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Re: KMBJN post# 183369

Friday, 05/26/2017 11:28:52 AM

Friday, May 26, 2017 11:28:52 AM

Post# of 402685
Glad to see u back too KMBJN - your analyses many pay grades above mine :) Is very interesting to read about these p53 combo-type approaches. Targeting the once-considered "undruggable"... seems we're getting closer and closer.

http://tatcongress.org/wp-content/uploads/2016/03/O6.1-Gary-Schwartz.pdf

I recall this is where Aprea (APR-246 / PRIMA-1 MET) is headed as it seems their compound has some toxicity concerns (unlike Kevetrin) as a Monotherapy (like Nutlins) -- below articles, Wiman Group.

Also saw long dormant Aileron posted an abstract at ASCO. Their stapled-peptide approach.

http://www.businesswire.com/news/home/20170518005400/en/Aileron-Therapeutics-Announces-Oral-Presentation-ASCO-ALRN-6924

APREA
https://academic.oup.com/biohorizons/article/doi/10.1093/biohorizons/hzv006/1742527/PRIMA-1-as-a-cancer-therapy-restoring-mutant-p53-a

"PRIMA-1 acts to restore the mutant p53 by modifying thiol groups in the core domains of the protein. Its success is well documented, with many studies in different cancer models proving its effectiveness. This, however, is not unanimous, with some questions being raised about its efficacy and other aspects such as possible resistance mechanisms as well as potentially harmful degradation products."

https://www.researchgate.net/profile/Vladimir_Lazarevic2/publication/305366769_An_open-label_phase_I_dose-finding_study_of_APR-246_in_hematological_malignancies/links/578b4c9708ae254b1de34a18.pdf

http://ki.se/en/onkpat/klas-g-wimans-group

http://tatcongress.org/wp-content/uploads/2016/03/O6.3-John-Green.pdf
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