Results 181 to 190 of about 5,561 (208)

Structural basis of TRPV3 inhibition by an antagonist

Nature Chemical Biology, 2022
The TRPV3 channel plays vital roles in skin physiology. Dysfunction of TRPV3 causes skin diseases, including Olmsted syndrome. However, the lack of potent and selective inhibitors impedes the validation of TRPV3 as a therapeutic target. In this study, we identified Trpvicin as a potent and subtype-selective inhibitor of TRPV3.
Junping Fan, Linghan Hu, Zongwei Yue, Daohong Liao, Fusheng Guo, Han Ke, Daohua Jiang, Yong Yang, Xiaoguang Lei   +8 more
openaire   +2 more sources

A pentameric TRPV3 channel with a dilated pore

Nature, 2023
Transient receptor potential (TRP) channels are a large, eukaryotic ion channel superfamily that control diverse physiological functions, and therefore are attractive drug targets1-5. More than 210 structures from more than 20 different TRP channels have been determined, and all are tetramers4. Despite this wealth of structures, many aspects concerning
Shifra Lansky, John Michael Betancourt, Jingying Zhang, Yining Jiang, Elizabeth D. Kim, Navid Paknejad, Crina M. Nimigean, Peng Yuan, Simon Scheuring   +8 more
openaire   +2 more sources

Unlocking the therapeutic potential of TRPV3: Insights into thermosensation, channel modulation, and skin homeostasis involving TRPV3

BioEssays
AbstractRecent insights reveal the significant role of TRPV3 in warmth sensation. A novel finding elucidated how thermosensation is affected by TRPV3 membrane abundance that is modulated by the transmembrane protein TMEM79. TRPV3 is a warmth‐sensitive ion channel predominantly expressed in epithelial cells, particularly skin keratinocytes.
Makoto Tominaga, Jing Lei
exaly   +3 more sources

Genotype‒Phenotype Correlation of TRPV3-Related Olmsted Syndrome

Journal of Investigative Dermatology, 2021
We have previously shown that gain-of-function variations in transient receptor potential vanilloid-3 (TRPV3) underlay Olmsted syndrome, a rare hyperkeratotic skin channelopathy. In this study, we attempt to establish a genotype‒phenotype correlation in Olmsted syndrome, which has been unclear owing to the rarity and heterogeneity of the condition.
Weilong Zhong, Linghan Hu, Xu Cao, Jiahui Zhao, Xianning Zhang, Mingyang Lee, Huijun Wang, Jie Zhang, Quan Chen, Cheng Feng, Lina Duo, Xiuli Wang, Li Tang, Zhimiao Lin, Yong Yang   +14 more
openaire   +2 more sources

TRPV3

2014
Transient receptor potential vanilloid-3 (TRPV3) is a Ca(2+)-permeable nonselective cation channel widely expressed in skin keratinocytes, as well as oral and nasal epithelia. TRPV3 is activated by innocuous warm as well as noxious hot temperatures. Activation of TRPV3 in skin keratinocytes causes release of multiple substances, which in turn regulate ...
Pu, Yang, Michael X, Zhu
openaire   +2 more sources

Thermally Activated TRPV3 Channels

2014
TRPV3 is a temperature-sensitive transient receptor potential (TRP) ion channel. The TRPV3 protein functions as a Ca(2+)-permeable nonselective cation channel with six transmembrane domains forming a tetrameric complex. TRPV3 is known to be activated by warm temperatures, synthetic small-molecule chemicals, and natural compounds from plants.
Jialie, Luo, Hongzhen, Hu
openaire   +2 more sources

A plant‐derived TRPV3 inhibitor suppresses pain and itch

British Journal of Pharmacology, 2021
Background and PurposeItching is the most frequent pathology in dermatology that has significant impacts on people's mental health and social life. Transient receptor potential vanilloid 3 (TRPV3) channel is a promising target for treating pruritus. However, few selecetive and potent antagonists have been reported.
Chantana Boonyarat, Ren Lai
exaly   +3 more sources

Transient receptor potential vanilloid-3 (TRPV3) channel induces dermal fibrosis via the TRPV3/TSLP/Smad2/3 pathways in dermal fibroblasts

Journal of Dermatological Science, 2020
Excessive wound healing can lead to hypertrophic scars, which are not only a cosmetic issue but could also be itchy or painful. Previously, we reported that, in comparison with normal tissue, thymic stromal lymphopoietin (TSLP) expression was increased in skin burn scars when the activation of transient receptor potential vanilloid-3 (TRPV3) of ...
Ji-Young, Um, Seok Young, Kang, Hyun Ji, Kim, Bo Young, Chung, Chun Wook, Park, Hye One, Kim   +5 more
openaire   +2 more sources

TRPV3 is a temperature-sensitive vanilloid receptor-like protein

Nature, 2002
Vanilloid receptor-1 (VR1, also known as TRPV1) is a thermosensitive, nonselective cation channel that is expressed by capsaicin-sensitive sensory afferents and is activated by noxious heat, acidic pH and the alkaloid irritant capsaicin. Although VR1 gene disruption results in a loss of capsaicin responses, it has minimal effects on thermal nociception.
Smith, G D, Gunthorpe, M, Kelsell, R E, Hayes, P D, Reilly, P, Facer, P, Wright, J E, Jerman, J C, Walhin, J P, Ooi, L, Egerton, J, Charles, K J, Smart, D, Randall, A D, Anand, P, Davis, J B   +15 more
openaire   +3 more sources

TRPV3 is a calcium-permeable temperature-sensitive cation channel

Nature, 2002
Transient receptor potential (TRP) proteins are cation-selective channels that function in processes as diverse as sensation and vasoregulation. Mammalian TRP channels that are gated by heat and capsaicin (>43 degrees C; TRPV1 (ref. 1)), noxious heat (>52 degrees C; TRPV2 (ref.
Haoxing, Xu, I Scott, Ramsey, Suhas A, Kotecha, Magdalene M, Moran, Jayhong A, Chong, Deborah, Lawson, Pei, Ge, Jeremiah, Lilly, Inmaculada, Silos-Santiago, Yu, Xie, Peter S, DiStefano, Rory, Curtis, David E, Clapham   +12 more
openaire   +2 more sources