Development of a novel electrochemical biosensor based on plastic antibodies for detection of STEAP1 biomarker in cancer.

STEAP1 is a cell surface protein of the STEAP family whose main function focuses on intercellular communication and cell growth. STEAP1 is considered a promising putative biomarker and a candidate target for prostate cancer treatment. For specific and selective detection of STEAP1, a molecularly imprinted polymers (MIP) was developed on a screen-printed electrode (C-SPE) whose surface was modified with a nanocomposite based on carbon nanotubes decorated with dendritic platinum nanoparticles (CNTs- PAH /Pt).

Development of a biosensor for phosphorylated Tau 181 protein detection in Early-Stage Alzheimer's disease.

Alzheimer's disease (AD) is the most common form of dementia in the elderly, and there are still no reliable methods for its early detection. Recently, the phosphorylated protein Tau181 (p-Tau181) was identified as a highly specific biomarker for AD. Therefore, in this work, a new strategy for the development of an electrochemical-based immunosensor for the detection of p-Tau181 is described.

Total synthesis of nahuoic acid A a putative biogenetic intramolecular Diels-Alder (IMDA) reaction.

Inspired by the biogenetic proposal of an intramolecular Diels-Alder (IMDA) cycloaddition, the total synthesis of natural product nahuoic acid A, a cofactor-competitive inhibitor of the epigenetic enzyme lysine methyl transferase SETD8, has been carried out. A non-conjugated pentaenal precursor was synthesized with high levels of stereoselectivity at seven stereogenic centers and with the appropriate control of double bond geometries. Although the IMDA reaction of the non-conjugated pentaenal using MeAlCl for catalysis at -40 °C selectively afforded the -fused diastereomer corresponding to the mode of cycloaddition, under thermal reaction conditions it gave rise to a mixture of diastereomers, that preferentially formed through the mode, including the -fused angularly-methylated octahydronaphthalene diastereomer precursor of nahuoic acid A.

Synthesis and Biological Evaluation of Tripartin, a Putative KDM4 Natural Product Inhibitor, and 1-Dichloromethylinden-1-ol Analogues.

The natural product tripartin has been reported to inhibit the N-methyl-lysine histone demethylase KDM4A. A synthesis of tripartin starting from 3,5-dimethoxyphenylacrylic acid was developed, and the enantiomers were separated by chiral HPLC. We observed that both tripartin enantiomers manifested an apparent increase in H3K9me3 levels when dosed in cells, as measured by western blot analysis.

Synthesis of the octahydronaphthalene core of nahuoic acid A via a B(CF)-catalyzed intramolecular Diels-Alder (IMDA) reaction.

Model tetraenal 9b underwent intramolecular Diels-Alder cycloaddition in CHCl at -10 °C under catalysis by the bulky Lewis acid B(CF) to deliver as major components the cis-fused angularly-methylated octahydronaphthalene products, which are formed through the alternative exo orientations of the reacting moieties. One of these diastereomers features the relative and absolute configuration present in the core of nahuoic acid A, a natural product that acts as a cofactor-competitive inhibitor of the lysine methyl transferase SETD8. By contrast, catalysis of the reaction by MeAlCl at -40 °C selectively afforded the trans-fused isomer resulting from the Re-endo orientation.