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Similarly, it has been demonstrated that zinc chelators can inhibit the hydrolytic activity of metallo-β-lactamases against β-lactam antibiotics, restoring the activity of the latter. [6] Metallo-beta-lactamases are important enzymes because they are involved in the breakdown of antibiotics by antibiotic-resistant bacteria. [7]
The other type of beta-lactamase is of the metallo type ("type B"). Metallo-beta-lactamases (MBLs) need metal ion(s) (1 or 2 Zn 2+ ions [2]) on their active site for their catalytic activities. [3] The structure of the New Delhi metallo-beta-lactamase 1 is given by 6C89. It resembles a RNase Z, from which it is thought to have evolved.
The NDM-1 enzyme is one of the class B metallo-beta-lactamase; other types of carbapenemase are class A or class D beta-lactamases. [11] (The class A Klebsiella pneumoniae carbapenemase is currently the most common carbapenemase, which was first detected in North Carolina, United States, in 1996 and has since spread worldwide. [12]
A lactam is a cyclic amide, and beta-lactams are named so because the nitrogen atom is attached to the β-carbon atom relative to the carbonyl. The simplest β-lactam possible is 2-azetidinone. β-lactams are significant structural units of medicines as manifested in many β-lactam antibiotics . [ 2 ]
The addition of tazobactam to piperacillin has enhanced its stability against a wide range of β-lactamase enzymes including some Extended-Spectrum β-lactamases. [20] Other β-lactamase inhibitors such as boronic acids are being studied in which they irreversibly bind to the active site of β-lactamases. This is a benefit over clavulanic acid ...
The β-lactam core structures. (A) A penam.(B) A carbapenam.(C) An oxapenam.(D) A penem.(E) A carbapenem.(F) A monobactam.(G) A cephem.(H) A carbacephem.(I) An oxacephem. This is a list of common β-lactam antibiotics—both administered drugs and those not in clinical use—organized by structural class.
A zinc finger is a small protein structural motif that is characterized by the coordination of one or more zinc ions (Zn 2+) which stabilizes the fold. The term zinc finger was originally coined to describe the finger-like appearance of a hypothesized structure from the African clawed frog (Xenopus laevis) transcription factor IIIA.
Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the same molecule. Lactamization is most efficient in this way if the product is a γ-lactam.