Abstract: We describe the first chemical synthesis of a functional mutant of the DNA binding domain of the oncoprotein MYC, using two alternative strategies which involve either one or two Native Chemical Ligations (NCLs). Both routes allowed the efficient synthesis of a miniprotein which is capable of heterodimerizing with MAX, and replicate the DNA binding of the native protein. The versatility of the reported synthetic approach enabled the straightforward preparation of MYC and Omomyc analogues, as well as fluorescently labeled derivatives

External link: https://pubs.rsc.org/en/Content/ArticleLanding/2019/OB/C9OB01209E#!divAbstract

Abstract:

Rh(III) catalysts can promote a formal (4 + 2) intramolecular oxidative annulation between acrylic or benzoic acid derivatives and alkynes. The reaction, which involves a C–H activation process, allows for a rapid assembly of appealing bicyclic pyran-2-ones and tricyclic isocoumarin derivatives in moderate to good yields. The α-pyrone moiety of the products provides for further manipulations to obtain relatively complex cyclic skeletons in a very simple manner.

External link: https://pubs.acs.org/doi/10.1021/acsomega.9b00022

In this Account, we present recent efforts on the development of platinum- and gold-catalyzed formal cycloadditions of allenes, only including annulations initiated by a direct metal-promoted activation of the allene moiety.This Account is organized considering the number of atoms engaged in the annulation process, and when possible, we present the results in a chronological order.

External link: https://pubs.acs.org/doi/10.1021/acs.accounts.8b00567