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| 1 | Inhibition of temperature-sensitive TRPV3 channel by two natural isochlorogenic acid isomers for alleviation of dermatitis and chronic pruritus显示文摘Genetic gain-of-function mutations of warm temperature-sensitive transient receptor potential vanilloid 3(TRPV3)channel cause Olmsted syndrome characterized by severe itching and keratoderma,indicating that pharmacological inhibition of TRPV3 may hold promise for therapy of chronic pruritus and skin diseases.However,currently available TRPV3 tool inhibitors are either nonselective or less potent,thus impeding the validation of TRPV3 as therapeutic target.Using whole-cell patch-clamp and single-channel recordings,we report the identification of two natural dicaffeoylquinic acid isomers isochlorogenic acid A(IAA)and isochlorogenic acid B(IAB)that selectively inhibit TRPV3 currents with IC50 values of 2.7±1.3 and 0.9±0.3μmol/L,respectively,and reduce the channel open probability to 3.7±1.2%and 3.2±1.1%from 26.9±5.5%,respectively.In vivo evaluation confirms that both IAA and IAB significantly reverse the ear swelling of dermatitis and chronic pruritus.Furthermore,the isomer IAB is able to rescue the keratinocyte death induced by TRPV3 agonist carvacrol.Molecular docking combined with site-directed mutations reveals two residues T636 and F666 critical for the binding of the two isomers.Taken together,our identification of isochlorogenic acids A and B that act as specific TRPV3 channel inhibitors and gating modifiers not only provides an essential pharmacological tool for further investigation of the channel pharmacology and pathology,but also holds developmental potential for treatment of dermatitis and chronic pruritus. | Hang Qi Yuntao Shi Han Wu Canyang Niu Xiaoying Sun KeWei Wang | 2022 | Acta Pharmaceutica Sinica B2022,12,2: | 3 |
| 2 | UV-enhanced bioactivity and cell response of micro-arc oxidized titania coatings显示文摘 | Yong Han Donghui Chen Jifeng Sun Yumei Zhang Kewei Xu | 2008 | Acta Biomaterialia2008,,5: | 2 |
| 3 | Prostate specific membrane antigen knockdown impairs the tumorigenicity of LNCaP prostate cancer cells by inhibiting the phosphatidylinositol 3-kinase/Akt signaling pathway显示文摘 | Guo Zhenghui Lai Yiming Du Tao Zhang Yiming Chen Jieqing Bi Liangkuan Lin Tianxin Liu Hao Wang Wei Xu Kewei Jiang Chun Han Jinli Zhang Caixia Dong Wen Huang Jian Huang Hai | 2014 | Chinese Medical Journal2014,,5: | 2 |
| 4 | Structure and in vitro bioactivity of titania-based films by micro-arc oxidation显示文摘 | Yong Han Seong-Hyeon Hong Kewei Xu | 2003 | Surface & Coatings Technology2003,,2: | 1 |
| 5 | Structure and in vitro bioactivity of titania-based films by micro-arc oxidation显示文摘 | Hong Seong-Hyeon Xu Kewei | 2003 | Surface and coatings technology2003,168,: | 1 |
| 6 | Synthesis of nanocrystalline titania films by micro-arc oxidation显示文摘 | Han Yong Hong Seong-Hyeon Xu Kewei | 2002 | Materials Letters2002,56,: | 1 |
| 7 | Synthesis of nanocrystalline titania films by micro-arc oxidation 显示文摘 | Yong Han Seong-Hyeon Hong Kewei Xu | 2002 | Materials Letters2002,56,: | 1 |
| 8 | Structure and in vitro bioactivity of titania-based films by micro-arc oxidation 显示文摘 | Yong Han Seong-Hyeon Hong Kewei Xu | 2003 | Surface and Coatings Technology2003,168,: | 1 |
| 9 | Structure and in vitro bioactivity of titania-based films by microarc oxidation显示文摘 | Yong Han Seong-Hyeon Hong Kewei Xu | 2003 | Surface and Coatings Technology2003,,168: | 1 |
| 10 | Synthesis of Nanocrustalline Titania Films by Micro-Arc Oxidation显示文摘 | Han Yong Hong Seonghyeon Xu Kewei | 2002 | Materials Letters2002,56,: | 1 |
| 11 | Strueture and in vitro bioaetivity of titania-based films by miero-arc oxidation显示文摘 | HAN YONG HONG SEONG-HYEON XU KEWEI | 2003 | Surf Coat Technol2003,168,: | 1 |
| 12 | Synthesis of nanocrystalline titania films by micro-arc oxidation 显示文摘 | Yong Han Seong-Hyeon Hong Kewei Xu | 2002 | Materials Letters2002,56,: | 1 |
| 13 | Measurement of Critical Temperatures and Critical Pressures for Binary Mixtures of Methyl tert-Butyl Ether(MTBE)+ Alcohol and MTBE+Alkane显示文摘 | Han Kewei Xia Shuqian Ma Peisheng | 2013 | J Chem Thermodyn2013,62,6: | 1 |
| 14 | Morphology and composition of hydroxyapatite coatings prepared by hydrothermal treatment on electrodeposited brushite coatings显示文摘 | Yong Han Kewei Xu Jian Lu | 1999 | Journal of Materials Science: Materials in Medicine1999,,4: | 1 |
| 15 | Synthesis of Nanocrustalline Titania Films by Micro-arc Oxidation 显示文摘 | Yong Han Seong-Hyeon Hong Kewei Xu | 2002 | Materials Letters2002,56,: | 1 |
| 16 | Journal of Materials Science:Materials in Medicine显示文摘 | Han Yortg Xu Kewei Lu Jian | 1999 | 10:2431999,10,: | 1 |
| 17 | Synthesis of nanocrystalline titania films by micro-arc oxidation显示文摘 | HAN Yong HONG Seong-Hyeon XU Kewei | 2002 | Mater Lett2002,56,5: | 1 |
| 18 | Porous nanocrystalline titania films by plasma electrolytic oxidation显示文摘 | HAN Yong HONG Seong-Hyeon XU Kewei | 2002 | Surf Coat Technol2002,154,: | 1 |
| 19 | Structure and in vitro bioactivity of titania-based films by micro-arc oxidation显示文摘 | HAN Yong HONG Seong-Hyeon XU Kewei | 2003 | Surf Coat Technol2003,168,: | 1 |
| 20 | Synthesis of nanocrystalline titania films by micro arc oxidation 显示文摘 | HAN Y SEONG-HONG KEWEI X | 2002 | Mater Lett2002,56,: | 1 |