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Contribution of natural products to the discovery of the transient receptor potential (TRP) channels family and their functions.
Pharmacol Ther. 2005 May; 106(2):179-208.P&T

Abstract

Members of the transient receptor potential (TRP) family of nonselective cation channels are involved in several pathological and physiological conditions. The search for the molecular targets for naturally occurring substances, especially from plants, allowed the characterization of many TRP channels. In fact, attempts to understand the hot and painful action of the vanillyl group containing compounds capsaicin (from Capsicum sp.) and its ultrapotent analogue resiniferatoxin (RTX, from Euphorbia sp.) led to the cloning of the vanilloid receptor (TRPV1) 7 years ago. TRPV1 is found in sensory fibers and functions as a molecular integrator of several painful stimuli, being especially stimulated during inflammation. Since TRPV1 is involved in several pathological conditions, selective ligands or modulators of this channel are substances of potential interest to treat such diseases. Once again, natural products seem to be also interesting sources of compounds that might be prototype TRPV1 ligands. The cloning of TRPV1 also enabled the discovery of other members of the TRPV family of channels. Similar to TRPV1, these receptors function as molecular detectors of physical and chemical stimuli, such as innocuous and noxious heat, as well as mechanical force. Recently, novel TRP channels sensitive to low temperatures also have been cloned, namely, TRPM8 and TRPA1. Such channels are also activated by naturally occurring substances but knowledge of their involvement in health and disease is in its infancy. In the present review, we focused on the contribution of natural products to the discovery of TRP channels and to the development of novel drugs to treat pathological conditions in which these channels are involved.

Authors+Show Affiliations

Departamento de Farmacologia, Universidade Federal de Santa Catarina, Campus Universitário-Trindade, Bloco D-CCB-Cx. Postal: 476-CEP: 88049-900-Florianópolis, SC, Brazil. calixto@farmaco.ufsc.brNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

15866319

Citation

Calixto, João B., et al. "Contribution of Natural Products to the Discovery of the Transient Receptor Potential (TRP) Channels Family and Their Functions." Pharmacology & Therapeutics, vol. 106, no. 2, 2005, pp. 179-208.
Calixto JB, Kassuya CA, André E, et al. Contribution of natural products to the discovery of the transient receptor potential (TRP) channels family and their functions. Pharmacol Ther. 2005;106(2):179-208.
Calixto, J. B., Kassuya, C. A., André, E., & Ferreira, J. (2005). Contribution of natural products to the discovery of the transient receptor potential (TRP) channels family and their functions. Pharmacology & Therapeutics, 106(2), 179-208.
Calixto JB, et al. Contribution of Natural Products to the Discovery of the Transient Receptor Potential (TRP) Channels Family and Their Functions. Pharmacol Ther. 2005;106(2):179-208. PubMed PMID: 15866319.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Contribution of natural products to the discovery of the transient receptor potential (TRP) channels family and their functions. AU - Calixto,João B, AU - Kassuya,Candida A L, AU - André,Eunice, AU - Ferreira,Juliano, Y1 - 2005/01/16/ PY - 2004/11/18/accepted PY - 2005/5/4/pubmed PY - 2005/9/1/medline PY - 2005/5/4/entrez SP - 179 EP - 208 JF - Pharmacology & therapeutics JO - Pharmacol Ther VL - 106 IS - 2 N2 - Members of the transient receptor potential (TRP) family of nonselective cation channels are involved in several pathological and physiological conditions. The search for the molecular targets for naturally occurring substances, especially from plants, allowed the characterization of many TRP channels. In fact, attempts to understand the hot and painful action of the vanillyl group containing compounds capsaicin (from Capsicum sp.) and its ultrapotent analogue resiniferatoxin (RTX, from Euphorbia sp.) led to the cloning of the vanilloid receptor (TRPV1) 7 years ago. TRPV1 is found in sensory fibers and functions as a molecular integrator of several painful stimuli, being especially stimulated during inflammation. Since TRPV1 is involved in several pathological conditions, selective ligands or modulators of this channel are substances of potential interest to treat such diseases. Once again, natural products seem to be also interesting sources of compounds that might be prototype TRPV1 ligands. The cloning of TRPV1 also enabled the discovery of other members of the TRPV family of channels. Similar to TRPV1, these receptors function as molecular detectors of physical and chemical stimuli, such as innocuous and noxious heat, as well as mechanical force. Recently, novel TRP channels sensitive to low temperatures also have been cloned, namely, TRPM8 and TRPA1. Such channels are also activated by naturally occurring substances but knowledge of their involvement in health and disease is in its infancy. In the present review, we focused on the contribution of natural products to the discovery of TRP channels and to the development of novel drugs to treat pathological conditions in which these channels are involved. SN - 0163-7258 UR - https://www.unboundmedicine.com/medline/citation/15866319/Contribution_of_natural_products_to_the_discovery_of_the_transient_receptor_potential__TRP__channels_family_and_their_functions_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0163-7258(04)00204-9 DB - PRIME DP - Unbound Medicine ER -