Synthetic Routes to N-9 Alkylated 8-Oxoguanines; Weak Inhibitors of the Human DNA Glycosylase OGG1
Molecules, 2015 The human 8-oxoguanine DNA glycosylase OGG1 is involved in base excision repair (BER), one of several DNA repair mechanisms that may counteract the effects of chemo- and radiation therapy for the treatment of cancer. We envisage that potent inhibitors of
Tushar R. Mahajan +4 more
doaj +1 more source
Pharmaceuticals, 2020 The phytochemical profile of the methanolic extracts (pulp and peel) obtained from two dehydration methods (drying and freeze-lyophilization) of the traditional Italian apple Mela Rosa dei Monti Sibillini, as well as their inhibitory properties against ...
Víctor López +6 more
doaj +1 more source
Identifying Novel Inhibitors of RpFabG in Typhus-inducing Rickettsia prowazekii [PDF]
, 2019 Epidemic typhus is a rickettsial disease that is contracted via ticks and lice found on the flying squirrel. The disease is caused by Rickettsia prowazekii, an intracellular, gram-negative coccobacillus.
Panatpur, Aparna
core +1 more source
Social context prevents heat hormetic effects against mutagens during fish development
FEBS Letters, EarlyView.This study shows that sublethal heat stress protects fish embryos against ultraviolet radiation, a concept known as ‘hormesis’. However, chemical stress transmission between fish embryos negates this protective effect. By providing evidence for the mechanistic molecular basis of heat stress hormesis and interindividual stress communication, this study ...
Lauric Feugere +5 more
wiley +1 more source
Immobilized enzyme reactors in HPLC and its application in inhibitor screening: A review
Journal of Pharmaceutical Analysis, 2012 This paper sets out to summarize the literatures based on immobilized enzyme bio-chromatography and its application in inhibitors screening in the last decade.
Si-Meng Fang +3 more
doaj
Docking Studies on HIV Integrase Inhibitors Based On Potential Ligand Binding Sites [PDF]
International Journal on Bioinformatics & Biosciences, vol. 2, pp.
21-29, 2012, 2012 HIV integrase is a 32 kDa protein produced from the C-terminal portion of the Pol gene product, and is an attractive target for new anti-HIV drugs. Integrase is an enzyme produced by a retrovirus (such as HIV) that enables its genetic material to be integrated into the DNA of the infected cell.
arxiv +1 more source
Genome-scale architecture of small molecule regulatory networks and the fundamental trade-off between regulation and enzymatic activity [PDF]
, 2017 Metabolic flux is in part regulated by endogenous small molecules that modulate the catalytic activity of an enzyme, e.g., allosteric inhibition. In contrast to transcriptional regulation of enzymes, technical limitations have hindered the production of ...
Briars, Emma +6 more
core +2 more sources
miRNA‐29 regulates epidermal and mesenchymal functions in skin repair
FEBS Letters, EarlyView.miRNA‐29 inhibits cell‐to‐cell and cell‐to‐matrix adhesion by silencing mRNA targets. Adhesion is controlled by complex interactions between many types of molecules coded by mRNAs. This is crucial for keeping together the layers of the skin and for regenerating the skin after wounding.
Lalitha Thiagarajan +10 more
wiley +1 more source
Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 Inhibitors
Molecules, 2018 We recently found that a cyclohexanecarboxamide derived from 4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-ene displayed low nanomolar inhibition of 11β-HSD1.
Rosana Leiva +4 more
doaj +1 more source
Predicting inhibitors for SARS-CoV-2 RNA-dependent RNA polymerase using machine learning and virtual screening [PDF]
arXiv, 2020 Global coronavirus disease pandemic (COVID-19) caused by newly identified SARS- CoV-2 coronavirus continues to claim the lives of thousands of people worldwide. The unavailability of specific medications to treat COVID-19 has led to drug repositioning efforts using various approaches, including computational analyses.
arxiv