Structural and molecular determinants of glutamate transporter allosteric modulators. [PDF]
Mol PharmacolReeb KL +8 more
europepmc +1 more source
, 2018 Allosteric modulators have drawn intense attention because of their high specificity and low toxicity relative to traditional compounds which bind to the orthosteric site of a target protein.
山浦 圭 +9 more
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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 +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 +4 more
wiley +1 more source
Bend and Snap: Computationally Exploring the Helix Bias for Classifying Abl Kinase Allosteric Modulators. [PDF]
J Chem Inf ModelLeite PTTF +7 more
europepmc +1 more source
Synthesis and Structure–Activity Relationships for Glutamate Transporter Allosteric Modulators
Excitatory amino acid transporters (EAATs) are essential CNS proteins that regulate glutamate levels. Excess glutamate release and alteration in EAAT expression are associated with several CNS disorders.
Yellamelli V.V. Srikanth (18391031) +11 more
core +1 more source
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 +18 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 +5 more
wiley +1 more source
Computational investigation for exploring botanical ingredients as potential negative allosteric modulators targeting metabotropic glutamate receptor 5. [PDF]
Res Pharm SciSingh P +4 more
europepmc +1 more source
Allosteric Modulators of the A1 Adenosine receptor
, 2011 The present invention provides compounds active as allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor, such as treatment of pain, in particular chronic pain
ROMAGNOLI, Romeo +2 more
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