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clock Created with Sketch. 15/07/17
17:48
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Originally posted by waynesworld
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The listing of the collaboration with Professor Sir David Lane of A*Star, alongside Genentech, in the latest Operational Update tends to elevate the importance of the academic research work with Lane. So what do we know about the collaboration - a little or a lot?Guardian of the Genome , it was noted that Lane may be interested in the FPP platform for intracellular delivery of cargo payloads targeting the MDM-p53 pathway rather than the dual targeting of p53 and Myc;MDM/p53 as a drug target in Cancer . Phylogica discusses a DPMI-a peptide that binds MDM2 with high affinity but can't penetrate cells. A FPP-DPMI-a enhances the delivery of the peptide into breast cancer cells. SoT covered it in his post of 2 March 2015, "so it’s possible [FPP] 1746 could be linked to not only omomyc, but to other protein drug molecules [such as DPMI-a] that to-date have been unable to efficiently access inner cellular targets".Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays which includes several authors from the p53 lab including Lane, we find a reference to the intrinsic problem plaguing peptide inhibitors against MDM2/MDM4-p53 interactions. Whereas the new class of drugs have the potential to be optimised for high binding affinity and specificity, the mechanism for cellular uptake, cellular availability and intracellular binding is still elusive.Drugging the p53 pathway: understanding the route to clinical efficacy by authors including Lane, the subject of toxicity is discussed in initial clinical trials where inhibitors of MDM2 have shown efficacy but hint at on target toxicities.
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"A star in the making" "Blockbuster" and the many other Lofty expressions have brightened my week -especially after spending most of it in a very cold New Zealand.
(20min delay)