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- W2562804768 abstract "Protein-protein interactions (PPIs) present a challenging target for the development ofinhibitors, due to the large size and lipophilicity of protein binding sites. Because of this,work that is able to increase our understanding of how PPI inhibitors can be betterdeveloped is of great value.In unusual cases, approved drug compounds are able to exhibit excellent pharmacological(PK) profiles despite having unfavourable physical properties. New methodology wasdeveloped whereby the solubilising side chains found in one such compound, daclatasvir,could be incorporated onto aryl-bromides using palladium-catalysed C-H activation. Thescope of the reaction was tested, and in 18 different examples the C-H activation wasfound to be successful 11 times.1 This methodology has application in the potentialsynthesis of cell-permeable PPI inhibitors.Inhibiting the PALB2/BRCA2 PPI has the potential to produce synthetic lethality incancerous cells with damaged DNA repair mechanisms. Computational techniques wereused to design small-molecule and miniprotein mimetics of BRCA2, which couldpotentially competitively inhibit PALB2/BRCA2. This resulted in the purchase of 10miniprotein sequences ready for testing, one of which has been proven to have significanthelical secondary structure. The synthesis of small molecule α-helical mimetics ofBRCA2 has also been carried out, with one compound ready for biological testing andthe synthesis of two others close to completion.Publications:1 T. O. Moore, M. Paradowski and S. E. Ward, Org. Biomol. Chem., 2016, 14,3307–3313." @default.
- W2562804768 created "2017-01-06" @default.
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- W2562804768 date "2016-09-13" @default.
- W2562804768 modified "2023-09-27" @default.
- W2562804768 title "Synthetic strategies towards challenging PPI drug targets" @default.
- W2562804768 hasPublicationYear "2016" @default.
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