Results 151 to 160 of about 3,750,504 (279)

Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype [PDF]

ACS Medicinal Chemistry Letters, 2013
openaire   +2 more sources

Molecular Modeling Study of Receptor-Orthosteric Ligand-Allosteric Modulator Signaling Complex

, 2022
Allosteric modulators (AMs) are always the hotspot in research for their higher selectivity and various effects on the orthosteric ligands (OL), whereas AMs are also classified in terms of its functionalities as positive, negative, or silent allosteric ...
Jiang, Chen
core  

Effect of the Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulator Dipraglurant on Motor and Non-Motor Symptoms of Parkinson's Disease. [PDF]

Cells, 2023
Epping-Jordan MP, Girard F, Bessis AS, Mutel V, Boléa C, Derouet F, Bessif A, Mingard B, Barbier S, Paradis JS, Rocher JP, Lütjens R, Kalinichev M, Poli S.   +13 more
europepmc   +1 more source

Pharmacological characterization of cannabidiol as a negative allosteric modulator of the 5-HT2A receptor

Promising clinical evidence suggests that psychedelic compounds, like lysergic acid diethylamide (LSD), have therapeutic value for treatment of psychiatric disorders.
De Gregorio, Danilo, Billard, Etienne, Grant, Emily, Bertazzo, Antonella, Chatenet, David, Comai, Stefano, Gobbi, Gabriella, Torbey, Alexandre, Hébert, Terence E., Inserra, Antonio   +9 more
core   +2 more sources

Structure of the human P2X3 receptor reveals the basis for subtype-selective inhibition by sivopixant.

PLoS Biology
P2X receptors are ATP-gated cation channels, and the P2X3 subtype plays crucial roles in peripheral sensory neurons, including in chronic pain and chronic cough.
Zhixuan Zhao, Dong-Ping Wang, Xin Zhang, Yuan Gao, Hexin Xu, Xinyu Teng, Cheng Shen, Jirui Chen, Jinru Zhang, Chang-Run Guo, Motoyuki Hattori   +10 more
doaj   +1 more source

Long-term α5 GABA A receptor negative allosteric modulator treatment reduces NMDAR-mediated neuronal excitation and maintains basal neuronal inhibition. [PDF]

Neuropharmacology, 2023
Nuwer JL, Povysheva N, Jacob TC.
europepmc   +1 more source

Changes in social, sexual, and hedonic behaviors in rats in response to stress and restoration by a negative allosteric modulator of α5-subunit containing GABA receptor. [PDF]

Behav Brain Res, 2023
Bailey AM, Barrett A, Havens L, Leyder E, Merchant T, Starnes H, Thompson SM.   +6 more
europepmc   +1 more source

MDL‐800‐induced SIRT6 activation decreases age‐associated osteoarthritis in mice

Arthritis &Rheumatology, Accepted Article.
Objective SIRT6 is a nuclear‐localized histone deacetylase that regulates multiple pathways associated with aging. This study aimed to determine whether systemic administration of a small molecule activator of SIRT6, MDL‐800, decreases the severity of age‐associated osteoarthritis (OA) in mice.
Matheus Moreira Perez, Pranay Ramteke, Bahiyah Watson, Owen Haslam, Eirene Choi, Susan Chubinskaya, Mandy J. Peffers, William R. Davis, Jacqueline Shine, Brian O. Diekman, Richard F. Loeser, Theresa A. Freeman, Makarand V. Risbud, John A. Collins   +13 more
wiley   +1 more source

Harnessing ferroptosis from multilayer defense networks to nanoplatforms for specific cancer therapy

BMEMat, EarlyView.
Nanomaterials target metabolically‐regulated ferroptosis for cancer therapy. Iron‐based or alternative nanoplatforms integrate ferroptosis with chemotherapy, immunotherapy, or radiotherapy. They enable stimulus‐responsive therapies (photothermal, photodynamic, sonodynamic) activated by near‐infrared, light, or ultrasound, achieving potent synergistic ...
Xinyue Xu, Xuejian Wang, Wenyan Jiang, Wan Hairul Anuar Kamaruddin, Chunyan Fang, Pengfei Zhang   +5 more
wiley   +1 more source

An aptamer agonist of the insulin receptor acts as a positive or negative allosteric modulator, depending on its concentration. [PDF]

Exp Mol Med, 2022
Yunn NO, Lee J, Lee HS, Oh EJ, Park M, Park S, Jin SY, Shin E, Lee JWY, Kim Y, Bae SS, Ryu SH.   +11 more
europepmc   +1 more source