Literature DB >> 31951561

Sticking it to KRAS: Covalent Inhibitors Enter the Clinic.

Frank McCormick1.   

Abstract

Drugs that target KRAS 12C covalently, AMG 510 and MRTX849, are now in the clinic. Recent papers describe development of these compounds, their selectivity and properties, early clinical data, and potential combination therapies. These papers herald a new era in Ras research, with improved drugs and strategies certain to follow.
Copyright © 2019 Elsevier Inc. All rights reserved.

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Year:  2020        PMID： 31951561     DOI： 10.1016/j.ccell.2019.12.009

Source DB:  PubMed          Journal:  Cancer Cell        ISSN： 1535-6108            Impact factor:   31.743


  19 in total

Review 1.  Biology, pathology, and therapeutic targeting of RAS.

Authors:  J Matthew Rhett; Imran Khan; John P O'Bryan
Journal:  Adv Cancer Res       Date:  2020-07-09       Impact factor: 6.242

Review 2.  Synthetic Vulnerabilities in the KRAS Pathway.

Authors:  Marta Roman; Elizabeth Hwang; E Alejandro Sweet-Cordero
Journal:  Cancers (Basel)       Date:  2022-06-08       Impact factor: 6.575

3.  Inhibition of RAS: proven and potential vulnerabilities.

Authors:  Mariyam Zuberi; Imran Khan; John P O'Bryan
Journal:  Biochem Soc Trans       Date:  2020-10-30       Impact factor: 5.407

4.  Silencing of Oncogenic KRAS by Mutant-Selective Small Interfering RNA.

Authors:  Bjoern Papke; Salma H Azam; Anne Y Feng; Christina Gutierrez-Ford; Hayden Huggins; Pradeep S Pallan; Amanda E D Van Swearingen; Martin Egli; Adrienne D Cox; Channing J Der; Chad V Pecot
Journal:  ACS Pharmacol Transl Sci       Date:  2021-02-04

5.  Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.

Authors:  Joseph A Ippolito; Haichan Niu; Nicole Bertoletti; Zachary J Carter; Shengyan Jin; Krasimir A Spasov; José A Cisneros; Margarita Valhondo; Kara J Cutrona; Karen S Anderson; William L Jorgensen
Journal:  ACS Med Chem Lett       Date:  2021-01-06       Impact factor: 4.345

Review 6.  The genetics of ductal adenocarcinoma of the pancreas in the year 2020: dramatic progress, but far to go.

Authors:  Elizabeth D Thompson; Nicholas J Roberts; Laura D Wood; James R Eshleman; Michael G Goggins; Scott E Kern; Alison P Klein; Ralph H Hruban
Journal:  Mod Pathol       Date:  2020-07-23       Impact factor: 7.842

Review 7.  New Horizons: Emerging Therapies and Targets in Thyroid Cancer.

Authors:  Matthew D Ringel
Journal:  J Clin Endocrinol Metab       Date:  2021-01-01       Impact factor: 5.958

Review 8.  RLIP76: A Structural and Functional Triumvirate.

Authors:  Jasmine Cornish; Darerca Owen; Helen R Mott
Journal:  Cancers (Basel)       Date:  2021-05-04       Impact factor: 6.639

9.  Discovery of cryptic allosteric sites using reversed allosteric communication by a combined computational and experimental strategy.

Authors:  Duan Ni; Jiacheng Wei; Xinheng He; Ashfaq Ur Rehman; Xinyi Li; Yuran Qiu; Jun Pu; Shaoyong Lu; Jian Zhang
Journal:  Chem Sci       Date:  2020-11-02       Impact factor: 9.825

10.  Untangling Dual-Targeting Therapeutic Mechanism of Epidermal Growth Factor Receptor (EGFR) Based on Reversed Allosteric Communication.

Authors:  Yuran Qiu; Xiaolan Yin; Xinyi Li; Yuanhao Wang; Qiang Fu; Renhua Huang; Shaoyong Lu
Journal:  Pharmaceutics       Date:  2021-05-18       Impact factor: 6.321
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