Wyniki wyszukiwania dla: inhibitors
-
In silico design of telomerase inhibitors.
PublikacjaTelomerase is a reverse transcriptase enzyme involved in DNA synthesis at the end of linear chromosomes. Unlike in most other cells, telomerase is reactivated most cancerous cells and, therefore, has become a promising new anticancer target. Despite extensive research, direct telomerase inhibitors have yet not been introduced to the clinics because of the complexity of this enzyme. Structures of this protein from simple organisms...
-
Neuroprotective Effect of SGLT2 Inhibitors
Publikacja -
Proteinase 3 phosphonic inhibitors
Publikacja -
Clays as Inhibitors of Polyurethane Foams’ Flammability
PublikacjaPolyurethanes are a very important group of polymers with an extensive range of applications in different branches of industry. In the form of foams, they are mainly used in bedding, furniture, building, construction, and automotive sectors. Due to human safety reasons, these applications require an appropriate level of flame retardance, often required by various law regulations. Nevertheless, without the proper modifications,...
-
COMPUTER-AIDED DESIGN OF ORGANOPHOSPHORUS INHIBITORS OF UREASE
PublikacjaBased on the structure of the most potential inhibitor diamidophosphate, various novel groups of inhibitors were developed by knowledge-based design approach with covalent carbon-phosphorus or carbon-phosphorus-carbon bond to improve hydrolytic stability to inhibit the microbial ureases. Designed compounds were evaluated with 10 (LigScore1, LigScore2, PLP1, PLP2, JAIN, PMF, PMF04, LUDI_1, LUDI_2 and LUDI_3) different scoring functions...
-
Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors
PublikacjaThe aim of this work is review of tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant,...
-
HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublikacjaHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
-
Inhibitors of amino acids biosynthesis as antifungal agents
PublikacjaFungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit...
-
New potent cathepsin G phosphonate inhibitors
Publikacja -
ACEI and ARB — Each Unique RAAS Inhibitors
Publikacja -
Catalytic topoisomerase II inhibitors in cancer therapy.
PublikacjaDNA topoizomeraza II jest jednym z głównych celów molekularnych dla leków stosowanych w terapii przeciwnowotworowej. Wszystkie inhibitory tego enzymu są zdolne do zakłócania w jeden z etapów cyklu katalitycznego topoizomerazy II. Związki, które stabilizują kowalencyjny kompleks DNa i topoizomerazy II (znany jako kompleks rozszczepialny) są nazywane truciznami topoizomerazy, inne związki, które hamują aktywność enzymu na innych...
-
Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublikacjaIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
-
Inhibitors of angiogenesis in cancer therapy – synthesis and biological activity
PublikacjaAngiogenesis is the process of formation of new capillaries from preexisting blood vessels. Angiogenesis is involved in normal physiological processes, and plays an important role in tumor invasion and development of metastases. Vascular endothelial growth factor (VEGF) plays a key role in angiogenesis. VEGF is a mitogen for vascular endothelial cells and stimulates their proliferation. By inhibiting the biological activity of...
-
Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublikacjaBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
-
Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
Publikacja -
Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
-
Synthesis of anthraquinone-tuftsin analogues as potential topoisomerase inhibitors
PublikacjaZaprezentowano syntezę nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny oraz wstępne badania biologiczne (aktywność cytotoksyczną na wybranych liniach nowotworowych oraz zdolność hamowania topoizomerazy I).
-
CDK9 inhibitors in multiple myeloma: a review of progress and perspectives
Publikacja -
An Overview of Several Inhibitors for Alzheimer’s Disease: Characterization and Failure
Publikacja -
Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G
Publikacja