preparation-vivo-use-an-activity-based-probe-for-n-acylethanolamine

Preparation and <em>In Vivo</em> Use of an Activity-based Probe for <em>N</em>-acylethanolamine Acid Amidase

Activity-based protein profiling (ABPP) is a method for the identification of an enzyme of interest in a complex proteome through the use of a chemical ...

Istituto Italiano di Tecnologia

Among the growing family of ribosomally synthesized, post-translationally modified peptides, particularly intriguing are class III lanthipeptides containing the triamino acid labionin. In the course of a screening program aimed at finding bacterial cell wall inhibitors, we discovered a new lanthipeptide produced by an Actinoplanes sp. The molecule, designated NAI-112, consists of 22 amino acids and contains an N-terminal labionin and a C-terminal methyl-labionin. Unique among lanthipeptides, it carries a 6-deoxyhexose moiety N-linked to a tryptophan residue. Consistently, the corresponding gene cluster encodes, in addition to the LanKC enzyme characteristic of this lanthipeptide class, a glycosyl transferase. Despite possessing weak antibacterial activity, NAI-112 is effective in experimental models of nociceptive pain, reducing pain symptoms in mice in both the formalin and the chronic constriction injury tests. Thus, NAI-112 represents, after the labyrinthopeptins, the second example of a lanthipeptide effective against nociceptive pain.

Fabiola Bonezzi

Drug Discovery and Development

Istituto Italiano di Tecnologia

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Fabiola Bonezzi

.css-o250i3{font-size:18px;font-family:Open Sans,sans-serif;line-height:21.6px;}Drug Discovery and Development

Istituto Italiano di Tecnologia

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Drug Discovery and Development