Results 21 to 30 of about 1,083,474 (317)

New capsaicin analogs as molecular rulers to define the permissive conformation of the mouse TRPV1 ligand-binding pocket

eLife, 2020
The capsaicin receptor TRPV1 is an outstanding representative of ligand-gated ion channels in ligand selectivity and sensitivity. However, molecular interactions that stabilize the ligand-binding pocket in its permissive conformation, and how many ...
Simon Vu, Vikrant Singh, Heike Wulff, Vladimir Yarov-Yarovoy, Jie Zheng   +4 more
doaj   +1 more source

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

JCI Insight, 2020
Tirzepatide (LY3298176) is a dual GIP and GLP-1 receptor agonist under development for the treatment of type 2 diabetes mellitus (T2DM), obesity, and nonalcoholic steatohepatitis.
F. Willard, J. Douros, M. Gabe, A. D. Showalter, D. B. Wainscott, T. Suter, M. Capozzi, W. J. C. van der Velden, Cynthia Stutsman, G. Cardona, S. Urva, P. Emmerson, J. Holst, D. D’Alessio, M. Coghlan, M. Rosenkilde, Jonathan E. Campbell, K. Sloop   +17 more
semanticscholar   +1 more source

The synthesis of cis- and trans-3-(4-hydroxyphenyl)cyclobutanecarboxylic acids and the study of their derivatives as GPR-40 receptor ligands

Журнал органічної та фармацевтичної хімії, 2020
Aim. To synthesize cis- and trans-isomers of 3-(4-hydroxyphenyl)cyclobutanecarboxylic acid and evaluate the biological activity of their derivatives against GPR-40. Results and discussion.
I. O. Feskov, I. S. Kondratov, Yu. O. Kuchkovska, V. S. Naumchyk, O. V. Onopchenko, O. O. Grygorenko   +5 more
doaj   +1 more source

Terazosin Analogs Targeting Pgk1 as Neuroprotective Agents: Design, Synthesis, and Evaluation

Frontiers in Chemistry, 2022
Nitrogen-containing heterocyclic compounds have shown promising therapeutic effects in a variety of inflammatory and neurodegenerative diseases. Recently, terazosin (TZ), a heterocyclic compound with a quinazoline core, was found to combine with ...
Yang Wang, Yang Wang, Shihu Qian, Shihu Qian, Fang Zhao, Fang Zhao, Yujie Wang, Yujie Wang, Jiaming Li, Jiaming Li   +9 more
doaj   +1 more source

Antibody-Targeted TNFRSF Activation for Cancer Immunotherapy: The Role of FcγRIIB Cross-Linking

Frontiers in Pharmacology, 2022
Co-stimulation signaling in various types of immune cells modulates immune responses in physiology and disease. Tumor necrosis factor receptor superfamily (TNFRSF) members such as CD40, OX40 and CD137/4-1BB are expressed on myeloid cells and/or ...
Luyan Liu, Yi Wu, Kaiyan Ye, Kaiyan Ye, Meichun Cai, Meichun Cai, Guanglei Zhuang, Guanglei Zhuang, Jieyi Wang   +8 more
doaj   +1 more source

Design and Synthesis of an 18F-Labeled Version of Phenylethyl Orvinol ([18F]FE-PEO) for PET-Imaging of Opioid Receptors

Molecules, 2012
The semisynthetic oripavine derivative phenethyl orvinol (PEO), a full agonist at opioid receptors (OR), is an attractive structural motif for developing 18F-labeled PET tracers with a high degree of sensitivity for competition between endogenous and ...
Gjermund Henriksen, János Marton
doaj   +1 more source

Differential β-arrestin2 requirements for constitutive and agonist-induced internalization of the CB1 cannabinoid receptor [PDF]

, 2013
CB1 cannabinoid receptor (CB1R) undergoes both constitutive and agonist-induced internalization, but the underlying mechanisms of these processes and the role of beta-arrestins in the regulation of CB1R function are not completely understood.
Ahn, Bakshi, Bari, Brailoiu, Coutts, Daigle, Daigle, Dale, Derkinderen, DeWire, Eszter Boros, Fan, Ferguson, Ferguson, Freund, Gaborik, Graham, Guan, Gyombolai, Gábor Turu, Holliday, Hsieh, Hunyady, Jin, Keren, Kleyer, Kouznetsova, Krupnick, Leterrier, Leterrier, László Hunyady, Marullo, McDonald, McDonald, Nguyen, Oakley, Oakley, Pacher, Paing, Parent, Pál Gyombolai, Rinaldi-Carmona, Roche, Rozenfeld, Rozenfeld, Sanchez, Shenoy, Singh, Szekeres, Tohgo, Toth, Turu, Turu, Turu, Turu, Valjent, Varnai, Vines, Ward, Ward, Wei, Woo, Wu, Zhang, Zhao   +64 more
core   +1 more source

Functional Stoichiometry at the Nicotinic Receptor. The Photon Cross Section for Phase 1 Corresponds to Two Bis-Q Molecules per Channel [PDF]

, 1982
These experiments examine changes in the agonist-induced conductance that occur when the agonist-receptor complex is perturbed. Voltage-clamped Electrophorus electroplaques are exposed to the photoisomerizable agonist trans-Bis-Q A 1-µs laser flash ...
Lester, Henry A., Sheridan, Robert E.
core   +1 more source

Towards an Understanding of the Mode of Action of Human Aromatase Activity for Azoles through Quantum Chemical Descriptors-Based Regression and Structure Activity Relationship Modeling Analysis

Molecules, 2020
Aromatase is an enzyme member of the cytochrome P450 superfamily coded by the CYP19A1 gene. Its main action is the conversion of androgens into estrogens, transforming androstenedione into estrone and testosterone into estradiol.
Chayawan Chayawan, Cosimo Toma, Emilio Benfenati, Ana Y. Caballero Alfonso   +3 more
doaj   +1 more source

Long-acting beta(2)-agonist in addition to tiotropium versus either tiotropium or long-acting beta(2)-agonist alone for chronic obstructive pulmonary disease [PDF]

, 2012
BackgroundLong-acting bronchodilators comprising long-acting beta(2)-agonists and the anticholinergic agent tiotropium are commonly used for managing persistent symptoms of chronic obstructive pulmonary disease.
Aaron, Aaron, Appleton, Arievich, Barr, Bateman, Berger, Brusasco, Calverley, Cazzola, Cheyne, Effing, Fujimoto, Gross, Hacken, Higgins, Hutchinson, Johnson, Kaplan, Karner, Lacasse, Mahler, Mahler, Marco, Meer, Meyer, Najafzadeh, Najafzadeh, New, Noord, Noord, Noord, Proskocil, Rodrigo, Roisman, Singh, Tanaka, Tashkin, Tashkin, Tashkin, Tashkin, Tashkin, Tashkin, Tashkin, Vogelmeier, Vogelmeier, Wallukat, Welsh   +47 more
core   +1 more source