Show simple item record

dc.contributor.authorSantos, R
dc.contributor.authorUrsu, O
dc.contributor.authorGaulton, A
dc.contributor.authorBento, AP
dc.contributor.authorDonadi, RS
dc.contributor.authorBologa, CG
dc.contributor.authorKarlsson, A
dc.contributor.authorAl-Lazikani, B
dc.contributor.authorHersey, A
dc.contributor.authorOprea, TI
dc.contributor.authorOverington, JP
dc.date.accessioned2017-11-24T11:42:30Z
dc.date.issued2017-01
dc.identifier.citationNature reviews. Drug discovery, 2017, 16 (1), pp. 19 - 34
dc.identifier.issn1474-1776
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/947
dc.identifier.eissn1474-1784
dc.identifier.doi10.1038/nrd.2016.230
dc.description.abstractThe success of mechanism-based drug discovery depends on the definition of the drug target. This definition becomes even more important as we try to link drug response to genetic variation, understand stratified clinical efficacy and safety, rationalize the differences between drugs in the same therapeutic class and predict drug utility in patient subgroups. However, drug targets are often poorly defined in the literature, both for launched drugs and for potential therapeutic agents in discovery and development. Here, we present an updated comprehensive map of molecular targets of approved drugs. We curate a total of 893 human and pathogen-derived biomolecules through which 1,578 US FDA-approved drugs act. These biomolecules include 667 human-genome-derived proteins targeted by drugs for human disease. Analysis of these drug targets indicates the continued dominance of privileged target families across disease areas, but also the growth of novel first-in-class mechanisms, particularly in oncology. We explore the relationships between bioactivity class and clinical success, as well as the presence of orthologues between human and animal models and between pathogen and human genomes. Through the collaboration of three independent teams, we highlight some of the ongoing challenges in accurately defining the targets of molecular therapeutics and present conventions for deconvoluting the complexities of molecular pharmacology and drug efficacy.
dc.formatPrint-Electronic
dc.format.extent19 - 34
dc.languageeng
dc.language.isoeng
dc.rights.urihttps://www.rioxx.net/licenses/all-rights-reserved
dc.subjectHumans
dc.subjectDrug Delivery Systems
dc.subjectDrug Approval
dc.subjectPharmacogenetics
dc.subjectGenome, Human
dc.subjectUnited States Food and Drug Administration
dc.subjectUnited States
dc.subjectDrug Prescriptions
dc.subjectGenetic Variation
dc.subjectDrug Discovery
dc.subjectDatabases, Pharmaceutical
dc.titleA comprehensive map of molecular drug targets.
dc.typeJournal Article
dcterms.dateAccepted2016-12-02
rioxxterms.versionofrecord10.1038/nrd.2016.230
rioxxterms.licenseref.urihttps://www.rioxx.net/licenses/all-rights-reserved
rioxxterms.licenseref.startdate2017-01
rioxxterms.typeJournal Article/Review
dc.relation.isPartOfNature reviews. Drug discovery
pubs.issue1
pubs.notes6 months
pubs.organisational-group/ICR
pubs.organisational-group/ICR/Primary Group
pubs.organisational-group/ICR/Primary Group/ICR Divisions
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Computational Biology and Chemogenomics
pubs.organisational-group/ICR
pubs.organisational-group/ICR/Primary Group
pubs.organisational-group/ICR/Primary Group/ICR Divisions
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Computational Biology and Chemogenomics
pubs.publication-statusPublished
pubs.volume16
pubs.embargo.terms6 months
icr.researchteamComputational Biology and Chemogenomicsen_US
dc.contributor.icrauthorAl-Lazikani, Bissanen


Files in this item

Thumbnail

This item appears in the following collection(s)

Show simple item record