Conformational probes for elucidating the nature of substance P binding to the NK1 receptor: initial efforts to map the Phe7-Phe8 region.
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.
Tong
Y
Y
Department of Chemistry, Washington University, St. Louis, MO 63130, USA.
Fobian
Y M
YM
Wu
M
M
Boyd
N D
ND
Moeller
K D
KD
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*
D015335:Molecular Probes; D018040:Receptors, Neurokinin-1; D013373:Substance P; D010649:Phenylalanine