Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01496
Abstract: Discovery of potent selective inhibitors targeting a protein from a highly conserved family is challenging. Using a strategy combining structural and evolutionary information, we discovered transient receptor potential (TRP) subtype-selective inhibitors (transient receptor potential vanilloid… read more here.
Keywords: receptor potential; discovery; subtype selective; transient receptor ... See more keywords
Subtype selective γ-Aminobutyric Acid Type A Receptor (GABAAR) Modulators Acting at the Benzodiazepine Binding Site: An Update.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01312
Abstract: γ-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter within the central nervous system (CNS) with fast, trans-synaptic and modulatory extrasynaptic effects being mediated by the ionotropic GABA Type A receptors (GABAARs). These receptors are of… read more here.
Keywords: binding site; modulators acting; gabaar modulators; subtype selective ... See more keywords
Preclinical and Clinical Studies of Chidamide (CS055/HBI-8000), An Orally Available Subtype-selective HDAC Inhibitor for Cancer Therapy.
Sign Up to like & getrecommendations! Published in 2017 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520616666160901150427
Abstract: Epigenetic modifications play central roles in cellular differentiation and their deregulations really contribute to tumor development. Histone deacetylase (HDAC) enzymes can exert their functions in the epigenetic regulation of gene expression related to oncogenesis via… read more here.
Keywords: clinical studies; studies chidamide; cancer therapy; cancer ... See more keywords
Structural insights into the subtype-selective antagonist binding to the M2muscarinic receptor
Sign Up to like & getrecommendations! Published in 2018 at "Nature Chemical Biology"
DOI: 10.2210/pdb5yc8/pdb
Abstract: Human muscarinic receptor M2 is one of the five subtypes of muscarinic receptors belonging to the family of G-protein-coupled receptors. Muscarinic receptors are targets for multiple neurodegenerative diseases. The challenge has been designing subtype-selective ligands… read more here.
Keywords: muscarinic receptors; structural insights; receptor; subtype selective ... See more keywords