Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Stephan A Ohnmacht"'
Autor:
Hugo Brito, Ana Cláudia Martins, João Lavrado, Eduarda Mendes, Ana Paula Francisco, Sofia A Santos, Stephan A Ohnmacht, Nam-Soon Kim, Cecília M P Rodrigues, Rui Moreira, Stephen Neidle, Pedro M Borralho, Alexandra Paulo
Publikováno v:
PLoS ONE, Vol 10, Iss 5, p e0126891 (2015)
A guanine-rich strand within the promoter of the KRAS gene can fold into an intra-molecular G-quadruplex structure (G4), which has an important role in the regulation of KRAS transcription. We have previously identified indolo[3,2-b]quinolines with a
Externí odkaz:
https://doaj.org/article/9348c4e242ba4271be2e6aa2cac4aa40
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-11 (2020)
Scientific Reports
Scientific Reports
Gemcitabine is a drug of choice in the treatment of human pancreatic cancer. Chemo-resistance to this drug is common and has been attributed to a variety of distinct mechanisms, involving > 100 genes. A recently developed small-molecule G-quadruplex
Autor:
Tam Vo, W. David Wilson, Richard Angell, Sally Oxenford, Stephan A. Ohnmacht, Chiara Marchetti, Stephen Neidle
Publikováno v:
ACS Med Chem Lett
[Image: see text] Interactions are reported of three representative naphthalenediimide derivatives with three quadruplex targets, from the promoter region of the telomerase (hTERT) gene, a human telomeric DNA quadruplex, and a telomeric RNA quadruple
Autor:
Alberto Leoni, Stephen Neidle, Stephan A. Ohnmacht, Alessio De Magis, Yee-Peng Tiang, Jussara Amato, Rita Morigi, Antonio Randazzo, Alessandra Locatelli, Mirella Rambaldi, Ettore Novellino, Giovanni Capranico, Alessandra Graziadio, Bruno Pagano, Alessia Pagano
Publikováno v:
Journal of Medicinal Chemistry. 59:5706-5720
G-Quadruplex-binding compounds are currently perceived as possible anticancer therapeutics. Here, starting from a promising lead, a small series of novel hydrazone-based compounds were synthesized and evaluated as G-quadruplex binders. The in vitro G
Autor:
Xia Shao, Stephan A. Ohnmacht, Peter Scott, Franklin I. Aigbirhio, Lei Li, Patrick J. Riss, David J. Williamson, Valentina Ferrari, Tim D. Fryer, Phillip S. Sherman, Carole Quesada, Young T. Hong, Erin L. Cole
Publikováno v:
ACS Medicinal Chemistry Letters. 6:548-552
Quantifying glycogen synthase kinase-3 (GSK-3) activity in vivo using positron emission tomography (PET) imaging is of interest because dysregulation of GSK-3 is implicated in numerous diseases and neurological disorders for which GSK-3 inhibitors ar
Autor:
W. David Wilson, Ingrida Pazitna, Arvind Kumar, Mekala Gunaratnam, David W. Boykin, Mohamed A. Ismail, Ehsan Varavipour, Rupesh Nanjunda, Stephan A. Ohnmacht, Stephen Neidle, Gloria Di Vita
Publikováno v:
Chem. Commun.. 50:960-963
We report here on the discovery and preliminary evaluation of a novel non-macrocyclic low molecular weight quadruplex-stabilizing chemotype. The lead compounds, based on a furan core, show high G-quadruplex stabilisation and selectivity as well as po
Autor:
Stephan A. Ohnmacht, Marialuisa Micco, Aaron G. Dale, Ingrida Pazitna, Mekala Gunaratnam, Anthony P. Reszka, Gavin W. Collie, Stephen Neidle
Publikováno v:
Journal of Medicinal Chemistry. 56:2959-2974
Tetra-substituted naphthalene diimide (ND) derivatives with positively charged termini are potent stabilizers of human telomeric and gene promoter DNA quadruplexes and inhibit the growth of human cancer cells in vitro and in vivo. The present study r
Autor:
Mekala Gunaratnam, Vanessa Petrucci, Anthony P. Reszka, Stephan A. Ohnmacht, Marta Carvalho, Marialuisa Micco, Mire Zloh, Stephen Neidle, Alan K. Todd
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5930-5935
The HSP90 protein is an important target in cancer. We report here that stable quadruplex DNAs can be formed from a promoter sequence in the HSP90 gene, on the basis of melting, circular and NMR studies, and show that these can be selectively targete
Autor:
Rui Moreira, Stephan A. Ohnmacht, Alexandra Paulo, Pedro M. Borralho, Cecília M. P. Rodrigues, Mekala Gunaratnam, Hugo Brito, João Lavrado, Stephen Neidle, Nam-Soon Kim, Sílvia Pisco, Clara Leitão
Publikováno v:
Scientific Reports
KRAS is one of the most frequently mutated oncogenes in human cancer, yet remaining undruggable. To explore a new therapeutic strategy, a library of 5-methyl-indolo[3,2-c]quinoline derivatives (IQc) with a range of alkyldiamine side chains was design
Autor:
Stephan A Ohnmacht, Chiara Marchetti, Mekala Gunaratnam, Rachael J Besser, Shozeb M Haider, Gloria Di Vita, Helen L Lowe, Maria Mellinas-Gomez, Seckou Diocou, Mathew Robson, Jiri Šponer, Barira Islam, R Barbara Pedley, John A Hartley, Stephen Neidle
Publikováno v:
Scientific Reports
We report here that a tetra-substituted naphthalene-diimide derivative (MM41) has significant in vivo anti-tumour activity against the MIA PaCa-2 pancreatic cancer xenograft model. IV administration with a twice-weekly 15 mg/kg dose produces ca 80% t