Cited by 192Protein Kinase Regulation and GTPase SignalingProtein Tyrosine PhosphatasesReceptor Mechanisms and Signaling

Drugging Ras GTPase: a comprehensive mechanistic and signaling structural view

Open access
Lu, Shaoyong, Jang, Hyunbum, Gu, Shuo, Zhang, Jian, Nussinov, Ruth·2016·Chemical Society Reviews

Abstract

In this review we overview current advances in Ras structural knowledge and the signaling pathways that can be co-targeted along with Ras to mitigate drug resistance.

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Crossref · 10.1039/c5cs00911a

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  • Designing PPI inhibitors to block the interaction of RAS and RAS effect factors represents a promising paradigm for modulating RAS function and provides new impetus for the discovery of related drugs.

    “Designing PPI inhibitors to block the interaction of RAS and RAS effect factors represents a promising paradigm for modulating RAS function and provides new impetus for the discovery of related drugs.86,326–329”

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Research works printed but not linked: 2

  1. [50]Evelyn CR Biesiada J Duan X Tang H Shang X Papoian R Seibel WL Nelson S Meller J Zheng Y Chem. Biol 2015 290 12879 12898 PMC4432303 25825487
  2. [165]Sayyed-Ahmed A Cho KJ Hancock JF Gorfe AA J. Phys. Chem. B 2016 PMC5048749 27072779

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Authors
Lu, S., Jang, H., Gu, S., Zhang, J., & Nussinov, R.
Affiliations
  • Shanghai Jiao Tong University (CN)
  • Frederick National Laboratory for Cancer Research (US)
  • Tel Aviv University (IL)
Corresponding author
  • Zhang, Jian
  • Nussinov, Ruth
Venue
Chemical Society Reviews
Published
2016
Volume
45
Issue
18
Pages
4929-4952
ISSN
  • 0306-0012 (ISSN-L)
  • 1460-4744
OpenAlex
W2464027273
Cited by
188
References
243
Citations by year
2026: 13 · 2025: 14 · 2024: 14 · 2023: 18 · 2022: 22 · 2021: 26 · 2020: 12 · 2019: 24 · 2018: 18 · 2017: 17 · 2016: 10
FWCI
2.08
Type
journal article
Language
en
Open access
Locations
  • Chemical Society Reviews (publishedVersion)
  • PubMed (publishedVersion)
  • Europe PMC (PubMed Central) (acceptedVersion)
  • PubMed Central (acceptedVersion)
Funders
  • National Institutes of Health (HHSN261200800001C)
  • National Cancer Institute (Z01BC010440, HHSN261200800001E))
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Tyrosine Phosphatases
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords
Ras GTPase, RAS inhibitors, RAS mutations, drug resistance, allosteric site, YAP, c-Myc, MAPK/ERK pathway, PI3K/AKT/mTOR pathway, cell cycle regulation, RAS-driven cancers
MeSH terms
Allosteric Regulation, Antineoplastic Agents, Humans, Mutation, Neoplasms, ras Proteins, Drug Resistance, Neoplasm, Phosphatidylinositol 3-Kinases, Catalytic Domain, RNA, Small Interfering, Molecular Targeted Therapy

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