer cell lines.

Funder

Agency for Science, Technology and Research

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/SC/D1SC05187C

Reference26 articles.

1. RAS-targeted therapies: is the undruggable drugged?

2. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

3. The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients