Literature summary for 3.5.2.6 extracted from

Xu, H.; Hazra, S.; Blanchard, J.S.
NXL104 irreversibly inhibits the beta-lactamase from Mycobacterium tuberculosis (2012), Biochemistry, 51, 4551-4557.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
enzyme in complex with inhibitor NXL104, hanging drop vapor diffusion, mixing of 12 mg/ml protein solution in a 1:1 ratio with well solution containing 0.1 M HEPES and 2 M NH4H2PO4, pH 4.1, 10°C, 4-5 days, microseeding, X-ray diffraction structure determination and analysis at 2.3 A resolution	Mycobacterium tuberculosis

Inhibitors

Inhibitors	Comment	Organism	Structure
clavulanate	the enzyme-inhibitor adduct is completely hydrolyzed within 48 h, binding structure comparison, inhibition kinetics and mechanism, modeling, overview	Mycobacterium tuberculosis
trans-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octan-2-carboxamide	NXL104, inhibits both class A and class C beta-lactamases, irreversible inhibition of enzyme BlaC by the inhibitor with a non-lactam structural scaffold, forming a carbamyl adduct with the enzyme, the enzyme-inhibitor adduct remains stable for at least 48 hours, three-dimensional crystal structure of the BlaC-NXL104 carbamyl adduct, overview. Inhibition kinetics and mechanism, modeling, overview	Mycobacterium tuberculosis

Molecular Weight [Da]

Molecular Weight [Da]	Molecular Weight Maximum [Da]	Comment	Organism
28785	-	x * 28785, recombinant enzyme BlaC, mass spectrometry	Mycobacterium tuberculosis

Organism

Organism	UniProt	Comment	Textmining
Mycobacterium tuberculosis	-	gene blaC, chromosomally encoded	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
meropenem + H2O	low activity	Mycobacterium tuberculosis	(4R,5S)-5-[(1S,2R)-1-carboxy-2-hydroxypropyl]-3-[[(3S,5S)-5-(dimethylcarbamoyl)pyrrolidin-3-yl]sulfanyl]-4-methyl-4,5-dihydro-1H-pyrrole-2-carboxylic acid	-	?

Subunits

Subunits	Comment	Organism
?	x * 28785, recombinant enzyme BlaC, mass spectrometry	Mycobacterium tuberculosis

Synonyms

Synonyms	Comment	Organism
BlaC	-	Mycobacterium tuberculosis

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
22	-	assay at room temperature	Mycobacterium tuberculosis

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
6.5	-	assay at	Mycobacterium tuberculosis

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	inhibition kinetics and mechanism, modeling, overview	Mycobacterium tuberculosis

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Release 2023.1 (January 2023)