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Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof-of-Principle.
Hamed MM, Abdelsamie AS, Rox K, Schütz C, Kany AM, Röhrig T, Schmelz S, Blankenfeldt W, Arce-Rodriguez A, Borrero-de Acuña JM, Jahn D, Rademacher J, Ringshausen FC, Cramer N, Tümmler B, Hirsch AKH, Hartmann RW, Empting M. Hamed MM, et al. Among authors: abdelsamie as. Adv Sci (Weinh). 2023 Feb;10(5):e2204443. doi: 10.1002/advs.202204443. Epub 2023 Jan 3. Adv Sci (Weinh). 2023. PMID: 36596691 Free PMC article.
Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing.
Abdelsamie AS, Herath S, Biskupek Y, Börger C, Siebenbürger L, Salah M, Scheuer C, Marchais-Oberwinkler S, Frotscher M, Pohlemann T, Menger MD, Hartmann RW, Laschke MW, van Koppen CJ. Abdelsamie AS, et al. J Med Chem. 2019 Feb 14;62(3):1362-1372. doi: 10.1021/acs.jmedchem.8b01493. Epub 2019 Jan 15. J Med Chem. 2019. PMID: 30645111
Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17β-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation.
Abdelsamie AS, Salah M, Siebenbürger L, Hamed MM, Börger C, van Koppen CJ, Frotscher M, Hartmann RW. Abdelsamie AS, et al. Eur J Med Chem. 2019 Sep 15;178:93-107. doi: 10.1016/j.ejmech.2019.05.084. Epub 2019 May 31. Eur J Med Chem. 2019. PMID: 31176098
Effects of 17β-HSD2 inhibition in bones on osteoporosis based on an animal rat model.
Müller ST, Pählig S, Merabet A, Abdelsamie AS, van Koppen CJ, Marchais-Oberwinkler S, Hartmann RW, Zierau O, Vollmer G. Müller ST, et al. Among authors: abdelsamie as. J Steroid Biochem Mol Biol. 2019 Sep;192:105405. doi: 10.1016/j.jsbmb.2019.105405. Epub 2019 Jun 8. J Steroid Biochem Mol Biol. 2019. PMID: 31185280
Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.
Abdelsamie AS, Salah M, Siebenbürger L, Merabet A, Scheuer C, Frotscher M, Müller ST, Zierau O, Vollmer G, Menger MD, Laschke MW, van Koppen CJ, Marchais-Oberwinkler S, Hartmann RW. Abdelsamie AS, et al. J Med Chem. 2019 Aug 8;62(15):7289-7301. doi: 10.1021/acs.jmedchem.9b00932. Epub 2019 Jul 25. J Med Chem. 2019. PMID: 31343176
A New PqsR Inverse Agonist Potentiates Tobramycin Efficacy to Eradicate Pseudomonas aeruginosa Biofilms.
Schütz C, Ho DK, Hamed MM, Abdelsamie AS, Röhrig T, Herr C, Kany AM, Rox K, Schmelz S, Siebenbürger L, Wirth M, Börger C, Yahiaoui S, Bals R, Scrima A, Blankenfeldt W, Horstmann JC, Christmann R, Murgia X, Koch M, Berwanger A, Loretz B, Hirsch AKH, Hartmann RW, Lehr CM, Empting M. Schütz C, et al. Among authors: abdelsamie as. Adv Sci (Weinh). 2021 Jun;8(12):e2004369. doi: 10.1002/advs.202004369. Epub 2021 Mar 18. Adv Sci (Weinh). 2021. PMID: 34165899 Free PMC article.
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