title: Synthesis and evaluation of isoleucine derived angiotensin II AT(2) receptor ligands.
abstract: Sixteen new C-terminally modified analogues of 2, a previously described potent and selective AT2R ligand, were designed, synthesized and evaluated for their affinity to the AT2R receptor. The introduction of large, hydrophobic substituents was shown to be beneficial and the most active compound (17, Ki=8.5 μM) was over 12-times more potent than the lead compound 2.
authors.affiliation: Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Center, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Jean-Baptiste
authors.initials: JB
authors.lastname: Veron
authors.affiliation: Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Center, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Advait
authors.initials: A
authors.lastname: Joshi
authors.affiliation: Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Center, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Charlotta
authors.initials: C
authors.lastname: Wallinder
authors.affiliation: Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Center, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Mats
authors.initials: M
authors.lastname: Larhed
authors.affiliation: Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Center, Box 574, SE-751 23 Uppsala, Sweden. Electronic address: luke.odell@orgfarm.uu.se.
authors.forename: Luke R
authors.initials: LR
authors.lastname: Odell
mesh_terms: D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods; D057809:HEK293 Cells; D006801:Humans; D007532:Isoleucine / Q000138:chemical synthesis* / Q000378:metabolism*; D008024:Ligands; D009842:Oligopeptides / Q000138:chemical synthesis / Q000378:metabolism; D011485:Protein Binding / Q000502:physiology; D044139:Receptor, Angiotensin, Type 2 / Q000378:metabolism*; D013552:Swine
chemical_list: D008024:Ligands; D009842:Oligopeptides; D044139:Receptor, Angiotensin, Type 2; D007532:Isoleucine; C060894:CGP 42112A
keywords: AT(1) receptor; AT(2) receptor; Angiotensin; Isoleucine