Biological versatility of crotamine--a cationic peptide from the venom of a South American rattlesnake.
BACKGROUND
Molecules isolated from animals, insects, plants or microorganisms can provide prototypes for design of biopharmaceutical products. Some venom toxins and their derivatives are used in medicine, while others provide templates for development of new drugs.


METHODS
The mild toxin, crotamine, a small basic low-molecular-weight polypeptide purified from the venom of a South American rattlesnake, Crotalus durissus terrificus. Crotamine was discovered more than 50 years ago and only in the past six years has its exceptional biological versatility been demonstrated. Particularly, its cell-penetrating ability, which allows crotamine to cross cell membranes and to accumulate in the nucleus; its use for intracellular vesicle tracking and as a cell cycle marker and its capability for delivering DNA into replicating mammalian cells. Both antimicrobial action and potential selective antitumor activity of crotamine have also been found.


RESULTS
Multidisciplinary approaches and pathways of discovery placed crotamine in a rare category of versatile biomolecules, in which concentration, molecular target preference, structural ancestry and specificity toward biological membranes play an integral role.


CONCLUSIONS
Crotamine is a druggable peptide with high potential for use as an imaging agent for detecting dividing cells, for intracellular delivery of hydrophilic biomolecules, and as an alternative chemotherapeutic compound against aggressive types of cancer.
Laboratório de Genética e Laboratório Especial de Toxinologia Aplicada - CAT/CEPID do Instituto Butantan, Av. Vital Brazil 1500, 05503-900, São Paulo, SP, Brasil. ikerkis@butantan.gov.br
Irina
I
Kerkis
Fernando de Sá
Fde S
Silva
Alexandre
A
Pereira
Alexandre
A
Kerkis
Gandhi
G
Rádis-Baptista
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D015415:Biomarkers / Q000737:chemistry / Q000378:metabolism; D002453:Cell Cycle / Q000502:physiology; D002462:Cell Membrane / Q000378:metabolism; D003435:Crotalid Venoms / Q000737:chemistry* / Q000378:metabolism*; D017839:Crotalus; D006801:Humans; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism*; D013020:South America
D000970:Antineoplastic Agents; D015415:Biomarkers; D003435:Crotalid Venoms; D010455:Peptides; C010563:crotamine