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Novel Inhibitors of Nicotinamide-N-Methyltransferase for the Treatment of Metabolic Disorders.
Kannt, Aimo; Rajagopal, Sridharan; Hallur, Mahanandeesha S; Swamy, Indu; Kristam, Rajendra; Dhakshinamoorthy, Saravanakumar; Czech, Joerg; Zech, Gernot; Schreuder, Herman; Ruf, Sven.
Afiliación
  • Kannt A; Fraunhofer Institute for Translational Medicine and Pharmacology-ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Rajagopal S; Jubilant Biosys Limited, #96, Industrial Suburb, 2nd Stage Yeshwanthpur, Bangalore 560022, India.
  • Hallur MS; Jubilant Biosys Limited, #96, Industrial Suburb, 2nd Stage Yeshwanthpur, Bangalore 560022, India.
  • Swamy I; Jubilant Biosys Limited, #96, Industrial Suburb, 2nd Stage Yeshwanthpur, Bangalore 560022, India.
  • Kristam R; Jubilant Biosys Limited, #96, Industrial Suburb, 2nd Stage Yeshwanthpur, Bangalore 560022, India.
  • Dhakshinamoorthy S; Jubilant Biosys Limited, #96, Industrial Suburb, 2nd Stage Yeshwanthpur, Bangalore 560022, India.
  • Czech J; Sanofi-Aventis Deutschland Gmbh, Industriepark Hoechst, 65926 Frankfurt am Main, Germany.
  • Zech G; Sanofi-Aventis Deutschland Gmbh, Industriepark Hoechst, 65926 Frankfurt am Main, Germany.
  • Schreuder H; Sanofi-Aventis Deutschland Gmbh, Industriepark Hoechst, 65926 Frankfurt am Main, Germany.
  • Ruf S; Sanofi-Aventis Deutschland Gmbh, Industriepark Hoechst, 65926 Frankfurt am Main, Germany.
Molecules ; 26(4)2021 Feb 13.
Article en En | MEDLINE | ID: mdl-33668468
Nicotinamide-N-methyltransferase (NNMT) is a cytosolic enzyme catalyzing the transfer of a methyl group from S-adenosyl-methionine (SAM) to nicotinamide (Nam). It is expressed in many tissues including the liver, adipose tissue, and skeletal muscle. Its expression in several cancer cell lines has been widely discussed in the literature, and recent work established a link between NNMT expression and metabolic diseases. Here we describe our approach to identify potent small molecule inhibitors of NNMT featuring different binding modes as elucidated by X-ray crystallographic studies.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Nicotinamida N-Metiltransferasa / Enfermedades Metabólicas Límite: Animals / Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Nicotinamida N-Metiltransferasa / Enfermedades Metabólicas Límite: Animals / Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2021 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Suiza