《Functional characterization of a PROTAC directed against BRAF mutant V600E》 was written by Posternak, Ganna; Tang, Xiaojing; Maisonneuve, Pierre; Jin, Ting; Lavoie, Hugo; Daou, Salima; Orlicky, Stephen; Goullet de Rugy, Theo; Caldwell, Lauren; Chan, Kin; Aman, Ahmed; Prakesch, Michael; Poda, Gennady; Mader, Pavel; Wong, Cassandra; Maier, Stefan; Kitaygorodsky, Julia; Larsen, Brett; Colwill, Karen; Yin, Zhe; Ceccarelli, Derek F.; Batey, Robert A.; Taipale, Mikko; Kurinov, Igor; Uehling, David; Wrana, Jeff; Durocher, Daniel; Gingras, Anne-Claude; Al-Awar, Rima; Therrien, Marc; Sicheri, Frank. Application In Synthesis of N-Boc-1,6-Diaminohexane And the article was included in Nature Chemical Biology in 2020. The article conveys some information:
Abstract: The RAF family kinases function in the RAS-ERK pathway to transmit signals from activated RAS to the downstream kinases MEK and ERK. This pathway regulates cell proliferation, differentiation and survival, enabling mutations in RAS and RAF to act as potent drivers of human cancers. Drugs targeting the prevalent oncogenic mutant BRAF(V600E) have shown great efficacy in the clinic, but long-term effectiveness is limited by resistance mechanisms that often exploit the dimerization-dependent process by which RAF kinases are activated. Here, we investigated a proteolysis-targeting chimera (PROTAC) approach to BRAF inhibition. The most effective PROTAC, termed P4B, displayed superior specificity and inhibitory properties relative to non-PROTAC controls in BRAF(V600E) cell lines. In addition, P4B displayed utility in cell lines harboring alternative BRAF mutations that impart resistance to conventional BRAF inhibitors. This work provides a proof of concept for a substitute to conventional chem. inhibition to therapeutically constrain oncogenic BRAF. [graphic not available: see fulltext]. The results came from multiple reactions, including the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Application In Synthesis of N-Boc-1,6-Diaminohexane)
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsApplication In Synthesis of N-Boc-1,6-Diaminohexane
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