Results 1 to 10 of about 419,324 (239)

Identification of a Raloxifene Analog That Promotes AhR-Mediated Apoptosis in Cancer Cells

Biology, 2017
We previously reported that raloxifene, an estrogen receptor modulator, is also a ligand for the aryl hydrocarbon receptor (AhR). Raloxifene induces apoptosis in estrogen receptor-negative human cancer cells through the AhR.
Hyo Sang Jang, Martin Pearce, Edmond F. O’Donnell, Bach Duc Nguyen, Lisa Truong, Monica J. Mueller, William H. Bisson, Nancy I. Kerkvliet, Robert L. Tanguay, Siva Kumar Kolluri   +9 more
doaj   +1 more source

Managing Opioid Addiction in Adolescents in the Community: Experiences from Two Cases

Journal of Mental Health and Human Behaviour
Introduction: Adolescent opioid use in India has emerged as a critical public health concern, with a 2018 survey revealing 1.8% of adolescents aged 10–17 years as past-year opioid users.
Manmeet Kaur Brar, Biswadip Chatterjee, Siddharth Sarkar, Brahm Prakash   +3 more
doaj   +1 more source

Adenosine A1 Receptor Agonist 2-chloro-N6-cyclopentyladenosine and Hippocampal Excitability During Brain Development in Rats

Frontiers in Pharmacology, 2019
Objective: The adenosinergic system may influence excitability in the brain. Endogenous and exogenous adenosine has anticonvulsant activity presumably by activating A1 receptors.
Petr Fabera, Petr Fabera, Martina Parizkova, Martina Parizkova, Libor Uttl, Libor Uttl, Katerina Vondrakova, Katerina Vondrakova, Hana Kubova, Grygoriy Tsenov, Grygoriy Tsenov, Pavel Mares   +11 more
doaj   +1 more source

Chemerin Elicits Potent Constrictor Actions via Chemokine‐Like Receptor 1 (CMKLR1), not G‐Protein‐Coupled Receptor 1 (GPR1), in Human and Rat Vasculature

Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2016
BackgroundCirculating levels of chemerin are significantly higher in hypertensive patients and positively correlate with blood pressure. Chemerin activates chemokine‐like receptor 1 (CMKLR1 or ChemR23) and is proposed to activate the “orphan” G‐protein ...
Amanda J. Kennedy, Peiran Yang, Cai Read, Rhoda E. Kuc, Lucy Yang, Emily J. A. Taylor, Colin W. Taylor, Janet J. Maguire, Anthony P. Davenport   +8 more
doaj   +1 more source

The different effects of four adenosine receptors in liver fibrosis

Frontiers in Pharmacology
BackgroundThe adenosine–adenosine receptor pathway plays important roles in the immune system and inflammation. Four adenosine receptors (i.e., A1R, A2AR, A2BR, and A3R) have been identified.
Lan Yang, Zhao-wei Gao, Xi Wang, Xia-nan Wu, Si-min Li, Ke Dong, Xiao-ming Zhu   +6 more
doaj   +1 more source

Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives

Frontiers in Chemistry, 2019
Among the other members of the adhesion molecules' family, α4β1 integrin, a heterodimeric receptor, plays a crucial role in inflammatory diseases, cancer development, metastasis and stem cell mobilization or retention.
Monica Baiula, Santi Spampinato, Luca Gentilucci, Alessandra Tolomelli   +3 more
doaj   +1 more source

Identification and Semi-Synthesis of 3-O-Protocatechuoylceanothic Acid, a Novel and Natural GPR120 Agonist †

Molecules, 2019
The identification and three step synthesis of 3-O-protocatechuoylceanothic acid, a novel and natural GPR120 agonist, is described. This ceanothane-type triterpenoid was identified from the components of Ziziphus jujuba roots and was found to be a new ...
Changjin Lim, Jung Gyu Park, Kyo Bin Kang, Young-Ger Suh   +3 more
doaj   +1 more source

MEDI1873, a potent, stabilized hexameric agonist of human GITR with regulatory T-cell targeting potential

OncoImmunology, 2017
Glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) is part of a system of signals involved in controlling T-cell activation. Targeting and agonizing GITR in mice promotes antitumor immunity by enhancing the function of effector ...
Natalie J. Tigue, Lisa Bamber, John Andrews, Samantha Ireland, James Hair, Edward Carter, Sudharsan Sridharan, Jelena Jovanović, D. Gareth Rees, Jeremy S. Springall, Emilie Solier, Yi-Ming Li, Matthieu Chodorge, David Perez-Martinez, Daniel R. Higazi, Michael Oberst, Maureen Kennedy, Chelsea M. Black, Li Yan, Martin Schwickart, Shaun Maguire, Jennifer A. Cann, Lolke de Haan, Lesley L. Young, Tristan Vaughan, Robert W. Wilkinson, Ross Stewart   +26 more
doaj   +1 more source

Structural Changes Due to Antagonist Binding in Ligand Binding Pocket of Androgen Receptor Elucidated Through Molecular Dynamics Simulations

Frontiers in Pharmacology, 2018
When a small molecule binds to the androgen receptor (AR), a conformational change can occur which impacts subsequent binding of co-regulator proteins and DNA.
Sugunadevi Sakkiah, Rebecca Kusko, Bohu Pan, Wenjing Guo, Weigong Ge, Weida Tong, Huixiao Hong   +6 more
doaj   +1 more source

Discovery of a Novel Chemo-Type for TAAR1 Agonism via Molecular Modeling

Molecules
The search for novel effective TAAR1 ligands continues to draw great attention due to the wide range of pharmacological applications related to TAAR1 targeting. Herein, molecular docking studies of known TAAR1 ligands, characterized by an oxazoline core,
Giancarlo Grossi, Naomi Scarano, Francesca Musumeci, Michele Tonelli, Evgeny Kanov, Anna Carbone, Paola Fossa, Raul R. Gainetdinov, Elena Cichero, Silvia Schenone   +9 more
doaj   +1 more source