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Exploration of the binding pocket of histone deacetylases: the design of potent and isoform-selective inhibitors
(Tübitak, 2017)
Histone deacetylases (HDACs) are enzymes that act on histone proteins to remove the acetyl group and thereby regulate the
chromatin state. HDACs act not only on histone protein but also nonhistone proteins that are key ...
Synthesis, Anticancer Activity on Prostate Cancer Cell Lines and Molecular Modeling Studies of Flurbiprofen-Thioether Derivatives as Potential Target of MetAP (Type II)
(Bentham Science PUBL LTD, 2020)
Background: Prostate cancer is still one of the serious causes of mortality and morbidity in men. Despite recent advances in anticancer therapy, there is a still need of novel agents with more efficacy and specificity in ...
Drug Design for CNS Diseases: Polypharmacological Profiling of Compounds Using Cheminformatic, 3D-QSAR and Virtual Screening Methodologies
(Frontiers Media Sa, 2016)
The diverse cerebral mechanisms implicated in Central Nervous System (CNS) diseases together with the heterogeneous and overlapping nature of phenotypes indicated that multitarget strategies may be appropriate for the ...
Pharmacophore-based virtual screening for identification of potential selective inhibitors of human histone deacetylase 6
(Elsevier Sci Ltd, 2018)
Histone deacetylase (HDAC) 6 plays a role in oncogenic transformation and cancer metastasis via tubulin deacetylation, making it a critical target for anticancer drug design. However, lack of selectivity shown by many of ...
Potent inhibitors designed for methionine aminopeptidase II using pharmocophore modeling /
(Kadir Has Üniversitesi, 2019)
Metaloenzimlerden Metiyonin Aminopeptidazlar (MetAP2), yeni sentezlenmiş polipep-titlerin başından metionin amino asidini kesmekle sorumludur. MetAP2'nin seçimli olarak engellenmesi damar oluşumunu baskıladığını, katı ...
Discovery of novel isoform-selective histone deacetylases 5 and 9 inhibitors through combined ligand-based pharmacophore modeling, molecular mocking, and molecular dynamics simulations for cancer treatment
(Elsevier, 2021-07)
Class IIa histone deacetylases (HDACs) 5 and 9 play crucial roles in several human disorders such as cancer, making them important targets for drug design. Continuous research is pursed to overcome the cytotoxicity side ...
"2-pirazolin yapısındaki yeni bir bileşiğin sentezi, moleküler modellemesi ve monoaminoksidaz inhibitörü etkisinin araştırılması"
(Türkiye Halk Sağlığı Kurumu, 2018)
Amaç: Nöromediatörlerin yıkımından sorumlu olan
monoamin oksidaz (MAO) enziminin izoformlarının
(MAO-A ve -B) birçok hastalık ile yakından ilişkili olduğu;
MAO inhibitörlerinin depresyon, Parkinson ve Alzheimer
hastalığı ...
Design, Synthesis and hMAO Inhibitory Screening of Novel 2-Pyrazoline Analogues
(Bentham Science Publ Ltd, 2017)
Aim and Objective: MAO inhibitors have a significant effect on the nervous system since they act in regulation of neurotransmitter concentrations. Neurotransmitter levels are critical for a healthy nervous system. MAO ...
Potential inhibitors of methionine aminopeptidase type II identified via structure-based pharmacophore modeling
(Springer Science and Business Media Deutschland GmbH, 2021)
Methionine aminopeptidase (MetAP2) is a metal-containing enzyme that removes initiator methionine from the N-terminus of a newly synthesized protein. Inhibition of the enzyme is crucial in diminishing cancer growth and ...
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors
(AMER CHEMICAL SOC, 2021-02)
Thirty compounds having 1-[2-(5-substituted-2-benzoxazolinone-3-yl) acetyl]-3,5-disubstitutedphenyl-2-pyrazoline structure and nine compounds having N'-(1,3-disubstitutedphenylallylidene)-2-(5-substituted- 2-benzoxazolin ...