Literature DB >> 23939923

Targeting the K-Ras/PDEδ protein-protein interaction: the solution for Ras-driven cancers or just another therapeutic mirage?

Brendan Frett1, Yuanxiang Wang, Hong-Yu Li.   

Abstract

The holy grail, finally? After years of unsuccessful attempts at drugging the Ras oncogene, a recent paper by Zimmerman et al. has revealed the possibility of inhibiting Ras signaling on a clinically relevant level by blocking the K-Ras/PDEδ protein-protein interaction. The results, reported in Nature, are highlighted herein with future implications and directions to evaluate the full clinical potential of this research.
Copyright © 2013 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  Ras; anticancer agents; drug resistance; protein–protein interactions; targeted therapeutics

Mesh:

Substances:

Year:  2013        PMID: 23939923      PMCID: PMC4666017          DOI: 10.1002/cmdc.201300311

Source DB:  PubMed          Journal:  ChemMedChem        ISSN: 1860-7179            Impact factor:   3.466


  14 in total

Review 1.  What we have learned about pancreatic cancer from mouse models.

Authors:  Pedro A Pérez-Mancera; Carmen Guerra; Mariano Barbacid; David A Tuveson
Journal:  Gastroenterology       Date:  2012-03-08       Impact factor: 22.682

2.  Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity.

Authors:  Till Maurer; Lindsay S Garrenton; Angela Oh; Keith Pitts; Daniel J Anderson; Nicholas J Skelton; Benjamin P Fauber; Borlan Pan; Shiva Malek; David Stokoe; Mary J C Ludlam; Krista K Bowman; Jiansheng Wu; Anthony M Giannetti; Melissa A Starovasnik; Ira Mellman; Peter K Jackson; Joachim Rudolph; Weiru Wang; Guowei Fang
Journal:  Proc Natl Acad Sci U S A       Date:  2012-03-19       Impact factor: 11.205

Review 3.  Blocking oncogenic Ras signaling for cancer therapy.

Authors:  A A Adjei
Journal:  J Natl Cancer Inst       Date:  2001-07-18       Impact factor: 13.506

4.  Therapeutic strategies for targeting ras proteins.

Authors:  Stephan Gysin; Megan Salt; Amy Young; Frank McCormick
Journal:  Genes Cancer       Date:  2011-03

5.  Activated Src and Ras induce gefitinib resistance by activation of signaling pathways downstream of epidermal growth factor receptor in human gallbladder adenocarcinoma cells.

Authors:  Baoli Qin; Hiroshi Ariyama; Eishi Baba; Risa Tanaka; Hitoshi Kusaba; Mine Harada; Shuji Nakano
Journal:  Cancer Chemother Pharmacol       Date:  2006-03-11       Impact factor: 3.333

Review 6.  Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer.

Authors:  P J Roberts; C J Der
Journal:  Oncogene       Date:  2007-05-14       Impact factor: 9.867

Review 7.  Multidrug resistance mediated by the ATP-binding cassette transporter protein MRP.

Authors:  S P Cole; R G Deeley
Journal:  Bioessays       Date:  1998-11       Impact factor: 4.345

8.  Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling.

Authors:  Gunther Zimmermann; Björn Papke; Shehab Ismail; Nachiket Vartak; Anchal Chandra; Maike Hoffmann; Stephan A Hahn; Gemma Triola; Alfred Wittinghofer; Philippe I H Bastiaens; Herbert Waldmann
Journal:  Nature       Date:  2013-05-22       Impact factor: 49.962

9.  Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.

Authors:  Gideon Bollag; Peter Hirth; James Tsai; Jiazhong Zhang; Prabha N Ibrahim; Hanna Cho; Wayne Spevak; Chao Zhang; Ying Zhang; Gaston Habets; Elizabeth A Burton; Bernice Wong; Garson Tsang; Brian L West; Ben Powell; Rafe Shellooe; Adhirai Marimuthu; Hoa Nguyen; Kam Y J Zhang; Dean R Artis; Joseph Schlessinger; Fei Su; Brian Higgins; Raman Iyer; Kurt D'Andrea; Astrid Koehler; Michael Stumm; Paul S Lin; Richard J Lee; Joseph Grippo; Igor Puzanov; Kevin B Kim; Antoni Ribas; Grant A McArthur; Jeffrey A Sosman; Paul B Chapman; Keith T Flaherty; Xiaowei Xu; Katherine L Nathanson; Keith Nolop
Journal:  Nature       Date:  2010-09-30       Impact factor: 49.962

10.  Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.

Authors:  Qi Sun; Jason P Burke; Jason Phan; Michael C Burns; Edward T Olejniczak; Alex G Waterson; Taekyu Lee; Olivia W Rossanese; Stephen W Fesik
Journal:  Angew Chem Int Ed Engl       Date:  2012-05-08       Impact factor: 15.336

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  1 in total

Review 1.  Emerging strategies to target RAS signaling in human cancer therapy.

Authors:  Kun Chen; Yalei Zhang; Ling Qian; Peng Wang
Journal:  J Hematol Oncol       Date:  2021-07-23       Impact factor: 17.388

  1 in total

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