TRPV1: A Target for Rational Drug Design

作者: Vincenzo Carnevale , Tibor Rohacs

DOI: 10.3390/PH9030052

关键词:

摘要: Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin resiniferatoxin (RTX). Many compounds have been developed that either activate or inhibit TRPV1, but none of them are in routine clinical practice. This review will discuss the rationale for antagonists agonists TRPV1 pain relief other conditions, strategies to develop new, better drugs target this ion channel, using newly available high-resolution structures.

参考文章(158)
Anna Garcia-Elias, Sanela Mrkonjić, Carole Jung, Carlos Pardo-Pastor, Rubén Vicente, Miguel A Valverde, None, The TRPV4 Channel Handbook of Experimental Pharmacology. ,vol. 222, pp. 293- 319 ,(2014) , 10.1007/978-3-642-54215-2_12
Michael J. Caterina, Tobias A. Rosen, Makoto Tominaga, Anthony J. Brake, David Julius, A capsaicin-receptor homologue with a high threshold for noxious heat. Nature. ,vol. 398, pp. 436- 441 ,(1999) , 10.1038/18906
János Szolcsányi, Effect of capsaicin on thermoregulation: an update with new aspects Temperature (Austin, Tex.). ,vol. 2, pp. 277- 296 ,(2015) , 10.1080/23328940.2015.1048928
Michael J. Caterina, Mark A. Schumacher, Makoto Tominaga, Tobias A. Rosen, Jon D. Levine, David Julius, The capsaicin receptor: a heat-activated ion channel in the pain pathway Nature. ,vol. 389, pp. 816- 824 ,(1997) , 10.1038/39807
T. Hoffmann, K. Kistner, F. Miermeister, R. Winkelmann, J. Wittmann, M.J.M. Fischer, C. Weidner, P.W. Reeh, TRPA1 and TRPV1 are differentially involved in heat nociception of mice. European Journal of Pain. ,vol. 17, pp. 1472- 1482 ,(2013) , 10.1002/J.1532-2149.2013.00331.X
Fan Yang, Xian Xiao, Wei Cheng, Wei Yang, Peilin Yu, Zhenzhen Song, Vladimir Yarov-Yarovoy, Jie Zheng, Structural mechanism underlying capsaicin binding and activation of the TRPV1 ion channel Nature Chemical Biology. ,vol. 11, pp. 518- 524 ,(2015) , 10.1038/NCHEMBIO.1835
Santosh K Mishra, Sarah M Tisel, Peihan Orestes, Sonia K Bhangoo, Mark A Hoon, TRPV1-lineage neurons are required for thermal sensation The EMBO Journal. ,vol. 30, pp. 582- 593 ,(2011) , 10.1038/EMBOJ.2010.325
Donald A. Simone, Maria Nolano, Timothy Johnson, Gwen Wendelschafer-Crabb, William R. Kennedy, Intradermal Injection of Capsaicin in Humans Produces Degeneration and Subsequent Reinnervation of Epidermal Nerve Fibers: Correlation with Sensory Function The Journal of Neuroscience. ,vol. 18, pp. 8947- 8959 ,(1998) , 10.1523/JNEUROSCI.18-21-08947.1998
Parvinder Kaur Rathee, Carsten Distler, Otilia Obreja, Winfried Neuhuber, Ging Kuo Wang, Sho-Ya Wang, Carla Nau, Michaela Kress, PKA/AKAP/VR-1 Module: A Common Link of Gs-Mediated Signaling to Thermal Hyperalgesia The Journal of Neuroscience. ,vol. 22, pp. 4740- 4745 ,(2002) , 10.1523/JNEUROSCI.22-11-04740.2002
Patricia A. Koplas, Robert L. Rosenberg, Gerry S. Oxford, The Role of Calcium in the Desensitization of Capsaicin Responses in Rat Dorsal Root Ganglion Neurons The Journal of Neuroscience. ,vol. 17, pp. 3525- 3537 ,(1997) , 10.1523/JNEUROSCI.17-10-03525.1997