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How Chemoproteomics Can Enable Drug Discovery and Development

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Moellering, Raymond E., Cravatt, Benjamin F.·2012·Chemistry & Biology

DOI 10.1016/j.chembiol.2012.01.001PMC PMC3312051

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Abstract

Creating first-in-class medications to treat human disease is an extremely challenging endeavor. While genome sequencing and genetics are making direct connections between mutations and human disorders at an unprecedented rate, matching molecular targets with a suitable therapeutic indication must ultimately be achieved by pharmacology. Here, we discuss how the integration of chemical proteomic platforms (such as activity-based protein profiling) into the earliest stages of the drug discovery process has the potential to greatly expand the scope of proteins that can be pharmacologically evaluated in living systems, and, through doing so, promote the identification and prioritization of new therapeutic targets.

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Authors: Moellering, R. E., & Cravatt, B. F.
Affiliations: Scripps Research Institute (US)
Corresponding author: Cravatt, Benjamin F.
ORCID: Moellering, Raymond E.
Cravatt, Benjamin F.
Venue: Chemistry & Biology
Publisher: Elsevier BV
Published: 2012-01
Volume: 19
Issue: 1
Pages: 11-22
ISSN: 1074-5521 (ISSN-L)
DOI: 10.1016/j.chembiol.2012.01.001
PMC: PMC3312051
OpenAlex: W2030953184
Cited by: 182
References: 96
Citations by year: 2026: 9 · 2025: 12 · 2024: 22 · 2023: 7 · 2022: 5 · 2021: 11 · 2020: 16 · 2019: 21 · 2018: 9 · 2017: 10 · 2016: 16 · 2015: 15 · 2014: 7 · 2013: 14 · 2012: 7
FWCI: 6.47
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 563 d)
Locations: Chemistry & Biology (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: Howard Hughes Medical Institute
Cancer Research Institute
Damon Runyon Cancer Research Foundation
National Institutes of Health
National Institute on Drug Abuse (DA025285, R01DA025285)
National Cancer Institute (R01CA132630, CA-087660, R37CA087660, R01CA087660, CA132630)
Topics: Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
Physical Sciences › Chemistry › Spectroscopy › Advanced Proteomics Techniques and Applications
Keywords: chemoproteomics, drug discovery, drug development, activity-based protein profiling, drug target identification, target prioritization, first-in-class drugs
MeSH terms: Enzymes, Humans, Serine Proteinase Inhibitors, Genome, Human, Proteomics, Metabolic Networks and Pathways, Small Molecule Libraries, Drug Discovery

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How Chemoproteomics Can Enable Drug Discovery and Development

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