Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes.

Chen, Yueyi; Sonawane, Amol; Manda, Rajesh; Gadi, Ranjith Kumar; Tesmer, John J G; Ghosh, Arun K

Chen, Yueyi; Sonawane, Amol; Manda, Rajesh; Gadi, Ranjith Kumar; Tesmer, John J G; Ghosh, Arun K.

Affiliation

Chen Y; Department of Biological Sciences, Purdue University, West Lafayette, IN, 47907, USA; Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Sonawane A; Department of Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
Manda R; Department of Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
Gadi RK; Department of Chemistry, Purdue University, West Lafayette, IN, 47907, USA.
Tesmer JJG; Department of Biological Sciences, Purdue University, West Lafayette, IN, 47907, USA; Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.
Ghosh AK; Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA; Department of Chemistry, Purdue University, West Lafayette, IN, 47907, USA. Electronic address: akghosh@purdue.edu.

Eur J Med Chem ; 264: 115931, 2024 Jan 15.

Article in En | MEDLINE | ID: mdl-38016297

Subject(s)

Heart Failure; Humans; Binding Sites; Receptors, G-Protein-Coupled

Key words

Covalent; GRK5 inhibitors; Reversible; Sunitinib; Synthesis; X-ray crystal structure

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Heart Failure Limits: Humans Language: En Journal: Eur J Med Chem Year: 2024 Document type: Article Affiliation country: United States Country of publication: France

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