Results 11 to 20 of about 1,182,206 (391)

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

A TNFR2-Specific TNF Fusion Protein With Improved In Vivo Activity

Frontiers in Immunology, 2022
Tumor necrosis factor (TNF) receptor-2 (TNFR2) has attracted considerable interest as a target for immunotherapy. Indeed, using oligomeric fusion proteins of single chain-encoded TNFR2-specific TNF mutants (scTNF80), expansion of regulatory T cells and ...
Juan Gamboa Vargas, Juan Gamboa Vargas, Jennifer Wagner, Haroon Shaikh, Haroon Shaikh, Isabell Lang, Juliane Medler, Mohamed Anany, Mohamed Anany, Tim Steinfatt, Josefina Peña Mosca, Josefina Peña Mosca, Stephanie Haack, Julia Dahlhoff, Maike Büttner-Herold, Carolin Graf, Estibaliz Arellano Viera, Hermann Einsele, Harald Wajant, Andreas Beilhack, Andreas Beilhack   +20 more
doaj   +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

Analogs of 6-Bromohypaphorine with Increased Agonist Potency for α7 Nicotinic Receptor as Anti-Inflammatory Analgesic Agents

Marine Drugs, 2023
Hypaphorines, tryptophan derivatives, have anti-inflammatory activity, but their mechanism of action was largely unknown. Marine alkaloid L-6-bromohypaphorine with EC50 of 80 μM acts as an agonist of α7 nicotinic acetylcholine receptor (nAChR) involved ...
Igor A. Ivanov, Andrei E. Siniavin, Victor A. Palikov, Dmitry A. Senko, Irina V. Shelukhina, Lyubov A. Epifanova, Lucy O. Ojomoko, Svetlana Y. Belukhina, Nikita A. Prokopev, Mariia A. Landau, Yulia A. Palikova, Vitaly A. Kazakov, Natalia A. Borozdina, Arina V. Bervinova, Igor A. Dyachenko, Igor E. Kasheverov, Victor I. Tsetlin, Denis S. Kudryavtsev   +17 more
doaj   +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

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

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