Results 151 to 160 of about 702,558 (291)

Neurotransmitter‐Defined Degeneration Patterns in Sporadic and C9orf72‐Associated Amyotrophic Lateral Sclerosis: Predilection to GABAergic, Serotonergic, Opioid, Glutamatergic, Endocannabinoid, and Microglial Systems—Implications for Therapy Development

Annals of Neurology, EarlyView.
Objective Amyotrophic lateral sclerosis (ALS) has a markedly distinctive clinical and neuroradiological signature, with the preferential involvement of specific brain networks and the apparent sparing of others. The molecular underpinnings of the strikingly selective anatomical vulnerability have not been fully elucidated to date despite the potential ...
Marlene Tahedl, We Fong Siah, Jasmin Lope, Jennifer C. Hengeveld, Mark A. Doherty, Russell L. McLaughlin, Orla Hardiman, Ee Ling Tan, Alison Toomey, Jana Kleinerova, Peter Bede   +10 more
wiley   +1 more source

Evaluation of allosteric NMDA receptor modulation by GluN2A-selective antagonists using pharmacological equilibrium modeling

NMDA-type ionotropic glutamate receptors are critically involved in excitatory neurotransmission and their dysfunction is implicated in many brain disorders.
Volkmann, Robert A, Zhao, Fabao, Jones, Jaron, Hansen, Kasper B, Yi, Feng, Menniti, Frank S, Farnsworth, Jill C, Clausen, Rasmus P, Lotti, James S   +8 more
core   +1 more source

Allosteric Modulator [PDF]

, 2020
openaire   +1 more source

Structure-guided allosteric modulation of the delta opioid receptor. [PDF]

Nat Commun
Mobbs JI, Nguyen MD, Deo O, Bartuzi D, Venugopal H, Alvi S, Pham V, Barnes N, Christopoulos A, Poole DP, Carbone SE, Jörg M, Capuano B, Carlsson J, Gondin AB, Scammells PJ, Valant C, Thal DM.   +17 more
europepmc   +1 more source

Structural and mechanistic insights into gating and allosteric modulation of GluN1-GluN3A NMDA receptors. [PDF]

Nat Struct Mol Biol
Kim J, Benton AJ, Lotti JS, Rouzbeh N, Hansen KB, Gouaux E.   +5 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

Zuranolone: A case study in (regulatory) rush to judgement?

British Journal of Clinical Pharmacology, EarlyView.
Abstract Sage, in collaboration with Biogen, submitted a new drug approval for zuranolone for postpartum depression (PPD) and major depressive disorder (MDD) in December 2022. In August 2023, the US Food and Drug Administration granted approval for PPD but denied approval for MDD.
Lisa Cosgrove, Milutin Kostic, Barbara Mintzes, Gianna D'Ambrozio, Allen Shaughnessy   +4 more
wiley   +1 more source

Targeted Mutations Activate Allosteric Modulation of α5-Containing Nicotinic Acetylcholine Receptors. [PDF]

ACS Chem Neurosci
Marotta CB, Lester HA, Dougherty DA.
europepmc   +1 more source

The Korea Chemical Bank: Over 25 years of national chemical infrastructure alongside KRICT's 50‐year journey

Bulletin of the Korean Chemical Society, EarlyView.
This graphic abstract illustrates the role of the Korea Chemical Bank (KCB) as a central national hub that integrates government R&D, academic compound deposits, and industrial drug discovery throughout the latter half of KRICT's 50‐year history. Abstract Since its establishment in 2000 under the Korea Research Institute of Chemical Technology (KRICT),
Seul‐Gee Hwang, Su‐Min Kang, Soon Hee Hwang, Yuri Lee, Suyoun Lee, Ho‐Jin Kwon, Sunjong Yu, Soo Hee Kim, Eun Suk An, Sun Ho Kim, Sun Woo Kim, Hyeon Kyu Lee, Min Sung Kim, Seung Yeon Lee, Mali Prakash, Jaehyeon Park, Gehyeong Lee, Yuno Lee, Nam‐Chul Cho   +18 more
wiley   +1 more source

G Protein-Mediated Allosteric Modulation of Ligand Binding in Class A GPCRs: Receptor-Ligand-Transducer Ensembles in Disease and Drug Discovery. [PDF]

Pharmaceuticals (Basel)
Kurihara Y, Kurihara H.
europepmc   +1 more source