Interaction of endothelin-1 with cloned bovine ETA receptors: biochemical parameters and functional consequences

Biochemistry
J DesmaretsC Frelin

Abstract

This paper defines the properties of interaction of endothelin-1 (Et-1) with cloned bovine ETA receptors. The Kd value of Et-1/ETA receptor complexes was estimated in membrane preparations to 20 pM using kinetic experiments and saturation experiments performed under quasi equilibrium conditions. Competition experiments yield a wide range of apparent Kd(Et-1) values from 20 pM to 1 nM which were in fact measures of the receptor concentrations rather than of Kd values. This resulted from the fact that complex second-order rate kinetics rather than pseudo-first-order kinetics control the association of Et-1 to its receptor when the receptor concentration is larger than Kd(Et-1). Et-1 induced a production of inositol phosphates with an apparent affinity of 2.3 nM, 100 times higher than the Kd(Et-1) value determined previously. Numerical simulation suggested that under time-limited conditions, sub-nanomolar rather than picomolar concentrations of Et-1 are necessary to occupy an important fraction of picomolar sites. It is concluded that bovine ETA receptors have a single affinity state for Et-1 (Kd = 20 pM) and that this affinity state can account for nanomolar actions of Et-1 in intact cells. It is suggested that the sensitivity of...Continue Reading

References

Dec 1, 1991·The American Journal of Physiology·R MarsaultC Frelin
Jan 1, 1991·The Journal of Clinical Investigation·C Serradeil-Le GalS Lotersztajn
Mar 1, 1995·British Journal of Pharmacology·P VigneC Frelin
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Citations

Mar 18, 1999·Biochemical and Biophysical Research Communications·J Desmarets, C Frelin
Aug 21, 2010·Canadian Journal of Physiology and Pharmacology·Faquan LiangKelly R Pitts
Jan 23, 2016·Cell Calcium·Cedric VieroPeter Lipp
Jul 28, 1999·Biochemical Pharmacology·P A ModestiG G Neri Serneri
Aug 18, 2010·Clinical Science·Marc Iglarz, Martine Clozel
May 7, 2014·La Presse médicale·Vincent Richard
Sep 7, 2016·Nature·Wataru ShihoyaTomoko Doi
Aug 16, 2006·Circulation·Xiao-Song ZhaoRalph V Shohet
Jan 28, 2005·Biochemistry and Cell Biology = Biochimie Et Biologie Cellulaire·Hala Farhat, Bruce G Allen
Nov 28, 2000·Molecular Pharmacology·V BlandinC Frelin

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