Structure-based identification and characterisation of structurally novel human P2X7 receptor antagonists

Biochemical Pharmacology

Volumn 116, Issue , 2016, Pages 130-139

  Caseley, Emily A ^a   Muench, Stephen P ^a   Fishwick, Colin W ^a   Jiang, Lin Hua ^a  

^a UNIVERSITY OF LEEDS   (United Kingdom)

Author keywords

Ca2+ imaging; hP2X7R antagonists; Patch clamp recording; Virtual screening; YO PRO 1 dye uptake

Indexed keywords

ADENOSINE TRIPHOSPHATE; CALCIUM; PURINERGIC P2X3 RECEPTOR; PURINERGIC P2X4 RECEPTOR; PURINERGIC P2X7 RECEPTOR; PURINERGIC P2X7 RECEPTOR ANTAGONIST; PURINERGIC RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; 3'-O-(4-BENZOYL)BENZOYLADENOSINE 5'-TRIPHOSPHATE; AMIDE; INDOLE DERIVATIVE; LIGAND; MOLECULAR LIBRARY; NONSTEROID ANTIINFLAMMATORY AGENT; P2RX3 PROTEIN, RAT; P2RX4 PROTEIN, HUMAN; P2XR RECEPTOR, HUMAN; PURINERGIC P2X RECEPTOR ANTAGONIST; RECOMBINANT PROTEIN; THIOPHENE DERIVATIVE; ZINC09315614; ZINC58368839; ZINC67825876;

ARTICLE; CELL DEATH; CHANNEL GATING; CONCENTRATION RESPONSE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG SCREENING; HUMAN; HUMAN CELL; IC50; PATCH CLAMP TECHNIQUE; PRIORITY JOURNAL; PROPIDIUM IODIDE ASSAY; ZEBRA FISH; ANALOGS AND DERIVATIVES; ANIMAL; BINDING SITE; CALCIUM SIGNALING; CHEMISTRY; CYTOLOGY; DRUG EFFECTS; FLUORESCENCE MICROSCOPY; GENETICS; HEK293 CELL LINE; IMAGE PROCESSING; LIVER CELL; METABOLISM; MOLECULAR LIBRARY; MOLECULAR MODEL; RAT; SINGLE CELL ANALYSIS; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; AMIDES; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; BINDING SITES; CALCIUM SIGNALING; HEK293 CELLS; HEPATOCYTES; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; INDOLES; LIGANDS; MICROSCOPY, FLUORESCENCE; MODELS, MOLECULAR; PATCH-CLAMP TECHNIQUES; PURINERGIC P2X RECEPTOR ANTAGONISTS; RATS; RECEPTORS, PURINERGIC P2X3; RECEPTORS, PURINERGIC P2X4; RECEPTORS, PURINERGIC P2X7; RECOMBINANT PROTEINS; SINGLE-CELL ANALYSIS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES;

EID: 84983789002     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2016.07.020     Document Type: Article

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