title: Conformational probes for elucidating the nature of substance P binding to the NK1 receptor: initial efforts to map the Phe7-Phe8 region.
abstract: Three substance P analogs with conformation constraints in the Phe7-Phe8 region have been prepared in connection with an effort to differentiate two families of potential conformations for the binding of substance P to its NK1 receptor. While the analogs did not bind the NK1 receptor with high affinity, the synthesis of the analogs demonstrated the utility of a general method for constructing piperazinone based peptidomimetics.
authors.affiliation: Department of Chemistry, Washington University, St. Louis, MO 63130, USA.
authors.forename: Y
authors.initials: Y
authors.lastname: Tong
authors.forename: Y M
authors.initials: YM
authors.lastname: Fobian
authors.forename: M
authors.initials: M
authors.lastname: Wu
authors.forename: N D
authors.initials: ND
authors.lastname: Boyd
authors.forename: K D
authors.initials: KD
authors.lastname: Moeller
mesh_terms: D000595:Amino Acid Sequence; D009682:Magnetic Resonance Spectroscopy; D015335:Molecular Probes; D010649:Phenylalanine / Q000737:chemistry*; D011487:Protein Conformation; D018040:Receptors, Neurokinin-1 / Q000378:metabolism*; D013373:Substance P / Q000737:chemistry / Q000378:metabolism*
chemical_list: D015335:Molecular Probes; D018040:Receptors, Neurokinin-1; D013373:Substance P; D010649:Phenylalanine