Literature DB >> 26004579

Recent advances for FLAP inhibitors.

Daniel Pettersen1, Öjvind Davidsson2, Carl Whatling2.   

Abstract

A number of FLAP inhibitors have been progressed to clinical trials for respiratory and other inflammatory indications but so far no drug has reached the market. With this Digest we assess the opportunity to develop FLAP inhibitors for indications beyond respiratory disease, and in particular for atherosclerotic cardiovascular disease. We also show how recently disclosed FLAP inhibitors have structurally evolved from the first generation FLAP inhibitors paving the way for new compound classes.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  5-LO; Cardiovascular; FLAP; Inflammatory; Leukotrienes

Mesh:

Substances:

Year:  2015        PMID: 26004579     DOI: 10.1016/j.bmcl.2015.04.090

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  Androgen-mediated sex bias impairs efficiency of leukotriene biosynthesis inhibitors in males.

Authors:  Simona Pace; Carlo Pergola; Friederike Dehm; Antonietta Rossi; Jana Gerstmeier; Fabiana Troisi; Helmut Pein; Anja M Schaible; Christina Weinigel; Silke Rummler; Hinnak Northoff; Stefan Laufer; Thorsten J Maier; Olof Rådmark; Bengt Samuelsson; Andreas Koeberle; Lidia Sautebin; Oliver Werz
Journal:  J Clin Invest       Date:  2017-07-24       Impact factor: 14.808

2.  Structural and mechanistic insights into 5-lipoxygenase inhibition by natural products.

Authors:  Nathaniel C Gilbert; Jana Gerstmeier; Erin E Schexnaydre; Friedemann Börner; Ulrike Garscha; David B Neau; Oliver Werz; Marcia E Newcomer
Journal:  Nat Chem Biol       Date:  2020-05-11       Impact factor: 15.040

Review 3.  The role of lipoxygenases in pathophysiology; new insights and future perspectives.

Authors:  Ryuichi Mashima; Torayuki Okuyama
Journal:  Redox Biol       Date:  2015-08-07       Impact factor: 11.799

4.  Pharmacological profile and efficiency in vivo of diflapolin, the first dual inhibitor of 5-lipoxygenase-activating protein and soluble epoxide hydrolase.

Authors:  Ulrike Garscha; Erik Romp; Simona Pace; Antonietta Rossi; Veronika Temml; Daniela Schuster; Stefanie König; Jana Gerstmeier; Stefanie Liening; Markus Werner; Heiner Atze; Sandra Wittmann; Christina Weinigel; Silke Rummler; Gerhard K Scriba; Lidia Sautebin; Oliver Werz
Journal:  Sci Rep       Date:  2017-08-24       Impact factor: 4.379

5.  Discovery of the first dual inhibitor of the 5-lipoxygenase-activating protein and soluble epoxide hydrolase using pharmacophore-based virtual screening.

Authors:  Veronika Temml; Ulrike Garscha; Erik Romp; Gregor Schubert; Jana Gerstmeier; Zsofia Kutil; Barbara Matuszczak; Birgit Waltenberger; Hermann Stuppner; Oliver Werz; Daniela Schuster
Journal:  Sci Rep       Date:  2017-02-20       Impact factor: 4.379

6.  Pharmacokinetics, Pharmacodynamics, and Tolerability of AZD5718, an Oral 5-Lipoxygenase-Activating Protein (FLAP) Inhibitor, in Healthy Japanese Male Subjects.

Authors:  Jane Knöchel; Karin Nelander; Maria Heijer; Eva-Lotte Lindstedt; Gun-Britt Forsberg; Carl Whatling; Hitoshi Shimada; David S Han; Anders Gabrielsen; Pavlo Garkaviy; Hans Ericsson
Journal:  Clin Drug Investig       Date:  2021-09-21       Impact factor: 2.859

7.  Shifting the Biosynthesis of Leukotrienes Toward Specialized Pro-Resolving Mediators by the 5-Lipoxygenase-Activating Protein (FLAP) Antagonist BRP-201.

Authors:  Christian Kretzer; Paul M Jordan; Rossella Bilancia; Antonietta Rossi; Tuğçe Gür Maz; Erden Banoglu; Ulrich S Schubert; Oliver Werz
Journal:  J Inflamm Res       Date:  2022-02-09

8.  Ethoxy acetalated dextran-based nanocarriers accomplish efficient inhibition of leukotriene formation by a novel FLAP antagonist in human leukocytes and blood.

Authors:  Christian Kretzer; Blerina Shkodra; Paul Klemm; Paul M Jordan; Daniel Schröder; Gizem Cinar; Antje Vollrath; Stephanie Schubert; Ivo Nischang; Stephanie Hoeppener; Steffi Stumpf; Erden Banoglu; Frederike Gladigau; Rossella Bilancia; Antonietta Rossi; Christian Eggeling; Ute Neugebauer; Ulrich S Schubert; Oliver Werz
Journal:  Cell Mol Life Sci       Date:  2021-12-31       Impact factor: 9.261

  8 in total

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