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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2010-5-6
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pubmed:abstractText |
Glucokinase (GK) is a glucose sensor that couples glucose metabolism to insulin release. The important role of GK in maintaining glucose homeostasis is illustrated in patients with GK mutations. In this publication, identification of the hit molecule 1 and its SAR development, which led to the discovery of potent allosteric GK activators 9a and 21a, is described. Compound 21a (RO0281675) was used to validate the clinical relevance of targeting GK to treat type 2 diabetes.
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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 |
May
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BizzarroFred TFT,
pubmed-author:CorbettWendy LWL,
pubmed-author:DvorozniakMark TMT,
pubmed-author:GrimsbyJosephJ,
pubmed-author:GrippoJoseph FJF,
pubmed-author:GuertinKevin RKR,
pubmed-author:HaynesNancy-EllenNE,
pubmed-author:HilliardDarryl WDW,
pubmed-author:HollandGeorge WGW,
pubmed-author:KesterRobert FRF,
pubmed-author:MahaneyPaige EPE,
pubmed-author:MatschinskyFranz MFM,
pubmed-author:QiLidaL,
pubmed-author:RailkarArunaA,
pubmed-author:SarabuRamakanthR,
pubmed-author:SpenceCheryl LCL,
pubmed-author:VissaV DVD
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pubmed:issnType |
Electronic
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pubmed:day |
13
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3618-25
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:20405948-Animals,
pubmed-meshheading:20405948-Blood Glucose,
pubmed-meshheading:20405948-Cell Line,
pubmed-meshheading:20405948-Cytotoxins,
pubmed-meshheading:20405948-Diabetes Mellitus, Type 2,
pubmed-meshheading:20405948-Dose-Response Relationship, Drug,
pubmed-meshheading:20405948-Drug Discovery,
pubmed-meshheading:20405948-Glucokinase,
pubmed-meshheading:20405948-Humans,
pubmed-meshheading:20405948-Hypoglycemic Agents,
pubmed-meshheading:20405948-Insulin,
pubmed-meshheading:20405948-Male,
pubmed-meshheading:20405948-Mice,
pubmed-meshheading:20405948-Pharmacokinetics,
pubmed-meshheading:20405948-Structure-Activity Relationship,
pubmed-meshheading:20405948-Sulfones,
pubmed-meshheading:20405948-Thiazoles
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675).
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pubmed:affiliation |
Department of Discovery Chemistry, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, New Jersey 07110, USA.
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pubmed:publicationType |
Journal Article
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