Person: AKDEMİR, ATİLLA
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Publication Metadata only Abietane diterpenoids as butyrylcholinesterase inhibitors from Salvia species(2012-08-01) Topcu, GÜLAÇTI; Akdemir, ATİLLA; Öztürk, Mahmut Serdar; Boğa, Miray; Kola, U.; TOPÇU, GÜLAÇTI; AKDEMİR, ATİLLAPublication Metadata only Molecular modelling studies to understand the effects of bioactive compounds on DNA and gene expression(2015-11-24) AKDEMİR, ATİLLA; AKDEMİR, ATİLLAPublication Metadata only Molecular docking and in vitro bioactivity of 5-fluoroindole derivatives on ER, aromatase and CYP1B1 activity in breast cancer cells(2019-10-15T00:00:00Z) Ince, E.; Fatullayev, H.; AKDEMİR, ATİLLA; Suzen, S.; Gurer-Orhan, H.; AKDEMİR, ATİLLAPublication Metadata only Molecular modeling studies on dithiocarbamates and dithiocarbonates containing 6-nitrosaccharin scaffold as antitubercular agents(2022-03-12T00:00:00Z) Dingiş Birgül, Serap İpek; Trawally, Muhammed; Demir Yazıcı, Kübra; Akdemir, Atilla; Güzel Akdemir, Özlen; DİNGİŞ BİRGÜL, SERAP İPEK; AKDEMİR, ATİLLAPublication Metadata only Nükleer Faktör Kappa-B İnhibisyon Etkili Ursan Türevi Triterpenlerin Sentezi(2017-04-02) TUNCAY, SALİH; SEÇEN, HASAN; ÖCAL, NÜKET; TOPÇU, GÜLAÇTI; AKDEMİR, ATİLLA; ŞENOL, HALİL; ŞENOL, HALIL; AKDEMİR, ATİLLA; TOPÇU, GÜLAÇTIPublication Metadata only The application of molecular modelling studies to understand the selectivity and potency of several novel carbonic anhydrase inhibitors(2019-11-14T00:00:00Z) Akdemir, Atilla; AKDEMİR, ATİLLAThe application of molecular modelling studies to understand the selectivity and potency of several novel carbonic anhydrase inhibitorsAtilla AkdemirComputer-Aided Drug Discovery Laboratory, Department of Pharmacology, Faculty of Pharmacy, Bezmialem Vakif University, 34093 Istanbul, Turkeyaakdemir@bezmialem.edu.trCAs are metalloenzymes that catalyse the reversible hydration of carbon dioxide to bicarbonate. Eventhough this is a simple reaction, it influences physiological pH values and provides bicarbonate for bioreactions or maintaining the ion balance.[1,2] Many isoforms exist with different tissue distribution and reaction kinetics and thus CA isoforms are involved in different physiological processes. For example, hCA IX and XII are overexpressed in hypoxic tumour cells and are involved in the survival of those cells. CAs from pathogenic microorganisms are involved in virulence. As such, selective inhibitors of specific target CAs may be drug candidates for antimicrobial or anticancer chemotherapy agents.In both previous and ongoing studies, we synthesized structurally novel sulfonamides and tested them against carbonic anhydrase (CA) isozymes that are considered drug targets for anticancer chemotherapeutics or antimicrobial agents.[3] Several inhibitors have been obtained that selectively and potently inhibit tumour-associated hCA IX/XII or pathenic CAs, while they only show poor inhibition of the widespread off-targets hCA I/II. Molecular modelling studies have been performed to understand the reasons behind the selectivity and potency of these compounds. These results will direct our synthesis efforts in obtaining inhibitors with higher selectivity and potency.References [1] Supuran, C.T.; Scozzafava, A. Carbonic anhydrases as targets for medicinal chemistry. Bioorganic and Medicinal Chemistry 2007, 13, 4336-4350 [2] Supuran, C.T. Carbonic anhydrases: novel therapeutic applications for inhibitors and activators. Nature Reviews Drug Discovery 2008, 2, 168-181 [3] Demir-Yazıcı, K.; Bua, S.; Akgüneş, N.M.; Akdemir, A.; Supuran, C.T. and Güzel-Akdemir, Ö. Indole-based hydrazones containing a sulfonamide moiety as selective inhibitors of tumor-associated human carbonic anhydrase isoforms IX and XII. Internationl Journal of Molecular Science 2019, 20(9), 2354Publication Metadata only The Search for Novel 3-hydroxyflavones with Anticholinergic Activity.(2015-06-16) Öztürk, Turan; Akdemir, ATİLLA; TOPÇU, GÜLAÇTI; BÜTÜN, BURCU; AKDEMİR, ATİLLA; TOPÇU, GÜLAÇTIPublication Metadata only Design, synthesis and investigation of dual benefits of 2-methyl indole derivatives in hormone-dependent breast cancer: Aromatase inhibitory and antioxidant activity(2016-09-07) Ozcan Sezer, S; İnci, E; Öztürk Ceylan, O; AKDEMİR, ATİLLA; Suzen, S; Gurer Orhan, H; AKDEMİR, ATİLLAPublication Metadata only Computer Aided Design and Synthesis of New Ursane Triterpenoids with Nuclear Factor Kappa B Inhibition Effect(2019-12-19) Şenol, Halil; Akdemir, Atilla; Topçu, Gülaçtı; ŞENOL, HALIL; AKDEMİR, ATİLLA; TOPÇU, GÜLAÇTIPublication Metadata only Potent inhibitors of mitochondrial carbonic anhydrase isozymes CA-VA and CA-VB and brain-associated CA-VII(2012-04-15) AKDEMİR, ATİLLA; Güzel, Özlen; Supuran, CT; AKDEMİR, ATİLLA