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Joan Miguel Ávila is our brand new Doctor in the group, after defending his PhD entitled "Transition Metal-Catalyzed Annulations in Biological Media".
External link: https://twitter.com/MetBioCat/status/1547901384208461825
Abstract: The relevance of chiral pharmaceuticals and fine chemicals has encouraged the development of synthetic methods that allow the preparation of these products in enantioselective form. Of the different strategies, those relying on the metal-catalyzed enantioselective activation of C-H bonds are especially appealing, owing to their step and atom economy. This is particularly the case in desymmetrization approaches, because of the simplicity of the reactants, and their intrinsic complexity increase characteristics. This article reviews the current state of the art on transition metal-catalyzed desymmetrizing functionalizations involving enantiodetermining C-H activation steps.
Abstract: RAS oncoproteins are molecular switches associated with critical signaling pathways that regulate cell proliferation and differentiation. Mutations in the RAS family, mainly in the KRAS isoform, are responsible for some of the deadliest cancers, which has made this protein a major target in biomedical research. Here we demonstrate that a designed bis-histidine peptide derived from the αH helix of the cofactor SOS1 binds to KRAS with high affinity upon coordination to Pd(II). NMR spectroscopy and MD studies demonstrate that Pd(II) has a nucleating effect that facilitates the access to the bioactive α-helical conformation. The binding can be suppressed by an external metal chelator and recovered again by the addition of more Pd(II), making this system the first switchable KRAS binder, and demonstrates that folding-upon-binding mechanisms can operate in metal-nucleated peptides. In vitro experiments show that the metallopeptide can efficiently internalize into living cells and inhibit the MAPK kinase cascade.
External link: https://www.nature.com/articles/s42004-022-00691-7
Abstract: Non-canonical DNA structures, particularly 3-Way Junctions (3WJs) that are transiently formed during DNA replication, have recently emerged as promising chemotherapeutic targets. Here, we describe a new approach to target 3WJs that relies on the cooperative and sequence-selective recognition of A/T-rich duplex DNA branches by three AT-Hook peptides attached to a three-fold symmetric and fluorogenic 1,3,5-tristyrylbenzene core.
External link: https://twitter.com/ciqususc/status/1535246221882834948