Synthetic, enzyme kinetic, and protein crystallographic studies of C-β-D-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase

European Journal of Medicinal Chemistry

Volumn 123, Issue , 2016, Pages 737-745

  Kantsadi, Anastassia L ^a   Bokor, Éva ^b   Kun, Sándor ^b   Stravodimos, George A ^a   Chatzileontiadou, Demetra S M ^a   Leonidas, Demetres D ^a   Juhász Tóth, Éva ^b   Szakács, Andrea ^b   Batta, Gyula ^b   Docsa, Tibor ^c   Gergely, Pál ^c   Somsák, László ^b  

^a UNIVERSITY OF THESSALY   (Greece)

^b UNIVERSITY OF DEBRECEN   (Hungary)

^c UNIVERSITY OF DEBRECEN   (Hungary)

Author keywords

C Glucopyranosyl derivative; Diabetes type 2; Glycogen phosphorylase inhibitor; Imidazole; Indole; Pyrrole

Indexed keywords

GLUCOSE; GLYCOGEN PHOSPHORYLASE; IMIDAZOLE DERIVATIVE; INDOLE DERIVATIVE; NAPHTHYL GROUP; NITROGEN; PYRIDINE DERIVATIVE; PYRROLE DERIVATIVE; ENZYME INHIBITOR;

ARTICLE; BINDING SITE; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DEBENZYLATION; DRUG SYNTHESIS; ELECTROPHILICITY; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME KINETICS; GLYCOSYLATION; HUMAN; HYDROGEN BOND; HYDROGENOLYSIS; INHIBITION CONSTANT; NONHUMAN; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; NUCLEAR OVERHAUSER EFFECT; RABBIT; REACTION ANALYSIS; X RAY CRYSTALLOGRAPHY; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; ENZYMOLOGY; KINETICS; LIVER; METABOLISM; MOLECULAR MODEL; PROTEIN CONFORMATION; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ANIMALS; CHEMISTRY TECHNIQUES, SYNTHETIC; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; GLYCOGEN PHOSPHORYLASE; HUMANS; IMIDAZOLES; KINETICS; LIVER; MODELS, MOLECULAR; PROTEIN CONFORMATION; PYRROLES; RABBITS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84981275473     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2016.06.049     Document Type: Article

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