Synthetic phospholipids as specific substrates for plasma endothelial lipase.

Papillon, Julien P N; Pan, Meihui; Brousseau, Margaret E; Gilchrist, Mark A; Lou, Changgang; Singh, Alok K; Stawicki, Todd; Thompson, James E

Papillon, Julien P N; Pan, Meihui; Brousseau, Margaret E; Gilchrist, Mark A; Lou, Changgang; Singh, Alok K; Stawicki, Todd; Thompson, James E.

Afiliação

Papillon JP; Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States. Electronic address: julien.papillon@novartis.com.
Pan M; Cardiovascular and Metabolism, Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, United States. Electronic address: meihui.pan@novartis.com.
Brousseau ME; Cardiovascular and Metabolism, Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, United States.
Gilchrist MA; Cardiovascular and Metabolism, Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, United States.
Lou C; Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.
Singh AK; Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.
Stawicki T; Cardiovascular and Metabolism, Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, United States.
Thompson JE; Cardiovascular and Metabolism, Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, United States.

Bioorg Med Chem Lett ; 26(15): 3514-7, 2016 08 01.

Article em En | MEDLINE | ID: mdl-27344207

ABSTRACT

ABSTRACT

We designed and prepared synthetic phospholipids that generate lyso-phosphatidylcholine products with a unique mass for convenient detection by LC-MS in complex biological matrices. We demonstrated that compound 4, formulated either as a Triton X-100 emulsion or incorporated in synthetic HDL particles can serve as a substrate for plasma EL with useful specificity.

Assuntos

Inibidores Enzimáticos/farmacologia; Lipase/antagonistas & inibidores; Fosfolipídeos/farmacologia; Relação Dose-Resposta a Droga; Inibidores Enzimáticos/síntese química; Inibidores Enzimáticos/química; Humanos; Lipase/sangue; Lipase/metabolismo; Estrutura Molecular; Fosfolipídeos/síntese química; Fosfolipídeos/química; Relação Estrutura-Atividade

Palavras-chave

Endothelial lipase; HPLCMS/MS; Lipid analysis; Lipid mass spectrometry; Plasma assay; Synthetic phospholipids; Tandem mass spectrometry

Texto completo

Adicionar na Minha BVS

Imprimir

XML

PubMed Links

Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fosfolipídeos / Inibidores Enzimáticos / Lipase Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de publicação: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM

Texto completo

Adicionar na Minha BVS

Imprimir

XML

PubMed Links

Buscar no Google