Results 161 to 170 of about 139,314 (301)

Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

, 2020
Drug discovery programs increasingly are focusing on allosteric modulators as a means to modify the activity of G protein-coupled receptor (GPCR) targets.
( K J G, K A E, C M N, P N V, A C C, M J N, J M R, Y Z, B A C, S R S, A S F, C W L, P J, A L R   +13 more
core  

The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned fear

, 2014
The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned ...
CE Handford (15829580), Jee Hyun Kim (13075509), S Tan (13447968), AJ Lawrence (5578280)   +3 more
core  

Allosteric Modulator [PDF]

, 2020
openaire   +1 more source

Identification and Characterization of a Phenyl(trifluoro-methyl)-pyrimidine Positive Allosteric Modulator of the Secretin Receptor. [PDF]

Membranes (Basel)
Harikumar KG, Dengler DG, Borrega Roman L, Ardecky R, Sergienko EA, Miller LJ.   +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

Positive allosteric modulator selective for adult muscle nicotinic acetylcholine receptor. [PDF]

Proc Natl Acad Sci U S A
Webster RG, Alabaf S, Li A, Beerli R, Siehler S, Imbert PE, Lee L, Cossins J, Koziczak-Holbro M, Flotte L, Gaudet L, Gerwin N, Beeson D, Dong YY.   +13 more
europepmc   +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

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

Discovery of VU6081679, a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor 8 with Efficacy in a Preclinical Model of Parkinson's Disease. [PDF]

ACS Chem Neurosci
Richardson AE, Ferranti AS, Peng L, Lei X, Han A, Qi A, Rodriguez AL, Chang S, Sant S, Zagol-Ikapitte I, Krishnan S, Thompson Gray A, Wilkinson JC, Kethanapalli SH, Cho HP, Temple KJ, Mi D, Days EL, Bauer JA, Wijesiri NK, Brown BP, Boutaud O, Jones CK, Engers DW, Lindsley CW, Niswender CM, Crocker KE.   +26 more
europepmc   +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