2mwt

Publication Abstract from PubMed

In silico dissection of crotalicidin (Ctn), a cathelicidin from a South American pit viper, yielded fragments Ctn[1-14] and Ctn[15-34], which were tested to ascertain to what extent they reproduced the structure and activity of the parent peptide. NMR data showing Ctn to be alpha-helical at the N-terminus and unstructured at the C-terminus were matched by similar data from the fragments. The peptides were tested against Gram-positive and -negative bacteria and for toxicity against both tumor and healthy cells. Despite its amphipathic alpha-helical structure, Ctn[1-14] was totally inert toward bacteria or eukaryotic cells. In contrast, unstructured Ctn[15-34] replicated the activity of parent Ctn against Gram-negative bacteria and tumor cells while being significantly less toxic toward eukaryotic cells. This selectivity for bacteria and tumor cells, plus a stability to serum well above that of Ctn, portrays Ctn[15-34] as an appealing candidate for further development as an anti-infective or antitumor lead.

Structural Dissection of Crotalicidin, a Rattlesnake Venom Cathelicidin, Retrieves a Fragment with Antimicrobial and Antitumor Activity.,Falcao CB, Perez-Peinado C, de la Torre BG, Mayol X, Zamora-Carreras H, Jimenez MA, Radis-Baptista G, Andreu D J Med Chem. 2015 Nov 12;58(21):8553-63. doi: 10.1021/acs.jmedchem.5b01142. Epub, 2015 Oct 26. PMID:26465972^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.