Literature DB >> 25148694

The renaissance of Ras.

Lech-Gustav Milroy1, Christian Ottmann.   

Abstract

Increased signaling by the small G protein Ras is found in many human cancers and is often caused by direct mutation of this protein. Hence, small-molecule attenuation of pathological Ras activity is of utmost interest in oncology. However, despite nearly three decades of intense drug discovery efforts, no clinically viable option for Ras inhibition has been developed. Very recently, reports of a number of new approaches of addressing Ras activity have led to the revival of this molecular target with the prospect of finally fulfilling the therapy promises associated with this important protein.

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Year:  2014        PMID: 25148694     DOI: 10.1021/cb500555h

Source DB:  PubMed          Journal:  ACS Chem Biol        ISSN: 1554-8929            Impact factor:   5.100


  8 in total

Review 1.  Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view.

Authors:  Shaoyong Lu; Hyunbum Jang; Shuo Gu; Jian Zhang; Ruth Nussinov
Journal:  Chem Soc Rev       Date:  2016-07-11       Impact factor: 54.564

Review 2.  Inhibition of Nonfunctional Ras.

Authors:  Ruth Nussinov; Hyunbum Jang; Attila Gursoy; Ozlem Keskin; Vadim Gaponenko
Journal:  Cell Chem Biol       Date:  2021-01-12       Impact factor: 8.116

3.  Computational Modeling Reveals that Signaling Lipids Modulate the Orientation of K-Ras4A at the Membrane Reflecting Protein Topology.

Authors:  Zhen-Lu Li; Matthias Buck
Journal:  Structure       Date:  2017-03-09       Impact factor: 5.006

4.  Crystal Structure of a Human K-Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d.

Authors:  Satoshi Sogabe; Yusuke Kamada; Masanori Miwa; Ayumu Niida; Tomoya Sameshima; Masahiro Kamaura; Kazuko Yonemori; Shigekazu Sasaki; Jun-Ichi Sakamoto; Kotaro Sakamoto
Journal:  ACS Med Chem Lett       Date:  2017-05-10       Impact factor: 4.345

5.  Identification of functional substates of KRas during GTP hydrolysis with enhanced sampling simulations.

Authors:  Juan Zeng; Jian Chen; Fei Xia; Qiang Cui; Xianming Deng; Xin Xu
Journal:  Phys Chem Chem Phys       Date:  2022-03-30       Impact factor: 3.676

6.  Wild-type KRAS is a novel therapeutic target for melanoma contributing to primary and acquired resistance to BRAF inhibition.

Authors:  P Dietrich; S Kuphal; T Spruss; C Hellerbrand; A K Bosserhoff
Journal:  Oncogene       Date:  2017-10-23       Impact factor: 9.867

7.  GTP Binding and Oncogenic Mutations May Attenuate Hypervariable Region (HVR)-Catalytic Domain Interactions in Small GTPase K-Ras4B, Exposing the Effector Binding Site.

Authors:  Shaoyong Lu; Avik Banerjee; Hyunbum Jang; Jian Zhang; Vadim Gaponenko; Ruth Nussinov
Journal:  J Biol Chem       Date:  2015-10-09       Impact factor: 5.157

8.  Exploring the interactions of the RAS family in the human protein network and their potential implications in RAS-directed therapies.

Authors:  Anibal Bueno; Ian Morilla; Diego Diez; Aurelio A Moya-Garcia; José Lozano; Juan A G Ranea
Journal:  Oncotarget       Date:  2016-11-15
  8 in total

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