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J. Biol. Chem., Vol. 265, Issue 17, 9621-9627, Jun, 1990
LM Leeb-Lundberg and SA Mathis
We have examined the binding of [3H]bradykinin to bovine myometrial
membranes and assessed its sensitivity to guanine nucleotides. Total
binding displayed a typical B2 kinin receptor specificity. However,
saturation binding isotherms were resolved into at least two components
with KD values of 8 pM (45%) and 378 pM (55%). Low affinity binding
exhibited relatively rapid rates of association (kobs = 1.40 x 10(-2) s- 1)
and dissociation (k-1 = 3.82 x 10(-3) s-1), while high affinity binding
exhibited considerably slower rates (kobs = 9.52 x 10(-4) s-1 and k-1 =
4.43 x 10(-5) s-1). Pre-equilibrium dissociation kinetics revealed that
formation of high affinity binding was characterized as a time-dependent
accumulation of the slow dissociation rate at the expense of at least one
other more rapid dissociation rate. In the presence of 10 microM
guanyl-5'-yl imidodiphosphate (Gpp(NH)p), at least two binding components
were resolved with KD values of 37 pM (12%) and 444 pM (88%). Gpp(NH)p
apparently specifically perturbed high affinity binding by completely
preventing the accumulation of the slow dissociation phase. Instead, two
more rapid dissociation rates (k-1 = 8.53 x 10(-3) s-1 and 4.43 x 10(-4)
s-1) were observed. These results suggest that [3H]bradykinin interacts
with at least two B2 kinin receptor-like binding sites in bovine myometrial
membranes. A three- state model for the guanine nucleotide-sensitive
agonist interaction with the high affinity binding sites is proposed.
Guanine nucleotide regulation of B2 kinin receptors. Time-dependent formation of a guanine nucleotide-sensitive receptor state from which [3H]bradykinin dissociates slowly
Department of Biochemistry, University of Texas Health Science Center, San Antonio 78284-7760.
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