Literature DB >> 27506872

Recent advances in cancer drug discovery targeting RAS.

Candice Y Wilson1, Peter Tolias2.   

Abstract

Mutated RAS is present in 30% of human tumors, appearing in 90% of pancreatic, 45% of colon and 35% of lung cancers. These high occurrences make RAS one of the most important drug targets in oncology. Three decades of effort to target RAS have been unsuccessful in generating drug therapies suggesting that it might represent an 'undruggable' target. However, recent reports highlighting new approaches for targeting RAS have uncovered more information on protein structure and identified new binding pockets. Efforts to target the KRAS G12C mutation specifically have shown promising results whereas other approaches have targeted various protein complexes. These advances could lead to development of new effective cancer drugs targeting RAS.
Copyright © 2016 Elsevier Ltd. All rights reserved.

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Year:  2016        PMID: 27506872     DOI: 10.1016/j.drudis.2016.08.002

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  19 in total

Review 1.  Ras and Rap1: A tale of two GTPases.

Authors:  Seema Shah; Ethan J Brock; Kyungmin Ji; Raymond R Mattingly
Journal:  Semin Cancer Biol       Date:  2018-04-03       Impact factor: 15.707

Review 2.  Comprehensive review of targeted therapy for colorectal cancer.

Authors:  Yuan-Hong Xie; Ying-Xuan Chen; Jing-Yuan Fang
Journal:  Signal Transduct Target Ther       Date:  2020-03-20

3.  Gene-Mutation-Based Algorithm for Prediction of Treatment Response in Colorectal Cancer Patients.

Authors:  Heather Johnson; Zahra El-Schich; Amjad Ali; Xuhui Zhang; Athanasios Simoulis; Anette Gjörloff Wingren; Jenny L Persson
Journal:  Cancers (Basel)       Date:  2022-04-18       Impact factor: 6.575

4.  Heterogeneity and mutation in KRAS and associated oncogenes: evaluating the potential for the evolution of resistance to targeting of KRAS G12C.

Authors:  Vincent L Cannataro; Stephen G Gaffney; Carly Stender; Zi-Ming Zhao; Mark Philips; Andrew E Greenstein; Jeffrey P Townsend
Journal:  Oncogene       Date:  2018-02-16       Impact factor: 9.867

5.  Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.

Authors:  Jason R Abbott; Pratiq A Patel; Jennifer E Howes; Denis T Akan; J Phillip Kennedy; Michael C Burns; Carrie F Browning; Qi Sun; Olivia W Rossanese; Jason Phan; Alex G Waterson; Stephen W Fesik
Journal:  ACS Med Chem Lett       Date:  2018-08-08       Impact factor: 4.345

Review 6.  New tricks for human farnesyltransferase inhibitor: cancer and beyond.

Authors:  Jingyuan Wang; Xue Yao; Jin Huang
Journal:  Medchemcomm       Date:  2017-02-16       Impact factor: 3.597

7.  Enhanced inflammation and attenuated tumor suppressor pathways are associated with oncogene-induced lung tumors in aged mice.

Authors:  Neha Parikh; Ryan L Shuck; Mihai Gagea; Lanlan Shen; Lawrence A Donehower
Journal:  Aging Cell       Date:  2017-10-18       Impact factor: 9.304

8.  Molecular Dynamics Simulations and Dynamic Network Analysis Reveal the Allosteric Unbinding of Monobody to H-Ras Triggered by R135K Mutation.

Authors:  Duan Ni; Kun Song; Jian Zhang; Shaoyong Lu
Journal:  Int J Mol Sci       Date:  2017-10-26       Impact factor: 5.923

Review 9.  KRAS-related noncoding RNAs in pancreatic ductal adenocarcinoma.

Authors:  Shuang-Ni Yu; Yi-Hui Ma; Wu-Gan Zhao; Xiang-Lan Jin; Hai-Yan Yang; Ping-Ping Liu; Jie Chen
Journal:  Chronic Dis Transl Med       Date:  2016-12-22

10.  Efficacy of MEK inhibition in a K-Ras-driven cholangiocarcinoma preclinical model.

Authors:  Mingjie Dong; Xianqiong Liu; Katja Evert; Kirsten Utpatel; Michele Peters; Shanshan Zhang; Zhong Xu; Li Che; Antonio Cigliano; Silvia Ribback; Frank Dombrowski; Antonio Cossu; John Gordan; Diego F Calvisi; Matthias Evert; Yan Liu; Xin Chen
Journal:  Cell Death Dis       Date:  2018-01-18       Impact factor: 8.469

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