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dc.contributor.authorTrapero, Ana
dc.contributor.authorPacitto, Angela
dc.contributor.authorChan, Daniel Shiu-Hin
dc.contributor.authorAbell, Chris
dc.contributor.authorBlundell, Tom L
dc.contributor.authorAscher, David B
dc.contributor.authorCoyne, Anthony G
dc.date.accessioned2019-11-16T00:30:55Z
dc.date.available2019-11-16T00:30:55Z
dc.date.issued2020-01-15
dc.identifier.issn0960-894X
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/298953
dc.description.abstractInosine-5'-monophosphate dehydrogenase (IMPDH) is a rate-limiting enzyme involved in nucleotide biosynthesis. Because of its critical role in purine biosynthesis, IMPDH is a drug design target for immunosuppressive, anticancer, antiviral and antimicrobial chemotherapy. In this study, we use mass spectrometry and X-ray crystallography to show that the inhibitor 6-Cl-purine ribotide forms a covalent adduct with the Cys-341 residue of Mycobacterium thermoresistibile IMPDH.
dc.format.mediumPrint-Electronic
dc.languageeng
dc.publisherElsevier BV
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 International
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectMycobacteriaceae
dc.subjectIMP Dehydrogenase
dc.subjectBacterial Proteins
dc.subjectPurine Nucleotides
dc.subjectEnzyme Inhibitors
dc.subjectCrystallography, X-Ray
dc.subjectBinding Sites
dc.subjectProtein Structure, Tertiary
dc.subjectDrug Design
dc.subjectMolecular Dynamics Simulation
dc.titleCovalent inactivation of Mycobacterium thermoresistibile inosine-5'-monophosphate dehydrogenase (IMPDH).
dc.typeArticle
prism.issueIdentifier2
prism.publicationDate2020
prism.publicationNameBioorg Med Chem Lett
prism.startingPage126792
prism.volume30
dc.identifier.doi10.17863/CAM.46010
dcterms.dateAccepted2019-10-30
rioxxterms.versionofrecord10.1016/j.bmcl.2019.126792
rioxxterms.versionAM
rioxxterms.licenseref.urihttp://www.rioxx.net/licenses/all-rights-reserved
rioxxterms.licenseref.startdate2020-01
dc.contributor.orcidAbell, Chris [0000-0001-9174-1987]
dc.contributor.orcidBlundell, Tom [0000-0002-2708-8992]
dc.contributor.orcidCoyne, Anthony [0000-0003-0205-5630]
dc.identifier.eissn1464-3405
rioxxterms.typeJournal Article/Review
pubs.funder-project-idBill & Melinda Gates Foundation (via Foundation for the National Institutes of Health (FNIH)) (ABELL11HTB0)
pubs.funder-project-idEuropean Commission (260872)
pubs.funder-project-idMedical Research Council (MR/M026302/1)
cam.issuedOnline2019-11-09
cam.orpheus.successThu Jan 30 10:37:09 GMT 2020 - Embargo updated
rioxxterms.freetoread.startdate2020-11-09


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Attribution-NonCommercial-NoDerivatives 4.0 International
Except where otherwise noted, this item's licence is described as Attribution-NonCommercial-NoDerivatives 4.0 International