1A8T

METALLO-BETA-LACTAMASE IN COMPLEX WITH L-159,061

Summary for 1A8T

• Entry DOI: 10.2210/pdb1a8t/pdb
• Descriptor: METALLO-BETA-LACTAMASE, ZINC ION, 2-BUTYL-6-HYDROXY-3-[2'-(1H-TETRAZOL-5-YL)-BIPHENYL-4-YLMETHYL]-3H-QUINAZOLIN-4-ONE, ... (4 entities in total)
• Functional Keywords: hydrolase, beta-lactamase, metallo-beta-lactamase, zinc, antibiotic resistance
• Biological source: Bacteroides fragilis
• Cellular location: Periplasm : P25910
• Total number of polymer chains: 2
• Total formula weight: 51489.48

Authors

Fitzgerald, P.M.D.,Toney, J.H.,Grover, N.,Vanderwall, D. (deposition date: 1998-03-23, release date: 1998-10-14, Last modification date: 2024-05-22)

Primary citation

Toney, J.H.,Fitzgerald, P.M.,Grover-Sharma, N.,Olson, S.H.,May, W.J.,Sundelof, J.G.,Vanderwall, D.E.,Cleary, K.A.,Grant, S.K.,Wu, J.K.,Kozarich, J.W.,Pompliano, D.L.,Hammond, G.G.
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.
Chem.Biol., 5:185-196, 1998

PubMed Abstract: High level resistance to carbapenem antibiotics in gram negative bacteria such as Bacteroides fragilis is caused, in part, by expression of a wide-spectrum metallo-beta-lactamase that hydrolyzes the drug to an inactive form. Co-administration of metallo-beta-lactamase inhibitors to resistant bacteria is expected to restore the antibacterial activity of carbapenems.

PubMed: 9545432
DOI: 10.1016/S1074-5521(98)90632-9

Experimental method

X-RAY DIFFRACTION (2.55 Å)