Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.

Animals Crystallography, X-Ray Drug Design Enzyme Inhibitors / chemistry Epoxide Hydrolases / antagonists & inhibitors HEK293 Cells Humans Mice Microsomes, Liver / drug effects PPAR gamma / agonists Polypharmacy Rats Structure-Activity Relationship

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
09 12 2021
Historique:
pubmed: 25 11 2021
medline: 22 1 2022
entrez: 24 11 2021
Statut: ppublish

Résumé

Polypharmaceutical regimens often impair treatment of patients with metabolic syndrome (MetS), a complex disease cluster, including obesity, hypertension, heart disease, and type II diabetes. Simultaneous targeting of soluble epoxide hydrolase (sEH) and peroxisome proliferator-activated receptor γ (PPARγ) synergistically counteracted MetS in various

Identifiants

DOI: 10.1021/acs.jmedchem.1c01331 PMID: 34818007
pubmed: 34818007
doi: 10.1021/acs.jmedchem.1c01331
doi:

Substances chimiques

Enzyme Inhibitors 0
PPAR gamma 0
Epoxide Hydrolases EC 3.3.2.-

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

17259-17276

Auteurs

Felix F Lillich (FF)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Sabine Willems (S)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
ORCID: 0000-0002-9755-3394

Xiaomin Ni (X)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe-University, Max-von-Laue-Str. 15, D-60438 Frankfurt, Germany.

Whitney Kilu (W)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Carmen Borkowsky (C)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Mirko Brodsky (M)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Jan S Kramer (JS)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Steffen Brunst (S)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Victor Hernandez-Olmos (V)

Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, D-60596 Frankfurt, Germany.

Jan Heering (J)

Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, D-60596 Frankfurt, Germany.
ORCID: 0000-0002-4922-1993

Simone Schierle (S)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Roxane-I Kestner (RI)

Department of Neurology, University Hospital Frankfurt, Goethe University, D-60590 Frankfurt am Main, Germany.

Franziska M Mayser (FM)

Department of Neurology, University Hospital Frankfurt, Goethe University, D-60590 Frankfurt am Main, Germany.

Moritz Helmstädter (M)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Tamara Göbel (T)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Lilia Weizel (L)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Dmitry Namgaladze (D)

Institute of Biochemistry I, University Hospital Frankfurt, Goethe University, D-60590 Frankfurt am Main, Germany.

Astrid Kaiser (A)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Dieter Steinhilber (D)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Waltraud Pfeilschifter (W)

Department of Neurology, University Hospital Frankfurt, Goethe University, D-60590 Frankfurt am Main, Germany.

Astrid S Kahnt (AS)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Anna Proschak (A)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Apirat Chaikuad (A)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe-University, Max-von-Laue-Str. 15, D-60438 Frankfurt, Germany.
ORCID: 0000-0003-1120-2209

Stefan Knapp (S)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe-University, Max-von-Laue-Str. 15, D-60438 Frankfurt, Germany.
ORCID: 0000-0001-5995-6494

Daniel Merk (D)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
ORCID: 0000-0002-5359-8128

Ewgenij Proschak (E)

Institute of Pharmaceutical Chemistry, Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, D-60596 Frankfurt, Germany.
ORCID: 0000-0003-1961-1859

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Epoxide hydrolase › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules HEK293 › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Récepteurs cytoplasmiques et nucléaires › Récepteur PPAR gamma › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Qualité, accès, évaluation des soins de santé › Prestations des soins de santé › Attitude envers la santé › Mésusage des services de santé › Surmédicalisation › Traitement excessif › Polypharmacie › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Structure-Based Design of Dual Partial...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Structure-Based Design of Dual Partial...