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Literature summary for 3.5.2.6 extracted from

  • White, D.S.; Choy, C.J.; Moural, T.W.; Martin, S.E.; Wang, J.; Gargaro, S.; Kang, C.; Berkman, C.E.
    Bis(benzoyl) phosphate inactivators of beta-lactamase C from Mtb (2019), Bioorg. Med. Chem. Lett., 29, 2116-2118 .
    View publication on PubMed

Application

Application Comment Organism
drug development enzyme BlaC is a rational enzyme target for therapeutic agents in treatment of tuberculosis caused by Mycobacterium tuberculosis Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
bis(3,4-dichlorobenzoyl) phosphate
-
Mycobacterium tuberculosis
bis(4-chlorobenzoyl) phosphate
-
Mycobacterium tuberculosis
bis(4-cyanobenzoyl) phosphate
-
Mycobacterium tuberculosis
bis(4-fluorobenzoyl) phosphate
-
Mycobacterium tuberculosis
bis(4-methoxybenzoyl)
-
Mycobacterium tuberculosis
bis(4-methylbenzoyl) phosphate
-
Mycobacterium tuberculosis
bis(4-nitrobenzoyl) phosphate
-
Mycobacterium tuberculosis
bis[4-(trifluoromethyl)benzoyl] phosphate
-
Mycobacterium tuberculosis
di([1,1'-biphenyl]-4-carbonyl) phosphate
-
Mycobacterium tuberculosis
dibenzoyl phosphate
-
Mycobacterium tuberculosis
additional information synthesis and structure-activity-relationship data for the first-generation library of bis(benzoyl)phosphates as enzyme inhibitors, overview. Phosphorylated Ser70 in BlaC following inactivation by dibenzoyl phosphate Mycobacterium tuberculosis

Localization

Localization Comment Organism GeneOntology No. Textmining
cell surface the class A beta-lactamase BlaC is a cell surface expressed serine hydrolase Mycobacterium tuberculosis 9986
-

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WKD3
-
-
Mycobacterium tuberculosis ATCC 25618 P9WKD3
-
-
Mycobacterium tuberculosis H37Rv P9WKD3
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein phosphorylated Ser70 in BlaC following inactivation by dibenzoyl phosphate Mycobacterium tuberculosis

Synonyms

Synonyms Comment Organism
BlaC
-
Mycobacterium tuberculosis
class A beta-lactamase
-
Mycobacterium tuberculosis

General Information

General Information Comment Organism
malfunction inactivation of the cell surface-expressed serine hydrolase and class A beta-lactamase BlaC in Mycobacterium tuberculosis (Mtb) causes increased susceptibility to beta-lactam antibiotics Mycobacterium tuberculosis