2026
conference-abstract
OpenAlex
William Tahaney, Yimao Liu, Ahmed Abdullah, Vittoria Massafra et autres
Abstract Using our QuEENTM molecular glue degrader (MGD) discovery engine that integrates biochemical and cellular assays with in silico modeling, we identified and optimized MGDs that induce proteasomal degradation of cyclin E1 (CCNE1) as a therapeutic strategy for CCNE1-amplified cancers. We generated …
us, ch
(code pays fourni par la source)
2026
conference-abstract
OpenAlex
William Tahaney, Yimao Liu, Ahmed Abdullah, Vittoria Massafra et autres
Abstract Using our QuEENTM molecular glue degrader (MGD) discovery engine that integrates biochemical and cellular assays with in silico modeling, we identified and optimized MGDs that induce proteasomal degradation of cyclin E1 (CCNE1) as a therapeutic strategy for CCNE1-amplified cancers. We generated …
us, ch
(code pays fourni par la source)
2023
conference-abstract
OpenAlex
Owen B. Wallace, Gérald Gavory, Mahmoud Ghandi, Anne-Cecile d’Alessandro et autres
Abstract MYC transcription factors have been demonstrated to be drivers of many cancers, yet have remained recalcitrant to new drug development. We hypothesized that MYC-driven cancer cell lines are addicted to protein translation, and therefore are vulnerable to the loss of the …
ch
(code pays fourni par la source)
2023
conference-abstract
OpenAlex
Gérald Gavory, Mahmoud Ghandi, Anne-Cecile d’Alessandro, Débora Bonenfant et autres
Abstract MYC transcription factors are well-established drivers of human cancers but despite being amongst the most frequently altered oncogenes, no approved therapy targeting MYC-driven tumors has been developed to date. MYC-driven cancers are known to be addicted to protein translation. This addiction …
us
(code pays fourni par la source)
2022
conference-abstract
OpenAlex
Gérald Gavory, Mahmoud Ghandi, Anne-Cecile d’Alessandro, Débora Bonenfant et autres
Abstract Myc transcription factors are well-established drivers of human cancers. However, despite being amongst the most frequently mutated, translocated and overexpressed oncogenes, no therapy targeting the Myc family members directly has been developed to date. To sustain uncontrolled cell proliferation and tumor …
ch
(code pays fourni par la source)
Accès ouvert
2020
preprint
OpenAlex
Simone Tortoioli, Astrid Friedli, Alice Prud’homme, Sylvia Richard‐Bildstein et autres
A novel, metal-free process for the challenging synthesis of 2-(3-methyl-1 H -1,2,4-triazol-1-yl) acetic acid ( 1 ) is reported, which features an efficient condensation for the triazole build-up under flow conditions. This continuous, two-step method is atom economical, highly selective and environmentally …
it
(code pays fourni par la source)
Accès ouvert
2020
preprint
OpenAlex
Simone Tortoioli, Astrid Friedli, Alice Prud’homme, Sylvia Richard‐Bildstein et autres
A novel, metal-free process for the challenging synthesis of 2-(3-methyl-1H-1,2,4-triazol-1-yl) acetic acid (1) is reported, which features an efficient condensation for the triazole build-up under flow conditions. This continuous, two-step method is atom economical, highly selective and environmentally benign, due to the …
it
(code pays fourni par la source)
Accès ouvert
2020
article
OpenAlex
Simone Tortoioli, Astrid Friedli, Alice Prud’homme, Sylvia Richard‐Bildstein et autres
A novel, metal-free process for the challenging synthesis of 1,2,4-triazoles is reported, which features an efficient construction of the triazole ring under flow conditions.
ch, us, cn
(code pays fourni par la source)
2018
article
OpenAlex
Sofia Almeida, Roger Martí, Ennio Vanoli, Stefan Abele et autres
A novel and convenient one-pot sequential cascade method for the preparation of 2-trifluoromethylquinazolin-4(3 H )-ones is described. Trifluoroacetic acid (TFA) was employed as inexpensive and readily available CF 3 source, which in the presence of T3P was condensed with a variety of …
ch
(code pays fourni par la source)
2016
article
OpenAlex
Linda Maria Bannwart, Stefan Abele, Simone Tortoioli
Abstract A simple one‐pot reaction of carboxylic acids with N,N‐dialkylformamides yields N,N‐dialkyl carboxamides.
ch
(code pays fourni par la source)
Accès ouvert
2016
article
OpenAlex
Bibia Heidmann, John Gatfield, Catherine Roch, Alexander Treiber et autres
The front cover picture shows the successful application of a scaffold-hopping approach starting from the upper model structure and replacing the central core with different bicyclic diamine templates (some representative templates are depicted above the funnel). The structure–activity relationship optimizations (represented by …
ch
(code pays fourni par la source)
2016
article
OpenAlex
Bibia Heidmann, John Gatfield, Catherine Roch, Alexander Treiber et autres
Starting from suvorexant (trade name Belsomra), we successfully identified interesting templates leading to potent dual orexin receptor antagonists (DORAs) via a scaffold-hopping approach. Structure-activity relationship optimization allowed us not only to improve the antagonistic potency on both orexin 1 and orexin 2 …
ch
(code pays fourni par la source)