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Discovery of Selective Pituitary Adenylate Cyclase 1 Receptor (PAC1R) Antagonist Peptides Potent in a Maxadilan/PACAP38-Induced Increase in Blood Flow Pharmacodynamic Model

Autor: Fang-Tsao Hong, Hongyan Li, Derek E. Piper, Leszek Poppe, Philip Wong, Todd Hager, Essa Hu, Jason Long, Jennifer Aral, Narender R. Gavva, Cen Xu, Les P. Miranda, Carl Davis, Dawn Zhu, Sonya G. Lehto, Licheng Shi, Kristin L. Andrews

Publikováno v: Journal of Medicinal Chemistry. 64:3427-3438

Inhibition of the pituitary adenylate cyclase 1 receptor (PAC1R) is a novel mechanism that could be used for abortive treatment of acute migraine. Our research began with comparative analysis of known PAC1R ligand scaffolds, PACAP38 and Maxadilan, wh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acd41c74ae7dbf93739b5d3ae1f169c1
https://doi.org/10.1021/acs.jmedchem.0c01396

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Cryo-EM structures of PAC1 receptor reveal ligand binding mechanism

Autor: Xin Huang, Yaping Sun, Hong-Wei Wang, Ruobing Ren, Dandan Zhang, Cui Li, Xiaoqing Chen, Xun Li, Yunpeng Song, Yao Ding, Wenge Zhong, Essa Hu Harrington, Cen Xu, Jia Wang, Xianqiang Song, Liaoyuan A. Hu, Yingli Ma

Publikováno v: Cell Research

The pituitary adenylate cyclase-activating polypeptide type I receptor (PAC1R) belongs to the secretin receptor family and is widely distributed in the central neural system and peripheral organs. Abnormal activation of the receptor mediates trigemin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf85fe25f4b0853fac1595a613be093b
https://doi.org/10.1038/s41422-020-0280-2

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Author Correction: Cryo-EM structures of PAC1 receptor reveal ligand binding mechanism

Autor: Yao Ding, Wenge Zhong, Dandan Zhang, Liaoyuan A. Hu, Xun Li, Xin Huang, Jia Wang, Yingli Ma, Cui Li, Yunpeng Song, Cen Xu, Essa Hu Harrington, Yaping Sun, Hong-Wei Wang, Xiaoqing Chen, Xianqiang Song, Ruobing Ren

Publikováno v: Cell Res

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f713923cdecdb71599b8e750cb6c7d54
https://europepmc.org/articles/PMC7265381/

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Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A)

Autor: Jianxia Shi, Xiaoning Zhao, Samer Chmait, Mary Dovlatyan, Silke Miller, Kristin L. Andrews, Geraldine Hill Della Puppa, James J. S. Treanor, Dianna Lester-Zeiner, Carl Davis, Essa Hu, Christopher Biorn, Jessica Able, Hang Chen, Jennifer R. Allen, Ji Ma

Publikováno v: ACS Medicinal Chemistry Letters. 5:700-705

We report the discovery of novel imidazo[4,5-b]pyridines as potent and selective inhibitors of PDE10A. The investigation began with our recently disclosed ketobenzimidazole 1, which exhibited single digit nanomolar PDE10A activity but poor oral bioav

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f48b3d8c765bcbadc35e47aee5474f6
https://doi.org/10.1021/ml5000993

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Initial characterization of a PDE10A selective positron emission tomography tracer [11C]AMG 7980 in non-human primates

Autor: Dah-Ren Hwang, John Castrillon, Shannon Rumfelt, Jennifer R. Allen, Essa Hu, Anissa Abi-Dargham, Carl Davis, Balu Easwaramoorthy, James J. S. Treanor, Hang Chen, Mark Slifstein

Publikováno v: Nuclear Medicine and Biology. 41:343-349

Introduction Phosphodiesterase 10A (PDE10A) is an intracellular enzyme responsible for the breakdown of cyclic nucleotides which are important secondary messengers in the central nervous system. Inhibition of PDE10A has been identified as a potential

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e513d78ed165d00a8bcf84edd85dfd4d
https://doi.org/10.1016/j.nucmedbio.2014.01.007

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Design, Optimization, and Biological Evaluation of Novel Keto-Benzimidazoles as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A)

Autor: Dianna Lester-Zeiner, Christopher Biorn, Essa Hu, Jianxia Shi, James J. S. Treanor, Sharon Zhao, Jennifer R. Allen, Amy Porter, Kristin L. Andrews, Samer Chmait, Shannon Rumfelt, Aaron C. Siegmund, Roxanne Kunz, Ning Chen, Hang Chen, Carl Davis, Ji Ma

Publikováno v: Journal of Medicinal Chemistry. 56:8781-8792

Our development of PDE10A inhibitors began with an HTS screening hit (1) that exhibited both high p-glycoprotein (P-gp) efflux ratios in rat and human and poor metabolic stability. On the basis of cocrystal structure of 1 in human PDE10A enzyme, we d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3066fe445a252131b55a29d74d2cd4ef
https://doi.org/10.1021/jm401234w

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Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux

Autor: Samer Chmait, Adrie D. Jones, Amy Porter, Kristin L. Andrews, Xiaoning Zhao, Jennifer R. Allen, Shannon Rumfelt, Wenge Zhong, Essa Hu, James R. Falsey, Robert M. Rzasa, Steven W. Louie, James J. S. Treanor, Ning Chen

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:7371-7375

We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c902b8d3ff73465c5b07e532310cd1d
https://doi.org/10.1016/j.bmcl.2012.10.078

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