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Two in a row!! A second publication in collaboration with Prof. E. Vázquez is also on-line

Extremely happy to announce the second 2022 collaborative paper is already published

We are really glad to share this second 2022 collaborative paper, published at Commun. Chem., has been already accepted and it's available through the journal website. The communication is entitled "Controlling oncogenic KRAS signaling pathways with a Palladium-responsive peptide" and authored by S. Learte-Aymamí, P. Martin-Malpartida, L. Roldán-Martín, G. Sciortino, J. R. Couceiro, J.-D. Maréchal, M. J. Macias, J. L. Mascareñas and M. E. Vázquez.

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.

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Our most recent collaboration is already on-line at Chem. Commun.

So glad to announce our first 2022 collaborative paper is already published

We are very happy to share our Chem. Commun. paper in collaboration with Vázquez & Vázquez research group, among others, has been accepted and it's already available through the journal website. This work is entitled "Selective recognition of A/T-rich DNA 3-way junctions with a three-fold symmetric tripeptide" and authored by J. Gomez-Gonzalez, L. Martinez-Castro, J. Tolosa-Barrilero, A. Alcalde-Ordoñez, S. Learte-Aymamí, J. L. Mascareñas, J. C. García-Martínez, J. Martínez-Costas, J.-D. Maréchal, M. Vázquez and E. Vázquez.

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.

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Congratulations to Soraya Learte, who received the Honorable Mention for the 2022 IUPAC-Solvay International Award for Young Chemists

Our group member has received her awarded PhD in April 2021

We are celebrating today the great success of Dr. Soraya Learte, who has been awarded with one of the threee honorable metions of the 2022 IUPAC-Solvay International Award for Young Chemists. The award is a consequence of her commitment and also her stunning results during her doctoral studies at our research group. Her PhD thesis is entitled "Metallopeptides and Metalloproteins in Chemical Biology: from DNA Binding to Intracellular Catalysis".

During her PhD studies, Soraya has mainly worked in the design, synthesis, and application of metallopeptides and metalloproteins within the area of Chemical Biology.

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A brand new review at Chemical Science is already on-line

Happy to announce our last review regarding "Organometallic Catalysis in Aqueous and Biological Environments" is already at the journal website

We are very glad to share here that our review at Chem. Sci., entitled "Organometallic Catalysis in Aqueous and Biological Environments: Harnessing the Power of Metal Carbenes" and authored by S. Gutiérrez, M. Tomás and J. L. Mascarenas, is already available through the journal website.

Abstract: Translating the power of transition metal catalysis to the native habitats of enzymes can significantly expand the possibilities of interrogating or manipulating natural biological systems, including living cells and organisms. This is especially relevant for organometallic reactions that have shown great potential in the field of organic synthesis, like the metalcatalyzed transfer of carbenes. While, at first sight, performing metal carbene chemistry in aqueous solvents, and especially in biologically relevant mixtures, does not seem obvious, in recent years there have been a growing number of reports demonstrating the feasibility of the task. Either using small molecule metal catalysts or artificial metalloenzymes, a number of carbene transfer reactions that tolerate aqueous and biorelevant media are being developed. This review intends to summarize the most relevant contributions, and establish the state of the art in this emerging research field.

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Our first review for 2022 is already on-line

Pleased to announce our review paper at Eur J. Org. Chem. has been accepted, and it's already available through the publisher website

We are so happy to announce here that our review article at EurJOC, entitled "Exporting Homogeneous Transition Metal Catalysts to Biological Habitats" and authored by A. Seoane and J. L. Mascarenas has been accepted and it's already on-line.

Abstract: The possibility of performing designed transition-metal catalyzed reactions in biological and living contexts can open unprecedented opportunities to interrogate and interfere with biology. However, the task is far from obvious, in part because of the presumed incompatibly between organometallic chemistry and complex aqueous environments.  Nonetheless, in the past decade there has been a steady progress in this research area, and several transition-metal (TM)-catalyzed bioorthogonal and biocompatible reactions have been developed. These reactions encompass a wide range of mechanistic profiles, which are very different from those used by natural metalloenzymes. Herein we present a summary of the latest progress in the field of TM-catalyzed bioorthogonal reactions, with a special focus on those triggered by activation of multiple carbon-carbon bonds.

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