Covalent inactivation of Mycobacterium thermoresistibile inosine-5'-monophosphate dehydrogenase (IMPDH).

Trapero, Ana; Pacitto, Angela; Chan, Daniel Shiu-Hin; Abell, Chris; Blundell, Tom L; Ascher, David B; Coyne, Anthony G

Trapero, Ana; Pacitto, Angela; Chan, Daniel Shiu-Hin; Abell, Chris; Blundell, Tom L; Ascher, David B; Coyne, Anthony G.

Affiliation

Trapero A; Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, United Kingdom.
Pacitto A; Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge CB2 1GA, United Kingdom.
Chan DS; Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, United Kingdom.
Abell C; Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, United Kingdom.
Blundell TL; Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge CB2 1GA, United Kingdom. Electronic address: tom@cryst.bioc.cam.ac.uk.
Ascher DB; Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge CB2 1GA, United Kingdom; Department of Biochemistry and Molecular Biology, Bio21 Institute, University of Melbourne, 30 Flemington Road, Parkville, Victoria 3052, Australia. Electronic address: david.ascher@unimelb.
Coyne AG; Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, United Kingdom. Electronic address: agc40@cam.ac.uk.

Bioorg Med Chem Lett ; 30(2): 126792, 2020 01 15.

Article in En | MEDLINE | ID: mdl-31757668

Subject(s)

Bacterial Proteins/antagonists & inhibitors; Enzyme Inhibitors/chemistry; IMP Dehydrogenase/antagonists & inhibitors; Mycobacteriaceae/enzymology; Bacterial Proteins/metabolism; Binding Sites; Crystallography, X-Ray; Drug Design; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/metabolism; IMP Dehydrogenase/metabolism; Molecular Dynamics Simulation; Protein Structure, Tertiary; Purine Nucleotides/chemical synthesis; Purine Nucleotides/chemistry; Purine Nucleotides/metabolism

Key words

6-Cl-purine ribotide; Covalent inhibitor; GuaB2; IMPDH; Mycobacterium thermoresistibile IMPDH

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Bacterial Proteins / Enzyme Inhibitors / IMP Dehydrogenase / Mycobacteriaceae Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2020 Type: Article Affiliation country: United kingdom

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