Search Results - "Abdelsamie, Ahmed"

Inhibitors of 17β-hydroxysteroid dehydrogenase type 1, 2 and 14: Structures, biological activities and future challenges by Salah, Mohamed, Abdelsamie, Ahmed S., Frotscher, Martin

“…During the past 25 years, the modulation of estrogen action by inhibition of 17β-hydroxysteroid dehydrogenase types 1 and 2 (17β-HSD1 and 17β-HSD2),…”
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First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases by Salah, Mohamed, Abdelsamie, Ahmed S, Frotscher, Martin

“…STS and 17β-HSD1 are attractive targets for the treatment of estrogen-dependent diseases like endometriosis and breast cancer. The simultaneous inhibition of…”
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Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis by Mohamed, Abdelrahman, Salah, Mohamed, Tahoun, Mariam, Hawner, Manuel, Abdelsamie, Ahmed S., Frotscher, Martin

“…A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1­(17β HSD1) by a single drug was explored,…”
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Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for In Vivo Proof-of-Principle Studies in an Endometriosis Mouse Model by Salah, Mohamed, Tahoun, Mariam, Rudzitis-Auth, Jeannette, Stotz, Lisa, van Koppen, Chris J., Laschke, Matthias W., Abdelsamie, Ahmed S., Frotscher, Martin

“…Treating estrogen-dependent diseases like endometriosis with drugs suppressing local estrogen activation may be superior to existing endocrine therapies…”
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Recurring ST-Elevation Myocardial Infarction With No-Reflow Caused by Hypercoagulable State: A Behcet Disease Case Report by Hegazi Abdelsamie, Ahmed, Al-Asiri, Nayef

“…Acute myocardial infarction (AMI) in young patients is an important issue because of its impact on health and social life. The mechanisms and disease courses…”
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Design, synthesis and molecular docking study of novel quinoxalin-2(1H)-ones as anti-tumor active agents with inhibition of tyrosine kinase receptor and studying their cyclooxygenase-2 activity by Galal, Shadia A., Khairat, Sarah H.M., Ragab, Fatma A.F., Abdelsamie, Ahmed S., Ali, Mamdouh M., Soliman, Salwa M., Mortier, Jérémie, Wolber, Gerhard, El Diwani, Hoda I.

“…On continuation to our work, new quinoxalin-2(1H)-ones were synthesized to study their cytotoxic effect against HepG-2 and MCF-7 with their effect on the human…”
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Divergent synthesis and biological evaluation of 2-(trifluoromethyl)pyridines as virulence-attenuating inverse agonists targeting PqsR by Schütz, Christian, Hodzic, Amir, Hamed, Mostafa, Abdelsamie, Ahmed S., Kany, Andreas M., Bauer, Maximilian, Röhrig, Teresa, Schmelz, Stefan, Scrima, Andrea, Blankenfeldt, Wulf, Empting, Martin

“…A short and divergent route towards new derivatives of 2-(trifluoromethyl)pyridines as potent inverse agonists of the bacterial target PqsR against Pseudomonas…”
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Discovery and optimization of thiazole-based quorum sensing inhibitors as potent blockers of Pseudomonas aeruginosa pathogenicity by Abdelsamie, Ahmed S., Hamed, Mostafa M., Schütz, Christian, Röhrig, Teresa, Kany, Andreas M., Schmelz, Stefan, Blankenfeldt, Wulf, Hirsch, Anna K.H., Hartmann, Rolf W., Empting, Martin

“…Pseudomonas aeruginosa causes life-threatening infections especially in hospitalized patients and shows an increasing resistance to established antibiotics. A…”
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Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases by Alhayek, Alaa, Abdelsamie, Ahmed S., Schönauer, Esther, Camberlein, Virgyl, Hutterer, Evelyn, Posselt, Gernot, Serwanja, Jamil, Blöchl, Constantin, Huber, Christian G., Haupenthal, Jörg, Brandstetter, Hans, Wessler, Silja, Hirsch, Anna K. H.

“…In view of the worldwide antimicrobial resistance (AMR) threat, new bacterial targets and anti-infective agents are needed. Since important roles in bacterial…”
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New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies by Abdel-Mohsen, Heba T, El Kerdawy, Ahmed M, Omar, Mohamed A, Berrino, Emanuela, Abdelsamie, Ahmed S, El Diwani, Hoda I, Supuran, Claudiu T

“…In the present work, a new series of thiopyrimidine-benzenesulfonamide conjugates was designed, synthesized and tested as carbonic anhydrase (CA, EC 4.2.1.1)…”
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Developing an Electronic Handover System for On-Call Doctors in a South London Mental Health Trust by Abdelsamie, Ahmed, Alexander, Laith, Wilkinson, Rebecca, Dawson, Olivia, Yadav, Prateek

“…Aims To replace pre-existing paper-based and informal handover systems with a confidential electronic handover system for on-call doctors across a large South…”
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Influence of metabolic tumor burden on reference tissues’ standardized uptake values in 18F-FDG PET/CT sequential imaging by Badawy, Ahmed, Maamoun, Marwa Mohamed, Kandeel, Ahmed Abdelsamie, Anwar, Hoda

“…BackgroundExtremely hypermetabolic neoplastic tissues have been hypothesized to act as a “sink” reducing the amount of radiopharmaceutical available for uptake…”
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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 by Abdelsamie, Ahmed S., Salah, Mohamed, Siebenbürger, Lorenz, Hamed, Mostafa M., Börger, Carsten, van Koppen, Chris J., Frotscher, Martin, Hartmann, Rolf W.

