Abstracts of papers Pharmacological Meeting

Bax, Willem A.; Biewenga, Gerreke Ph.; Jong, J. T.L.; Bloemen, P. G. M.; Tweel, M. C. van den; Molewijk, H.E.; Poel, A. M. Der Van; Olivier, Berend; Briejer, M.R.; Schuurkes, J. A. J.; Akkermans, L.M.A.; Bruning, T. A.; Hendriks, M. G. C.; Chang, P. C.; Kuypers, Elke; Zwieten, P. A. van; Cappendijk, Susan L.T.; Vries, René de; Dzoljic, M.R.; Bouwknecht, J. Adriaan; Crijns, F. R. L.; Huijberts, M. S. P.; Boudier, H. A. J. Struijker; Kruzeman, A. C. Nieuwenhuijzen; Wolffenbuttel, Bruce H. R.; Lannov, L. M.; Danser, A.H.J.; Schoemakef, R. G.; Schalekamp, M. A. D. H.; Du, Xiao Y.; Dubois, Éric; Batink, H. D.; Pfaffendorf, M.; Roven, E. A.; Garrelds, Ingrid M.; Veld, C. Graaf-in 't; Ziilstra, F. J.; Jansen, A.P.; Wijk, R. Gerth van; Gho, B. C. G.; Schoemaker, Regien G.; Lee, C. v. d.; Sharma, Hari Shanker; Verdouw, P. D.; Groenink, Lucianne; Gugten, Jan van der; Zethof, T. J. J.; Hasselaar, P.; Jansen, J.W.C.M.; Giezen, J.J.J. van; Dreteler, G.H.; Hulkenberq, A.; Reinders, Jan Hendrik; Toorop, G. P.; Herremans, Arnoud H.J.; Hijzen, Theo H.; Slangen, J. L.; Hessel, E. M.; Oosterhout, Antoon J. M. van; Hofstra, C.; Garssen, J.; Loveren, Henk Van; Savelkoul, H. F. J.; Nijkamp, Frans P.; Hol, T.; Ree, Jan M. van; Spruijt, Berry M.; Hüsken, B. C. P.; Zwieren, P. A.; Kalkman, Ed A.J.; Kam, K. L.; Keuzenkamp-Jansen, C.W.; Abreu, R. A.; Bökkerink, J. P. M.; Heijden, M. A. H.; Trijbels, J. M. F.; Kraneveld, Aletta D.; Schaik, Y.; Koster, A. Sj.; Mathôt, Ron A. A.; Aarsen, B. C. F. M.; Langemeijer, M. W. E.; Ijzerman, A. P.; Danhof, Meindert; Mohede, I.C.M.; Monshouwer, Mario; Witkamp, R.F.; Nijmeijer, S. M.; Miert, A. S. J. P. A. M. van; Oosting, Jan; Janssen, Ben J. A.; Pijl, A. J.; Wal, A. C.; Mathy, Marie-Jeanne; Pruimboom, W. M.; Dijk, A. P. M. van; Tak, C. J. A. M.; Bonta, I. L.; Wilson, Janet; Bac, Dirk Jan; Zijlstra, Freek J.; Hashjin, Gudarz Sadeghi; Folkerts, Gert; Henricks, Paul A.J.; Santing, Ruud E.; Pasman, Y.; Olymulder, Clemens G.; Roffel, Ad F.; Zaaqsma, J.; Meurs, Herman; Scheerens, Heleen; Buckley, Theresa L.; Sipma, Henk; Duin, Martin van; Hertog, Adriaan den; Nelemans, Adriaan; Smit, Jolanda M.; Coppes, Rob; Geurtsen, Alwin; Zaagsma, J.; Smit, Martine J.; Leurs, Rob; Bast, Aalt; Timmerman, H.; Stassen, Frank R. M.; Mey, Jo G. R. De; Berge, Ronald; Tjon, Guno H.K.; Vries, Taco J.; Ronken, Eric; Hogenboom, F.; Warden, George; Mulder, Arie H.; Schoffelmeer, Anton N. M.; Bergen, P. Van; Kleline, J. A.; Janssen, Paul M. L.; Vaart, Jan G.M. Van Der; Kasbergen, C. M.; Versteeg, Dirk H.G.; Wildt, Dick J. De; Velde, Marco J. van de; Engels, Ferdi; Berg, C.; Vleeming, W.; Amsterdam, Jan van; Werner, J.; Zee, Lucie van der; Hertoe, A.; Gelderen, E. Marcel van; Agteresch, Hendrik J.; Bruijne, E.L.E. de; Saxena, Pramod R.; Kats, Jorge P. van; Sassen, L. M. A.; Admiraal, P. J. J.; Verdouw, P. P.; Muiswinkel, F. L. Van; Steinhusch, H. W. M.; Drukarch, Benjamin; Sloof, J. C.; Vente, Jan de; Vanderschuren, Louk J. M. J.; Verkade, P.; Verkleij, A.J.; Gispen, Willem Hendrik; Oestreicher, A.B.; Vermeulen, R. Jeroen; Goosen, C.; Wolters, Erik Ch.; Stoof, Johannes C.; Vincent, V.A.M.; Steinbush, H. W. M.; Berlcenbosch, F.; Voss, Hans–Peter; Donnell, David; Wesselman, Jos P. M.; vanBavel, Ed; Spaan, J. A. E.; Zeilmaker, W. M.; Klooster, G. A. E. T; Horbach, G. Jean; Zhang, J.; Zhang, J. S.; Meet, J. C. A.

doi:10.1007/bf01875421

Cited by 1 publication

(1 citation statement)

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“…Endothelin analogs BQ3020 is a endothelin receptor ligand in which the Cys residues in the C-terminus, involved in disulphide bridges, are replaced by L-Ala residues (39). A chimera between galanin( 1-1 3) and BQ3020 was synthesised and tested for its affinity for galanin receptors.…”

Section: Leuenkephaline Analogsmentioning

confidence: 99%

Novel galanin receptor ligands

Pooga

Rezaei

Hasanvan

et al. 1998

The Journal of Peptide Research

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Galanin is a neuroendocrine peptide which is 29/30 amino acids in length and is recognised by G‐protein‐coupled central nervous system receptors via its N‐terminus. We synthesised several galanin receptor ligands and fragments around C‐terminal extensions of galanin(l‐13) to yield chimeric peptides with C‐terminals corresponding to bioactive peptides like bradykinin(2‐9), mastoparan, neuropeptide Y(25‐36) or substance P(5‐11), respectively. We also synthesised short galanin analogs in which galanin(l‐13) was C‐terminally elongated with Lys14; different pharmacologically active small molecules were then attached to the ε‐amino group of Lys14. Several cysteine‐substituted linear and ring closed analogs of galanin(l‐9) and galanin(l‐16) were also synthesised. The equilibrium binding constants for these peptides at hypothalamic galanin receptors were determined and found in the subnanomolar to micromolar range. The large number of peptides and their binding affinities presented here permit structure‐activity relationship analysis of peptide‐type ligands to galanin receptors.

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Section: Leuenkephaline Analogsmentioning

confidence: 99%