Results 11 to 20 of about 1,200,697 (382)

Prolonged activation of innate immune pathways by a polyvalent STING agonist

Nature Biomedical Engineering, 2021
The stimulator of interferon genes (STING) is an endoplasmic reticulum transmembrane protein that is a target of therapeutics for infectious diseases and cancer.
Suxin Li, Min Luo, Zhaohui Wang, Q. Feng, Jonathan Wilhelm, Xu Wang, Wei Li, Jian Wang, Agnieszka Cholka, yang-xin fu, B. Sumer, Hongtao Yu, Jinming Gao   +12 more
semanticscholar   +1 more source

CD40 Agonist Antibodies in Cancer Immunotherapy.

Annual Review of Medicine, 2020
CD40 is a cell-surface member of the TNF (tumor necrosis factor) receptor superfamily. Upon activation, CD40 can license dendritic cells to promote antitumor T cell activation and re-educate macrophages to destroy tumor stroma.
R. Vonderheide
semanticscholar   +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

Engineered PLGA microparticles for long-term, pulsatile release of STING agonist for cancer immunotherapy

Science Translational Medicine, 2020
Microfabricated particles mimic multiple intratumoral injections of STING agonist over weeks to improve ease of use and decrease metastasis. Squaring away tumors Cancer immunotherapy has been achieving increasing prominence in recent years, but many ...
Xueguang Lu, Lei Miao, Wenting Gao, Ziqi Chen, Kevin J. McHugh, Yehui Sun, Zachary L. Tochka, Stephanie Tomasic, Kaitlyn Sadtler, Alain Hyacinthe, Yuxuan Huang, Tyler P. Graf, Quanyin Hu, M. Sarmadi, R. Langer, Daniel G. Anderson, A. Jaklenec   +16 more
semanticscholar   +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

Novel 2-amino-isoflavones exhibit aryl hydrocarbon receptor agonist or antagonist activity in a species/cell-specific context [PDF]

, 2012
The aryl hydrocarbon receptor (AhR) mediates the induction of a variety of xenobiotic metabolism genes. Activation of the AhR occurs through binding to a group of structurally diverse compounds, most notably dioxins, which are exogenous ligands ...
BALBONI, GIANFRANCO, Bell DR, CONGIU, CENZO, Denison MS, Fernandes A, He G, Mellor I.R., ONNIS, VALENTINA, Rose M, Rowlands JC, Wall RJ   +10 more
core   +1 more source

α1D-Adrenoceptors are responsible for the high sensitivity and the slow time-course of noradrenaline-mediated contraction in conductance arteries [PDF]

, 2013
The objective of this study was to determine whether the different time-course characteristics of α1-adrenoceptor-mediated contraction in arteries can be related to the subtypes involved.
Alexander, Arévalo-León, Cavalli, Chalothorn, Chen, Cotecchia, Daly, Deighan, Docherty, García-Cazarín, García-Sainz, García-Sainz, García-Sainz, Gisbert, Gisbert, Gisbert, Gisbert, Goldstein, Hawrylyshyn, Hein, Hosoda, Hrometz, Hussain, Keffel, Kenny, Koshimizu, Lachnit, Lyssand, Lyssand, Lyssand, Martinez-Rivelles, Martí, McCune, Methven, Methven, Michelotti, Monto, Noguera, Noguera, Philipp, Piascik, Piascik, Pérez-Aso, Rudner, Schwinn, Stassen, Taguchi, Tanaka, Tanoue, Tanoue, Theroux, Yamamoto, Zhong, Ziani   +53 more
core   +1 more source

⁶⁸Ga-Labeled [Thz¹⁴]Bombesin(7–14) Analogs: Promising GRPR-Targeting Agonist PET Tracers with Low Pancreas Uptake

Molecules, 2023
With overexpression in various cancers, the gastrin-releasing peptide receptor (GRPR) is a promising target for cancer imaging and therapy. However, the high pancreas uptake of reported GRPR-targeting radioligands limits their clinical application.
Lei Wang, Ivica Jerolim Bratanovic, Zhengxing Zhang, Hsiou-Ting Kuo, Helen Merkens, Jutta Zeisler, Chengcheng Zhang, Ruiyan Tan, François Bénard, Kuo-Shyan Lin   +9 more
doaj   +1 more source

Beta-agonist stimulation ameliorates the phenotype of spinal and bulbar muscular atrophy mice and patient-derived myotubes [PDF]

, 2017
Spinal and bulbar muscular atrophy (SBMA) is a neuromuscular disease characterized by the loss of lower motor neurons. SBMA is caused by expansions of a polyglutamine tract in the gene coding for androgen receptor (AR).
Blaauw, Bert, Borgia, Doriana, Gomes Pereira, Marcelo, Lieberman, Andrew P., Maino, Eleonora, Malena, Adriana, Marchioretti, Caterina, Milioto, Carmelo, Pegoraro, Elena, Pennuto, Maria, Pennuto, Maria, Plebani, Mario, Polanco, Maria J., Sambataro, Fabio, Sambataro, Fabio, Sorar, Gianni, Soraru', Gianni, Venturini, Roberta, Vergani, Lodovica   +18 more
core   +3 more sources

High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist

Molecules, 2021
Relaxin/insulin-like family peptide receptor 3 (RXFP3) belongs to class A G protein-coupled receptor family. RXFP3 and its endogenous ligand relaxin-3 are mainly expressed in the brain with important roles in the regulation of appetite, energy metabolism,
Guangyao Lin, Yang Feng, Xiaoqing Cai, Caihong Zhou, Lijun Shao, Yan Chen, Linhai Chen, Qing Liu, Qingtong Zhou, Ross A.D. Bathgate, Dehua Yang, Ming-Wei Wang   +11 more
doaj   +1 more source