A family which segregates simultaneously for PGD, elliptocytosis, Rh, alphaFUC and PGM1 contains a recombinant suggesting that the loci lie in this order.
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http://dx.doi.org/10.1111/j.1469-1809.1977.tb01910.x | DOI Listing |
Biomolecules
December 2021
Research Centre for Natural Sciences, Institute of Organic Chemistry, Magyar Tudósok Körútja 2, 1117 Budapest, Hungary.
Connexin (Cx) proteins establish intercellular gap junction channels (Cx GJCs) through coupling of two apposed hexameric Cx hemichannels (Cx HCs, connexons). Pre- and post-GJ interfaces consist of extracellular EL1 and EL2 loops, each with three conserved cysteines. Previously, we reported that known peptide inhibitors, mimicking a variety of Cx43 sequences, appear non-selective when binding to homomeric Cx43 vs.
View Article and Find Full Text PDFEur J Med Chem
November 2015
Institute for Pharmaceutical and Medicinal Chemistry, Heinrich Heine University, Universitätsstr. 1, 40225 Düsseldorf, Germany. Electronic address:
TGR5 (Gpbar-1, M-Bar) is a class A G-protein coupled bile acid-sensing receptor predominately expressed in brain, liver and gastrointestinal tract, and a promising drug target for the treatment of metabolic disorders. Due to the lack of a crystal structure of TGR5, the development of TGR5 agonists has been guided by ligand-based approaches so far. Three binding mode models of bile acid derivatives have been presented recently.
View Article and Find Full Text PDFMol Pharmacol
December 2013
Department of Physiology and Biophysics, Institute for Computational Biomedicine, Weill Medical College of Cornell University, New York, New York (M.M., L.S.); Departments of Psychiatry and Pharmacology, Columbia University College of Physicians and Surgeons, New York, New York (P.D., L.D., Y.H., J.A.J.); Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (P.D., L.D., Y.H., J.A.J.); Schrödinger, Inc., New York, New York (T.B.); Medicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, Intramural Research Program of the National Institutes of Health National Institute on Drug Abuse, Baltimore, Maryland (A.B., A.H.N.); and Cisbio Bioassays, Codolet, France (T.R., E.T.).
Subtype-selective agents for the dopamine D3 receptor (D3R) have been considered as potential medications for drug addiction and other neuropsychiatric disorders. Medicinal chemistry efforts have led to the discovery of 4-phenylpiperazine derivatives that are >100-fold selective for the dopamine D3 receptor over dopamine D2 receptor (D2R), despite high sequence identity (78% in the transmembrane domain). Based on the recent crystal structure of D3R, we demonstrated that the 4-phenylpiperazine moiety in this class of D3R-selective compounds binds to the conserved orthosteric binding site, whereas the extended aryl amide moiety is oriented toward a divergent secondary binding pocket (SBP).
View Article and Find Full Text PDFA family which segregates simultaneously for PGD, elliptocytosis, Rh, alphaFUC and PGM1 contains a recombinant suggesting that the loci lie in this order.
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