“…Estrogens are the major female sex steroid hormones, estradiol (E2) being the most potent form in humans. Disturbing the balance between E2 and its weakly…”
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Part I: Design, synthesis and biological evaluation of novel pyrazole-benzimidazole conjugates as checkpoint kinase 2 (Chk2) inhibitors with studying their activities alone and in combination with genotoxic drugs by Galal, Shadia A., Abdelsamie, Ahmed S., Shouman, Samia A., Attia, Yasmin M., Ali, Hamed I., Tabll, Ashraf, El-Shenawy, Reem, El Abd, Yasmine S., Ali, Mamdouh M., Mahmoud, Abeer E., Abdel-Halim, Abeer H., Fyiad, Amal A., Girgis, Adel S., El-Diwani, Hoda I.

“…Activated checkpoint kinase 2 (Chk2) is a tumor suppressor as one of the main enzymes that affect the cell cycle. 2-Biarylbenzimidazoles are potent selective…”
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First Structure–Activity Relationship of 17β-Hydroxysteroid Dehydrogenase Type 14 Nonsteroidal Inhibitors and Crystal Structures in Complex with the Enzyme by Braun, Florian, Bertoletti, Nicole, Möller, Gabriele, Adamski, Jerzy, Steinmetzer, Torsten, Salah, Mohamed, Abdelsamie, Ahmed S, van Koppen, Chris J, Heine, Andreas, Klebe, Gerhard, Marchais-Oberwinkler, Sandrine

“…17β-HSD14 belongs to the SDR family and oxidizes the hydroxyl group at position 17 of estradiol and 5-androstenediol using NAD+ as cofactor. The goal of this…”
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Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis by Abdelsamie, Ahmed S, Salah, Mohamed, Siebenbürger, Lorenz, Merabet, Ahmed, Scheuer, Claudia, Frotscher, Martin, Müller, Sebastian T, Zierau, Oliver, Vollmer, Günter, Menger, Michael D, Laschke, Matthias W, van Koppen, Chris J, Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W

“…Osteoporosis is predominantly treated with drugs that inhibit further bone resorption due to estrogen deficiency. Yet, osteoporosis drugs that not only inhibit…”
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Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy by Siebenbuerger, Lorenz, Hernandez-Olmos, Victor, Abdelsamie, Ahmed S, Frotscher, Martin, van Koppen, Chris J, Marchais-Oberwinkler, Sandrine, Scheuer, Claudia, Laschke, Matthias W, Menger, Michael D, Boerger, Carsten, Hartmann, Rolf W

“…Intracellular elevation of E2 levels in bone by inhibition of 17β hydroxysteroid dehydrogenase type 2 (17β-HSD2) without affecting systemic E2 levels is an…”
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Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study by Abdelsamie, Ahmed S., van Koppen, Chris J., Bey, Emmanuel, Salah, Mohamed, Börger, Carsten, Siebenbürger, Lorenz, Laschke, Matthias W., Menger, Michael D., Frotscher, Martin

“…Current endocrine therapeutics for the estrogen-dependent disease endometriosis often lead to considerable side-effects as they act by reducing estrogen action…”
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Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing by Abdelsamie, Ahmed S, Herath, Steven, Biskupek, Yannik, Börger, Carsten, Siebenbürger, Lorenz, Salah, Mohamed, Scheuer, Claudia, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Pohlemann, Tim, Menger, Michael D, Hartmann, Rolf W, Laschke, Matthias W, van Koppen, Chris J

“…Current therapies of steroid hormone-dependent diseases predominantly alter steroid hormone concentrations (or their actions) in plasma, in target and…”
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Effects of 17β-HSD2 inhibition in bones on osteoporosis based on an animal rat model by Müller, Sebastian T., Pählig, Sophie, Merabet, Ahmed, Abdelsamie, Ahmed S., van Koppen, Chris J., Marchais-Oberwinkler, Sandrine, Hartmann, Rolf W., Zierau, Oliver, Vollmer, Günter

“…[Display omitted] •Testing 17β-HSD2 as target for prevention of ovariectomy-induced bone loss in rats.•First time proof-of-principle using 17β-HSD2 inhibitor…”
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