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Artículo
Stable Pyrrole-Linked Bioconjugates through Tetrazine-Triggered Azanorbornadiene Fragmentation
(Wiley-Blackwell, 2020)
An azanorbornadiene bromovinyl sulfone reagent for cysteine-selective bioconjugation has been developed. Subsequent reaction with dipyridyl tetrazine leads to bond cleavage and formation of a pyrrole-linked conjugate. The ...
Artículo
Inter-Ligand STD NMR: An Efficient 1D NMR Approach to Probe Relative Orientation of Ligands in a Multi-Subsite Protein Binding Pocket
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
In recent years, Saturation Transfer Difference NMR (STD NMR) has been proven to be a powerful and versatile ligand-based NMR technique to elucidate crucial aspects in the investigation of protein-ligand complexes. Novel ...
Artículo
Synthesis and Structure-activity Relationship of New Nicotinamide Phosphoribosyltransferase Inhibitors with Antitumor Activity on Solid and Haematological Cancer
(Elsevier, 2023)
Cancer cells are highly dependent on Nicotinamide phosphoribosyltransferase (NAMPT) activity for proliferation, therefore NAMPT represents an interesting target for the development of anti-cancer drugs. Several compounds, ...
Artículo
Transferring Substituents from Alkynes to Furans and Pyrroles through Heteronorbornadienes as Intermediates: Synthesis of β-Substituted Pyrroles/Furans
(American Chemical Society, 2023)
The use of 7-oxa/azanorbornadienes as synthetic intermediates for the preparation of 3/4-substituted (β-substituted) furans/pyrroles is presented. The method lies in the inverse electron demand Diels-Alder (iEDDA) cycloaddition ...
Artículo
Structure-Based Identification and Biological Characterization of New NAPRT Inhibitors
(Multidisciplinary Digital Publishing Institute (MDPI), 2022)
NAPRT, the rate-limiting enzyme of the Preiss–Handler NAD biosynthetic pathway, has emerged as a key biomarker for the clinical success of NAMPT inhibitors in cancer treatment. Previous studies found that high protein ...
Tesis Doctoral
Síntesis y reactividad de sistemas [2.2.1]bicíclicos. Estudio de la bioconjugación de proteínas con azanorbornadienos
(2020-05-24)
En esta Tesis Doctoral se presentan los resultados más relevantes obtenidos del estudio de reactividad llevado a cabo sobre sistemas [2.2.1]bicíclicos (7-heteronorbornanos y 7- heteronorbornadienos), así como su aplicación ...
Artículo
Discovery of human hexosaminidase inhibitors by in situ screening of a library of mono- and divalent pyrrolidine iminosugars
(Elsevier, 2022)
Two libraries of mono- and dimeric pyrrolidine iminosugars were synthesized by CuAAC and (thio)urea-bond-forming reactions from the respective azido/aminohexylpyrrolidine iminosugar precursors. The resulting monomeric and ...
Artículo
Exploring Multi-Subsite Binding Pockets in Proteins: DEEP-STD NMR Fingerprinting and Molecular Dynamics Unveil a Cryptic Subsite at the GM1 Binding Pocket of Cholera Toxin B
(Wiley, 2020)
Ligand-based NMRtechniquesto studyprotein–ligandinteractionsare potenttoolsin drugdesign.Satura-tiontransfer difference (STD)NMRspectroscopystandsoutas one of the mostversatiletechniques,allowing screeningof fragmentslibraries ...
Tesis Doctoral
Synthesis of new nampt inhibitors as potential anti-cancer drugs. An approach to antibody-drug conjugates
(2023-01-27)
Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step in the biosynthesis of Nicotinamide Adenine Dinucleotide (NAD+), a cofactor essential for several cellular processes. NAD+ is involved in ...
Artículo
Experimental and Theoretical Analysis of the Thiol-Promoted Fragmentation of 2-Halo-3-tosyl-oxanorbornadienes
(American Chemical Society, 2023)
2-Halo-3-tosyl-oxanorbornadienes are able to accept two thiol molecules through an initial nucleophilic substitution, giving isolable oxabicyclic thiovinyl sulfones that, subsequently, can react with a second thiol molecule ...