Development of creative and groundbreaking
research at the interface of Chemistry, Biology and Medicine.
Education of researchers in order they become
future leaders of academic or industrial projects.
Transferring of knowledge to Society in order
to propel economical and social progress
Abstract: Transcription factors (TFs) have a remarkable role in the homeostasis of the organisms and there is a growing interest in how they recognize and interact with specific DNA sequences. TFs recognize DNA using a variety of structural motifs. Among those, the ribbon-helix-helix (RHH) proteins, exemplified by the MetJ and ARC repressors, form dimers that insert antiparallel β-sheets into the major groove of DNA. A great chemical challenge consists of using the principles of DNA recognition by TFs to design minimized peptides that maintain the DNA affinity and specificity characteristics of the natural counterparts. In this context, a peptide mimic of an antiparallel β-sheet is very attractive since it can be obtained by a single peptide chain folding in a β-hairpin structure and can be as short as 14 amino acids or less. Herein, we designed eight linear and two cyclic dodeca-peptides endowed with β-hairpins. Their DNA binding properties have been investigated using fluorescence spectroscopy together with the conformational analysis through circular dichroism and solution NMR. We found that one of our peptides, peptide 6, is able to bind DNA, albeit without sequence selectivity. Notably, it shows a topological selectivity for the major groove of the DNA which is the interaction site of ARC and many other DNA-binding proteins. Moreover, we found that a type I’ β-hairpin folding pattern is a favorite peptide structure for interaction with the B-DNA major groove. Peptide 6 is a valuable lead compound for the development of novel analogs with sequence selectivity.
We are very happy to share here that our research article at J. Am. Chem. Soc., entitled "Kinetic Resolution of Allyltriflamides through a Pd-Catalyzed C–H Functionalization with Allenes: Asymmetric Assembly of Tetrahydropyridines" and authored by J. M. González, B. Cendón, J. L. Mascarenas and M. Gulías, has been accepted and it's already available through the journal website.
Abstract: Enantioenriched, six-membered azacycles are essential structural motifs in many products of pharmaceutical or agrochemical interest. Here we report a simple and practical method for enantioselective assembly of tetrahydropyridines, which is paired to a kinetic resolution of α-branched allyltriflamides. The reaction consists of a formal (4+2) cycloaddition between the allylamine derivatives and allenes and is initiated by a palladium(II)-catalyzed C–H activation process. Both the chiral allylamide precursors and the tetrahydropyridine adducts were successfully obtained in high yields, with excellent enantioselectivity (up to 99% ee) and selectivity values of up to 127.
External link: https://pubs.acs.org/doi/10.1021/jacs.1c01929
Abstract: Low‐valent cobalt complexes equipped with chiral ligands can efficiently promote highly enantioselective (3+2) cycloadditions of alkyne‐tethered alkylidenecyclopropanes. The annulation allows to assemble bicyclic systems containing five‐membered rings in good yields and with excellent enantiomeric ratios. We also present a mechanistic discussion based on experimental and computational data, which support the involvement of Co(I)/Co(III) catalytic cycles
External link: https://onlinelibrary.wiley.com/doi/10.1002/anie.202015202
José Luis Mascareñas, PhD leads this team of researchers. Find out more about him and the rest of the team in our Group members section.Group Members
We are always looking forward to welcoming exceptional candidates into our research Group. Please visit our Opportunities section or send us your cv.Opportunities
Annual mean temperature. The humid oceanic climate guarantees mild weather throughout the year.
Students attend the University. With the city population around 100,000.
Year old University. Currently imparting more than 60 degrees.
Santiago is well connected, having its own international airport, train station, etc.
Amongst many awards, Santiago was declared World Heritage City by UNESCO in 1985.
Santiago de Compostela is the capital of Galicia de most Nortwestern region of Spain.
Public transport is available in order to get around the city, which is also conveniently located to visit other sites in Galicia.
Spanish and Galician are the two official languages of Galicia. Your work will be carried out in English.