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Expert Opinion on Drug Discovery Volume 8, 2013 - Issue 1
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Overview of recent drug discovery approaches for new generation leukotriene A4 hydrolase inhibitors

Burcu ÇalışkanGazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Taç Sok. No:3 Yenimahalle, 06330 Ankara, Turkey
&
Erden BanogluGazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Taç Sok. No:3 Yenimahalle, 06330 Ankara, Turkey+90 312 2023236; +90 312 2235018; [email protected]; [email protected]
(Professor)
Pages 49-63 | Published online: 25 Oct 2012

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Fares Fenanir, Abderrahmane Semmeq, Yacine Benguerba, Michael Badawi, Marie-Antoinette Dziurla, Smain Amira & Hocine Laouer. (2022) In silico investigations of some Cyperus rotundus compounds as potential anti-inflammatory inhibitors of 5-LO and LTA4H enzymes. Journal of Biomolecular Structure and Dynamics 40:22, pages 11571-11586.
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Till A Röhn, Shin Numao, Heike Otto, Christian Loesche & Gebhard Thoma. (2021) Drug discovery strategies for novel leukotriene A4 hydrolase inhibitors. Expert Opinion on Drug Discovery 16:12, pages 1483-1495.
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Oliver Werz, Jana Gerstmeier & Ulrike Garscha. (2017) Novel leukotriene biosynthesis inhibitors (2012-2016) as anti-inflammatory agents. Expert Opinion on Therapeutic Patents 27:5, pages 607-620.
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Articles from other publishers (25)

