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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
19
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pubmed:dateCreated |
2001-9-6
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pubmed:abstractText |
High throughput screening of our small molecule combinatorial library identified a class of benzoylnaphthalenehydrazones with modest affinity for the human glucagon receptor. Optimization of this initial hit through a series of targeted libraries and traditional medicinal chemistry led to ligands with nanomolar affinities. Pharmacological evaluation demonstrated that these ligands were competitive glucagon receptor antagonists. Intravenous administration of a representative benzoylnaphthalenehydrazone into rats attenuated glucagon-stimulated glucose levels.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AndererHH,
pubmed-author:GonzalezJJ,
pubmed-author:GregorVV,
pubmed-author:HonyKK,
pubmed-author:KiesMM,
pubmed-author:KnudsenL BLB,
pubmed-author:KukiAA,
pubmed-author:LakisJJ,
pubmed-author:LawHH,
pubmed-author:LinkMM,
pubmed-author:MayJJ,
pubmed-author:MurphyDD,
pubmed-author:PolinskyAA,
pubmed-author:PorterJJ,
pubmed-author:ShiSS,
pubmed-author:TestonKK
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pubmed:issnType |
Print
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pubmed:day |
13
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3141-9
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11543683-Animals,
pubmed-meshheading:11543683-Benzamides,
pubmed-meshheading:11543683-Binding, Competitive,
pubmed-meshheading:11543683-Blood Glucose,
pubmed-meshheading:11543683-Cell Line,
pubmed-meshheading:11543683-Combinatorial Chemistry Techniques,
pubmed-meshheading:11543683-Cyclic AMP,
pubmed-meshheading:11543683-Glucagon,
pubmed-meshheading:11543683-Humans,
pubmed-meshheading:11543683-Hydrazones,
pubmed-meshheading:11543683-Liver,
pubmed-meshheading:11543683-Male,
pubmed-meshheading:11543683-Radioligand Assay,
pubmed-meshheading:11543683-Rats,
pubmed-meshheading:11543683-Rats, Sprague-Dawley,
pubmed-meshheading:11543683-Rats, Wistar,
pubmed-meshheading:11543683-Receptors, Glucagon,
pubmed-meshheading:11543683-Structure-Activity Relationship
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pubmed:year |
2001
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pubmed:articleTitle |
Identification of alkylidene hydrazides as glucagon receptor antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Pfizer Global Research and Development, La Jolla/Agouron Pharmaceuticals, Inc., San Diego, CA 92121, USA. anthony.ling@agouron.com
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pubmed:publicationType |
Journal Article,
In Vitro
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