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First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters.
Hernandez-Olmos, Victor; Heering, Jan; Planz, Viktoria; Liu, Ting; Kaps, Alexander; Rajkumar, Rinusha; Gramzow, Matthias; Kaiser, Astrid; Schubert-Zsilavecz, Manfred; Parnham, Michael J; Windbergs, Maike; Steinhilber, Dieter; Proschak, Ewgenij.
Afiliação
  • Hernandez-Olmos V; Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Heering J; Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Planz V; Institute of Pharmaceutical Technology and Buchmann Institute for Molecular Life Sciences, Goethe University, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.
  • Liu T; Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Kaps A; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
  • Rajkumar R; Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Gramzow M; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
  • Kaiser A; Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Schubert-Zsilavecz M; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
  • Parnham MJ; Branch for Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
  • Windbergs M; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
  • Steinhilber D; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
  • Proschak E; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.
J Med Chem ; 63(20): 11548-11572, 2020 10 22.
Article em En | MEDLINE | ID: mdl-32946232
ABSTRACT
The first potent leukotriene B4 (LTB4) receptor type 2 (BLT2) agonists, endogenous 12(S)-hydroxyheptadeca-5Z,8E,10E-trienoic acid (12-HHT), and synthetic CAY10583 (CAY) have been recently described to accelerate wound healing by enhanced keratinocyte migration and indirect stimulation of fibroblast activity in diabetic rats. CAY represents a very valuable starting point for the development of novel wound-healing promoters. In this work, the first structure-activity relationship study for CAY scaffold-based BLT2 agonists is presented. The newly prepared derivatives showed promising in vitro wound-healing activity.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Cicatrização / Queratinócitos / Receptores do Leucotrieno B4 / Desenvolvimento de Medicamentos Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Cicatrização / Queratinócitos / Receptores do Leucotrieno B4 / Desenvolvimento de Medicamentos Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article