5mxr
Crystal Structure of the Acquired VIM-2 Metallo-beta-Lactamase in Complex with ANT-330 InhibitorCrystal Structure of the Acquired VIM-2 Metallo-beta-Lactamase in Complex with ANT-330 Inhibitor
Structural highlights
FunctionPublication Abstract from PubMedThe clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-beta-lactamase (MBL) and serine-beta-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new beta-lactamase inhibitors to be used in conjunction with carbapenems and other beta-lactam antibiotics. Herein, we describe our initial exploration of a novel chemical series of metallo-beta-lactamase inhibitors, from concept to efficacy, in a survival model using an advanced tool compound (ANT431) in conjunction with meropenem. SAR Studies Leading to the Identification of a Novel Series of Metallo-beta-lactamase Inhibitors for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections That Display Efficacy in an Animal Infection Model.,Leiris S, Coelho A, Castandet J, Bayet M, Lozano C, Bougnon J, Bousquet J, Everett M, Lemonnier M, Sprynski N, Zalacain M, Pallin TD, Cramp MC, Jennings N, Raphy G, Jones MW, Pattipati R, Shankar B, Sivasubrahmanyam R, Soodhagani AK, Juventhala RR, Pottabathini N, Pothukanuri S, Benvenuti M, Pozzi C, Mangani S, De Luca F, Cerboni G, Docquier JD, Davies DT ACS Infect Dis. 2018 Nov 30. doi: 10.1021/acsinfecdis.8b00246. PMID:30427656[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
|
| ||||||||||||||||||