Design, synthesis, and biological evaluation of conformationally constrained glycerol 3-phosphate acyltransferase inhibitors (Record no. 47239)

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control field MX-MdCICY
005 - DATE AND TIME OF LATEST TRANSACTION
control field 20250625153914.0
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Transcribing agency CICY
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Classification number (OCLC) (R) ; Classification number, CALL (RLIN) (NR) B-13037
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245 10 - TITLE STATEMENT
Title Design, synthesis, and biological evaluation of conformationally constrained glycerol 3-phosphate acyltransferase inhibitors
490 0# - SERIES STATEMENT
Volume/sequential designation Bioorganic & Medicinal Chemistry, 18(17), p.6470-6479, 2010
520 3# - SUMMARY, ETC.
Summary, etc. Glycerol 3-phosphate acyltransferase (GPAT)isozymes are central control points for fat synthesis in mammals. Development of inhibitors of these membrane-bound enzymes could lead to an effective treatment for obesity, but is thwarted by an absence of direct structural information. Based on a highly successful study involving conformationally constrained glycerol 3-phosphate analogs functioning as potent glycerol 3-phosphate dehydrogenase inhibitors, several series of cyclic bisubstrate and transition state analogs were designed, synthesized, and tested as GPAT inhibitors. The weaker in vitro inhibitory activity of these compounds compared to a previously described benzoic acid series was then examined in docking experiments with the soluble squash chloroplast GPAT crystal structure. These in silico experiments indicate that cyclopentyl and cyclohexyl scaffolds prepared in this study may be occluded from the enzyme active site by two protein loops that sterically guard the phosphate binding region. In view of these findings, future GPAT inhibitor design will be driven toward compounds based on planar frameworks able to slide between these loops and enter the active site, resulting in improved inhibitory activity.
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element GLYCEROL 3-PHOSPHATE ACYLTRANSFERASE
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element GPAT
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element OBESITY
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element TRIACYLGLYCEROL
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Wydysh, E.A.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Vadlamudi, A.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Medghalchi, S.M.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Townsend, C.A.
856 40 - ELECTRONIC LOCATION AND ACCESS
Uniform Resource Identifier <a href="https://drive.google.com/file/d/1YVymsWGI1VqR-lduLDMbPLCcOJcxhrtZ/view?usp=drivesdk">https://drive.google.com/file/d/1YVymsWGI1VqR-lduLDMbPLCcOJcxhrtZ/view?usp=drivesdk</a>
Public note Para ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx
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Source of classification or shelving scheme Clasificación local
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  Clasificación local     Ref1 CICY CICY Documento préstamo interbibliotecario 25.06.2025   B-13037 25.06.2025 25.06.2025 Documentos solicitados