Zobrazeno 1 - 10
of 54
pro vyhledávání: '"Larry V. Pearce"'
Autor:
Mariana Cooke, Eleonora Elhalem, Marcelo G. Kazanietz, Ana Bellomo, Antonella Scravaglieri, Larry V. Pearce, Maria Julieta Comin, Megan L. Peach, Lucía Gandolfi Donadío
Publikováno v:
Journal of Medicinal Chemistry. 64:11418-11431
DAG-lactones represent useful templates for the design of potent and selective C1 domain ligands for PKC isozymes. The ester moiety at the sn-1 position, a common feature in this template, is relevant for C1 domain interactions, but it represents a l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d4b945efbd8a3199dab081038433fcf7
https://doi.org/10.1021/acs.jmedchem.1c00739
https://doi.org/10.1021/acs.jmedchem.1c00739
Autor:
Feng Zhang, Sonya M Hanson, Andres Jara-Oseguera, Dmitriy Krepkiy, Chanhyung Bae, Larry V Pearce, Peter M Blumberg, Simon Newstead, Kenton J Swartz
Publikováno v:
eLife, Vol 5 (2016)
The TRPV1 channel is a detector of noxious stimuli, including heat, acidosis, vanilloid compounds and lipids. The gating mechanisms of the related TRPV2 channel are poorly understood because selective high affinity ligands are not available, and the
Externí odkaz:
https://doaj.org/article/b0b36f46f00a4cf09242275a58243acc
Autor:
Eleonora, Elhalem, Ana, Bellomo, Mariana, Cooke, Antonella, Scravaglieri, Larry V, Pearce, Megan L, Peach, Lucía, Gandolfi Donadío, Marcelo G, Kazanietz, María J, Comin
Publikováno v:
Journal of medicinal chemistry. 64(15)
DAG-lactones represent useful templates for the design of potent and selective C1 domain ligands for PKC isozymes. The ester moiety at the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::49c93cff89a3cfdf7734d263e671a44d
https://pubmed.ncbi.nlm.nih.gov/34279947
https://pubmed.ncbi.nlm.nih.gov/34279947
Autor:
Ha Hee Jin, Jeewoo Lee, Timothy E. Esch, Ho Shin Kim, Noe A. Turcios, Kwang-Hyun Choi, Hee Kim, Larry V. Pearce, Minseok Kim, Shivaji A. Thorat, Peter M. Blumberg, Young Ho Kim, Jihyae Ann, Sun Wook Hwang
Publikováno v:
Journal of Medicinal Chemistry. 63:418-424
Paradoxically, some TRPV1 agonists are, at the organismal level, both nonpungent and clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and characterization in mouse models of a novel, nonpungent vanilloid. Potent anal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a92d7ff93acb00695c9d8c15da9ca695
https://doi.org/10.1021/acs.jmedchem.9b01046
https://doi.org/10.1021/acs.jmedchem.9b01046
Publikováno v:
Biomolecules & Therapeutics
The capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) has been an object of intense interest for pharmacological development on account of its critical role in nociception. In the course of structure activity analysis, it has become
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f9c064c4d1d4faff49256ffe31c0163
https://doi.org/10.4062/biomolther.2019.013
https://doi.org/10.4062/biomolther.2019.013
Autor:
Ha Hee Jin, Aeran Jung, Yoonji Lee, Timothy E. Esch, Nayeon Do, Jin Ju Jeong, Jeewoo Lee, Jisoo Baek, Peter M. Blumberg, Sunhye Hong, Dongxu Zuo, Shivaji A. Thorat, Jihyae Ann, Noe A. Turcios, Larry V. Pearce, Young Dong Yoo, Songyeon Ahn, Sun Choi
Publikováno v:
Journal of medicinal chemistry. 64(1)
Among a series of benzopyridone-based scaffolds investigated as human transient receptor potential vanilloid 1 (TRPV1) ligands, two isomeric benzopyridone scaffolds demonstrated a consistent and distinctive functional profile in which 2-oxo-1,2-dihyd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::338ff19e546a1571f36ac9f940448cc8
https://pubmed.ncbi.nlm.nih.gov/33385210
https://pubmed.ncbi.nlm.nih.gov/33385210
Autor:
Peter M. Blumberg, Zhiwei Feng, Xiang-Qun Xie, Anna K. McCall, Peng Yang, Yu Zhang, Noe A. Turcios, Qin Tong, Shifan Ma, Larry V. Pearce, Ziheng Hu, Brienna K. A. Herold, Changrui Xing
Publikováno v:
The AAPS Journal. 18:898-913
Transient receptor potential vanilloid type 1 (TRPV1), a heat-sensitive calcium channel protein, contributes to inflammation as well as to acute and persistent pain. Since TRPV1 occupies a central position in pathways of neuronal inflammatory signali
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4925c28a9537cda9a8e126687156ac3
https://doi.org/10.1208/s12248-016-9888-z
https://doi.org/10.1208/s12248-016-9888-z
Autor:
Larry V. Pearce, Zhiwei Feng, Xiaole Yang, Xiang-Qun Sean Xie, Xiaomeng Xu, Peng Yang, Peter M. Blumberg
Publikováno v:
Journal of Chemical Information and Modeling. 55:572-588
The transient receptor potential vanilloid type 1 (TRPV1) is a heat-activated cation channel protein, which contributes to inflammation, acute and persistent pain. Antagonists of human TRPV1 (hTRPV1) represent a novel therapeutic approach for the tre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb744138d9a25e5503109413a657cc25
https://doi.org/10.1021/ci5007189
https://doi.org/10.1021/ci5007189
Autor:
Mi-Kyoung Jin, Van-Hai Hoang, Sang-Uk Kang, Jeewoo Lee, Ju-Ok Lim, Ho Shin Kim, Vladimir A. Pavlyukovets, Tae-Hwan Ha, Phuong-Thao Tran, Peter M. Blumberg, Jihyae Ann, Larry V. Pearce
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2685-2688
A series of α-methylated analogues of the potent sRTX thiourea antagonists were investigated as rTRPV1 ligands in order to examine the effect of α-methylation on receptor activity. The SAR analysis indicated that activity was stereospecific with th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c62842acd927738d1ad4f2847b6bb53
https://doi.org/10.1016/j.bmcl.2014.04.054
https://doi.org/10.1016/j.bmcl.2014.04.054
Autor:
Hobin Lee, Young Ho Kim, Timothy E. Esch, Kwang-Hyun Hur, Songyeon Ahn, Nancy E. Lewin, Jihyae Ann, Young Dong Yoo, Larry V. Pearce, Choon-Gon Jang, Jeewoo Lee, Peter M. Blumberg, Hee-Jin Ha, Ji-Young Hwang
Publikováno v:
Eur J Med Chem
In order to discover a novel type of analgesic, we investigated dual activity ligands with TRPV1 antagonism and mu-opioid receptor affinity with the goal of eliciting synergistic analgesia while avoiding the side effects associated with single target
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b08b906ad90178998bd565e27805ab5
https://doi.org/10.1016/j.ejmech.2019.111634
https://doi.org/10.1016/j.ejmech.2019.111634