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J Biol Chem, Vol. 273, Issue 35, 22498-22505, August 28, 1998
From the Direct mapping of the interface between
parathyroid hormone (PTH) and its receptor (hPTH1-Rc) was carried out
by photoaffinity scanning studies. Photoreactive analogs of PTH
singularly substituted with a p-benzoylphenylalanine (Bpa)
at each of the first six N-terminal positions have been prepared. Among
these, the analog
[Bpa1,Nle8,18,Arg13,26,27,L-2-Nal23,Tyr34]bPTH-(1-34)NH2
(Bpa1-PTH-(1-34)) displayed in vitro
activity with potency similar to that of PTH-(1-34). The
radioiodinated analog 125I-Bpa1-PTH-(1-34)
cross-linked specifically to the hPTH1-Rc stably expressed in human
embryonic kidney cells. A series of chemical and enzymatic digestions
of the hPTH1-Rc-125I-Bpa1-PTH-(1-34)
conjugate suggested that a methionine residue (either Met414 or Met425) within the contact domain
hPTH1-Rc-(409-437), which includes the transmembrane helix 6 and part
of the third extracellular loop, as the putative contact point.
Site-directed mutagenesis (M414L or M425L) identified
Met425 as the putative contact point. Molecular modeling of
the hPTH1-Rc together with the NMR-derived high resolution structure of
hPTH-(1-34), guided by the cross-linking data, strongly supports
Met425, at the extracellular end of transmembrane helix 6, as the residue interacting with the N-terminal residue of the
hPTH-(1-34). The photocross-linking and molecular modeling studies
provide insight into the topologic arrangement of the receptor-ligand
complex.
Parathyroid Hormone-Receptor Interactions Identified Directly by
Photocross-linking and Molecular Modeling Studies
,,,, and
Division of Bone and Mineral Metabolism,
Charles A. Dana and Thorndike Laboratories, Department of Medicine,
Beth Israel Deaconess Medical Center and Harvard Medical School,
Boston, Massachusetts 02215, the § Department of
Pharmacology and Molecular Toxicology, University of Massachusetts
Medical School, Worcester, Massachusetts 01655, and the
¶ Department of Chemistry, Clark University,
Worcester, Massachusetts 01610
Copyright © 1998 by The American Society for Biochemistry and Molecular Biology, Inc.
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