Gebhard Thoma, Christian Markert, Rainer Lueoend, Wolfgang Miltz, Carsten Spanka, Birgit Bollbuck, Romain M. Wolf, Honnappa Srinivas, Carlos A. Penno, Michael Kiffe, Monika Gajewska, Dallas Bednarczyk, Grazyna Wieczorek, Amanda Evans, Christian Beerli & Till A. Röhn. (2023) Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase. Journal of Medicinal Chemistry.
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Zong-wei Wang, Chang Liu, Ai-hua Zhang, Guang-li Yan, Hui Sun, Ying Han, Wei-tong Ma & Xi-jun Wang. (2022) Discovery of Q-markers of Wenxin Formula based on a Chinmedomics strategy. Journal of Ethnopharmacology 298, pages 115576.
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Tuğba Gürses, Abdurrahman Olğaç, Ulrike Garscha, Tuğçe Gür Maz, Nur Banu Bal, Orhan Uludağ, Burcu Çalışkan, Ulrich S. Schubert, Oliver Werz & Erden Banoglu. (2021) Simple heteroaryl modifications in the 4,5-diarylisoxazol-3-carboxylic acid scaffold favorably modulates the activity as dual mPGES-1/5-LO inhibitors with in vivo efficacy. Bioorganic Chemistry 112, pages 104861.
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Christian Markert, Gebhard Thoma, Honnappa Srinivas, Birgit Bollbuck, Rainer M. Lüönd, Wolfgang Miltz, Rudolf Wälchli, Romain Wolf, Jürgen Hinrichs, Christian Bergsdorf, Kamal Azzaoui, Carlos A. Penno, Kai Klein, Nathalie Wack, Petra Jäger, Franziska Hasler, Christian Beerli, Pius Loetscher, Janet Dawson, Grazyna Wieczorek, Shin Numao, Amanda Littlewood-Evans & Till A. Röhn. (2021) Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A 4 Hydrolase . Journal of Medicinal Chemistry 64:4, pages 1889-1903.
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Tao Chen, Hao Xiong, Jing-Fang Yang, Xiao-Lei Zhu, Ren-Yu Qu & Guang-Fu Yang. (2020) Diaryl Ether: A Privileged Scaffold for Drug and Agrochemical Discovery. Journal of Agricultural and Food Chemistry 68:37, pages 9839-9877.
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Suaad A. Audat, Nizar A. Al-Shar’i, Buthina A. Al-Oudat, Amanda Bryant-Friedrich, Mel F. Bedi, Aref L. Zayed & Qosay A. Al-Balas. (2020) Identification of Human Leukotriene A4 Hydrolase Inhibitors Using Structure-Based Pharmacophore Modeling and Molecular Docking. Molecules 25:12, pages 2871.
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Johannes Morstein, Mahendra Awale, Jean-Louis Reymond & Dirk Trauner. (2019) Mapping the Azolog Space Enables the Optical Control of New Biological Targets. ACS Central Science 5:4, pages 607-618.
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Stefanie König, Simona Pace, Helmut Pein, Thorsten Heinekamp, Jan Kramer, Erik Romp, Maria Straßburger, Fabiana Troisi, Anna Proschak, Jan Dworschak, Kirstin Scherlach, Antonietta Rossi, Lidia Sautebin, Jesper Z. Haeggström, Christian Hertweck, Axel A. Brakhage, Jana Gerstmeier, Ewgenij Proschak & Oliver Werz. (2019) Gliotoxin from Aspergillus fumigatus Abrogates Leukotriene B4 Formation through Inhibition of Leukotriene A4 Hydrolase. Cell Chemical Biology 26:4, pages 524-534.e5.
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Andreas Koeberle & Oliver Werz. (2018) Natural products as inhibitors of prostaglandin E2 and pro-inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis. Biotechnology Advances 36:6, pages 1709-1723.
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Xia Mu & Dingguo Xu. (2018) QM/MM Molecular Dynamics Investigations of the Substrate Binding of Leucotriene A4 Hydrolase: Implication for the Catalytic Mechanism. The Journal of Physical Chemistry B 122:29, pages 7253-7263.
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Zehra Tuğçe Gür, Burcu Çalışkan & Erden Banoglu. (2018) Drug discovery approaches targeting 5-lipoxygenase-activating protein (FLAP) for inhibition of cellular leukotriene biosynthesis. European Journal of Medicinal Chemistry 153, pages 34-48.
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Shin Numao, Franziska Hasler, Claire Laguerre, Honnappa Srinivas, Nathalie Wack, Petra Jäger, Andres Schmid, Arnaud Osmont, Patrik Röthlisberger, Jeremy Houguenade, Christian Bergsdorf, Janet Dawson, Nathalie Carte, Andreas Hofmann, Christian Markert, Liz Hardaker, Andreas Billich, Romain M. Wolf, Carlos A. Penno, Birgit Bollbuck, Wolfgang Miltz & Till A. Röhn. (2017) Feasibility and physiological relevance of designing highly potent aminopeptidase-sparing leukotriene A4 hydrolase inhibitors. Scientific Reports 7:1.
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L. Bhatt, K. Roinestad, T. Van & E.B. Springman. (2017) Recent advances in clinical development of leukotriene B4 pathway drugs. Seminars in Immunology 33, pages 65-73.
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Fan Zhang, Dang Wu, Gao-Lei Wang, Shuang Hou, Ping Ou-Yang, Jin Huang & Xiao-Yong Xu. (2017) Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A 4 hydrolase aminopeptidase inhibitors. Chinese Chemical Letters 28:5, pages 1044-1048.
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Caroline M. Low, Samia Akthar, Dhiren F. Patel, Stephan Löser, Chi-Tung Wong, Patricia L. Jackson, J. Edwin Blalock, Stephen A. Hare, Clare M. Lloyd & Robert J. Snelgrove. (2017) The development of novel LTA4H modulators to selectively target LTB4 generation. Scientific Reports 7:1.
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Karoline Gangestad Primdahl, Jørn Eivind Tungen, Patricia Regina Soares De Souza, Romain Alexandre Colas, Jesmond Dalli, Trond Vidar Hansen & Anders Vik. (2017) Stereocontrolled synthesis and investigation of the biosynthetic transformations of 16(S),17(S)-epoxy-PD n-3 DPA . Org. Biomol. Chem. 15:40, pages 8606-8613.
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Robert B. Zurier. 2017. Kelley and Firestein's Textbook of Rheumatology. Kelley and Firestein's Textbook of Rheumatology 366 383.e3 .
Serkan Levent, Jana Gerstmeier, Abdurrahman Olgaç, Felix Nikels, Ulrike Garscha, Andrea Carotti, Antonio Macchiarulo, Oliver Werz, Erden Banoglu & Burcu Çalışkan. (2016) Synthesis and biological evaluation of C(5)-substituted derivatives of leukotriene biosynthesis inhibitor BRP-7. European Journal of Medicinal Chemistry 122, pages 510-519.
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Amit Gaggar & Nathaniel Weathington. (2016) Bioactive extracellular matrix fragments in lung health and disease. Journal of Clinical Investigation 126:9, pages 3176-3184.
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Norbert Furtmann, Ye Hu, Michael Gütschow & Jürgen Bajorath. (2015) Identification of Interaction Hot Spots in Structures of Drug Targets on the Basis of Three-Dimensional Activity Cliff Information. Chemical Biology & Drug Design 86:6, pages 1458-1465.
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Paula B. Paz, Esteban G. Vega-Hissi, Matias F. Andrada, Mario R. Estrada & Juan C. Garro Martinez. (2014) Quantitative structure activity relationship and binding investigation of N-alkyl glycine amides as inhibitors of Leukotriene A4 hydrolase. Medicinal Chemistry Research 24:2, pages 496-504.
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Olivier Corminboeuf & Xavier Leroy. (2014) FPR2/ALXR Agonists and the Resolution of Inflammation. Journal of Medicinal Chemistry 58:2, pages 537-559.
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Ingo Muegge & Qiang Zhang. (2015) 3D virtual screening of large combinatorial spaces. Methods 71, pages 14-20.
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Tohru Kambe, Bruno E. Correia, Micah J. Niphakis & Benjamin F. Cravatt. (2014) Mapping the Protein Interaction Landscape for Fully Functionalized Small-Molecule Probes in Human Cells. Journal of the American Chemical Society 136:30, pages 10777-10782.
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Anna Byzia, Jesper Z. Haeggström, Guy S. Salvesen & Marcin Drag. (2014) A remarkable activity of human leukotriene A4 hydrolase (LTA4H) toward unnatural amino acids. Amino Acids 46:5, pages 1313-1320.
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