title: Inhibiting prolyl isomerase activity by hybrid organic-inorganic molecules containing rhodium(II) fragments.
abstract: A small molecule containing a rhodium(II) tetracarboxylate fragment is shown to be a potent inhibitor of the prolyl isomerase FKBP12. The use of small molecules conjugates of rhodium(II) is presented as a general strategy for developing new protein inhibitors based on distinct structural and sequence features of the enzyme active site.
authors.affiliation: Rice University, 6100 Main St, Houston, TX 70005, USA.
authors.forename: Jane M
authors.initials: JM
authors.lastname: Coughlin
authors.affiliation: Rice University, 6100 Main St, Houston, TX 70005, USA.
authors.forename: Rituparna
authors.initials: R
authors.lastname: Kundu
authors.affiliation: Rice University, 6100 Main St, Houston, TX 70005, USA.
authors.forename: Julian C
authors.initials: JC
authors.lastname: Cooper
authors.affiliation: Rice University, 6100 Main St, Houston, TX 70005, USA. Electronic address: zb1@rice.edu.
authors.forename: Zachary T
authors.initials: ZT
authors.lastname: Ball
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D019696:Peptidylprolyl Isomerase / Q000037:antagonists & inhibitors / Q000378:metabolism; D017434:Protein Structure, Tertiary; D012238:Rhodium / Q000737:chemistry* / Q000494:pharmacology; D022061:Tacrolimus Binding Protein 1A / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D012238:Rhodium; D022061:Tacrolimus Binding Protein 1A; D019696:Peptidylprolyl Isomerase
keywords: Enzyme inhibition; FKBP; Metallodrug; Prolyl isomerase; Rhodium