Cited by 949Protein Kinase Regulation and GTPase SignalingProtein Degradation and InhibitorsCancer Mechanisms and Therapy

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Drugging the ‘undruggable’ cancer targets

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Dang, Chi V., Reddy, E. Premkumar, Shokat, Kevan M., Soucek, Laura·2017·Nature Reviews Cancer

DOI 10.1038/nrc.2017.36PMC PMC5945194

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Abstract

The term 'undruggable' was coined to describe proteins that could not be targeted pharmacologically. However, progress is being made to 'drug' many of these targets, and therefore more appropriate terms might be 'difficult to drug' or 'yet to be drugged'. Many desirable targets in cancer fall into this category, including the RAS and MYC oncogenes, and pharmacologically targeting these intractable proteins is now a key challenge in cancer research that requires innovation and the development of new technologies. In this Viewpoint article, we asked four scientists working in this field for their opinions on the most crucial advances, as well as the challenges and what the future holds for this important area of research.

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Self-citation
Discovery of Anticancer Hybrid Molecules by Supervised Machine Learning Models and in Vitro Validation in Drug Resistant Chronic Myeloid Leukemia Cells
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Authors: Dang, C. V., Reddy, E. P., Shokat, K. M., & Soucek, L.
Affiliations: The Wistar Institute (US)
Icahn School of Medicine at Mount Sinai (US)
Howard Hughes Medical Institute (US)
Institució Catalana de Recerca i Estudis Avançats (ES)
Corresponding author: Dang, Chi V.
Reddy, E. Premkumar
Shokat, Kevan M.
Soucek, Laura
ORCID: Dang, Chi V.
Reddy, E. Premkumar
Shokat, Kevan M.
Soucek, Laura
Venue: Nature Reviews Cancer
Publisher: Springer Science and Business Media LLC
Published: 2017-06-23
Volume: 17
Issue: 8
Pages: 502-508
ISSN: 1474-175X (ISSN-L)
1474-1768
DOI: 10.1038/nrc.2017.36
PMC: PMC5945194
OpenAlex: W2692768525
Cited by: 927
References: 57
Citations by year: 2026: 93 · 2025: 113 · 2024: 125 · 2023: 110 · 2022: 121 · 2021: 121 · 2020: 113 · 2019: 63 · 2018: 58 · 2017: 10
FWCI: 6.26
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.springer.com/tdm (tdm)
Locations: Nature reviews. Cancer (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
eScholarship (California Digital Library) (submittedVersion)
Funders: National Cancer Institute (R01CA057341, R01CA158209, R01CA051497)
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 Degradation and Inhibitors
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Mechanisms and Therapy
Keywords: oncogenic Ras, MYC oncogene, oncogene targeting, anticancer drug development
MeSH terms: Antineoplastic Agents, Humans, Neoplasms, Receptors, Androgen, Oncogene Proteins, Fusion, Proto-Oncogene Proteins c-myc, NF-kappa B, ras Proteins, Proto-Oncogene Proteins c-myb, Drug Discovery, Molecular Targeted Therapy

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