Results 41 to 50 of about 1,168,781 (390)

The β-blocker Nebivolol Is a GRK/β-arrestin Biased Agonist [PDF]

, 2013
Nebivolol, a third generation β-adrenoceptor (β-AR) antagonist (β-blocker), causes vasodilation by inducing nitric oxide (NO) production. The mechanism via which nebivolol induces NO production remains unknown, resulting in the genesis of much of the ...
Andresen, Bradley T., Bastepe, Murat, Blessing, Christopher P., Erickson, Catherine E., Gul, Rukhsana, Holowka, David, Jackson, Edwin K., Liu, Tammy, Nguyen, Jenny, Pulakat, Lakshmi   +9 more
core   +7 more sources

Intratumoral immunotherapy with TLR7/8 agonist MEDI9197 modulates the tumor microenvironment leading to enhanced activity when combined with other immunotherapies

Journal of Immunotherapy for Cancer, 2019
BackgroundImmune checkpoint blockade (ICB) promotes adaptive immunity and tumor regression in some cancer patients. However, in patients with immunologically “cold” tumors, tumor-resident innate immune cell activation may be required to prime an adaptive
Stefanie R. Mullins, J. Vasilakos, Katharina Deschler, Iwen F. Grigsby, P. Gillis, J. John, Matthew J. Elder, J. Swales, Elina Timosenko, Z. Cooper, S. Dovedi, A. Leishman, Nadia Luheshi, James Elvecrog, Ashenafi Y Tilahun, R. Goodwin, R. Herbst, M. Tomai, R. Wilkinson   +18 more
semanticscholar   +1 more source

A simple open source bioinformatic methodology for initial exploration of GPCR ligands’ agonistic/antagonistic properties

Pharmacology Research & Perspectives, 2020
Drug development is an arduous procedure, necessitating testing the interaction of a large number of potential candidates with potential interacting (macro)molecules.
Athanasios A. Panagiotopoulos, Christina Papachristofi, Konstantina Kalyvianaki, Panagiotis Malamos, Panayiotis A. Theodoropoulos, George Notas, Theodora Calogeropoulou, Elias Castanas, Marilena Kampa   +8 more
doaj   +1 more source

Predicting GPR40 Agonists with A Deep Learning‐Based Ensemble Model

ChemistryOpen, 2023
Recent studies have identified G protein‐coupled receptor 40 (GPR40) as a promising target for treating type 2 diabetes mellitus, and GPR40 agonists have several superior effects over other hypoglycemic drugs, including cardiovascular protection and ...
Jiamin Yang, Chen Jiang, Jing Chen, Dr. Lu‐Ping Qin, Dr. Gang Cheng   +4 more
doaj   +1 more source

RIG-I agonist SLR10 promotes macrophage M1 polarization during influenza virus infection

Frontiers in Immunology, 2023
RationaleA family of short synthetic, triphosphorylated stem-loop RNAs (SLRs) have been designed to activate the retinoic-acid-inducible gene I (RIG-I) pathway and induce a potent interferon (IFN) response, which may have therapeutic potential.
Wenxin Wu, Wei Zhang, Jeremy S. Alexandar, J. Leland Booth, Craig A. Miller, Chao Xu, Jordan P. Metcalf, Jordan P. Metcalf, Jordan P. Metcalf   +8 more
doaj   +1 more source

G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease [PDF]

, 2015
G protein-coupled receptor 35 (GPR35) is an orphan receptor, discovered in 1998, that has garnered interest as a potential therapeutic target through its association with a range of diseases.
Amanda E Mackenzie, Graeme eMilligan, Nina eDivorty, Nina eDivorty, Stuart A. Nicklin   +4 more
core   +3 more sources

Agonists and Partial Agonists of Rhodopsin:  Retinals with Ring Modifications [PDF]

Biochemistry, 2005
Activation of the visual pigment rhodopsin is initiated by isomerization of its retinal chromophore to the all-trans geometry, which drives the conformation of the protein to the active state. We have examined by FTIR spectroscopy the impact of a series of modifications at the ring of retinal on the activation process and on molecular interactions ...
Vogel, Reiner, Siebert, Friedrich, Lüdeke, Steffen, Hirshfeld, Amiram, Sheves, Mordechai   +4 more
openaire   +4 more sources

Immune Checkpoints as Therapeutic Targets in Autoimmunity

Frontiers in Immunology, 2018
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch, Christopher Paluch, Ana Mafalda Santos, Ana Mafalda Santos, Consuelo Anzilotti, Consuelo Anzilotti, Richard J. Cornall, Richard J. Cornall, Simon J. Davis, Simon J. Davis   +9 more
doaj   +1 more source

ChemR23 activation reprograms macrophages toward a less inflammatory phenotype and dampens carcinoma progression

Frontiers in Immunology, 2023
IntroductionTumor Associated Macrophages (TAM) are a major component of the tumor environment and their accumulation often correlates with poor prognosis by contributing to local inflammation, inhibition of anti-tumor immune response and resistance to ...
Margot Lavy, Vanessa Gauttier, Alison Dumont, Florian Chocteau, Sophie Deshayes, Judith Fresquet, Virginie Dehame, Virginie Dehame, Isabelle Girault, Charlène Trilleaud, Stéphanie Neyton, Caroline Mary, Philippe Juin, Philippe Juin, Nicolas Poirier, Sophie Barillé-Nion, Christophe Blanquart   +16 more
doaj   +1 more source

Cannabinoid receptor interacting protein suppresses agonist-driven CB1 receptor internalization and regulates receptor replenishment in an agonist-biased manner [PDF]

, 2016
Cannabinoid receptor interacting protein 1a (CRIP1a) is a CB1 receptor (CB1R) distal C-terminus-associated protein that modulates CB1R signaling via G proteins, and CB1R down-regulation but not desensitization (Blume et al.
Bass, Caroline E., Blumes, Lawrence C, Chen, Rong, Howlett, Allyn C., Leone-Kabler, Sandra, Luessen, Deborah J., Lyons, Erica, Marrs, Glenn S., Selley, Dana E.   +8 more
core   +2 more sources