A5068607171- Enzyme Catalysis and Immobilization
- Microbial Natural Products and Biosynthesis
- Cancer Mechanisms and Therapy
- Carbohydrate Chemistry and Synthesis
- Estrogen and related hormone effects
- Cytokine Signaling Pathways and Interactions
- Asymmetric Hydrogenation and Catalysis
- Synthesis and biological activity
- Chemical Synthesis and Analysis
- Sarcoma Diagnosis and Treatment
- Quinazolinone synthesis and applications
- Cancer therapeutics and mechanisms
- Biochemical and Molecular Research
- Steroid Chemistry and Biochemistry
- Click Chemistry and Applications
- Ubiquitin and proteasome pathways
- Cancer-related Molecular Pathways
- HIV/AIDS drug development and treatment
- Cancer Cells and Metastasis
- Enzyme function and inhibition
- RNA modifications and cancer
- Synthetic Organic Chemistry Methods
- HER2/EGFR in Cancer Research
- Microbial Metabolic Engineering and Bioproduction
- Peptidase Inhibition and Analysis
EntreChem (Spain)
2016-2025
Instituto de Ciencias de la Vid y del Vino
2018-2021
Universidad de Oviedo
1991-2020
Universidad de Salamanca
2016
Hospital General Universitario Gregorio Marañón
2016
Centro de Investigación del Cáncer
2012
Consejo Superior de Investigaciones Científicas
1992
Transition-metal complexes and purified ketoreductases work together in eutectic mixtures for the synthesis of enantiopure secondary alcohols.
Mithramycin is an antitumor compound produced by Streptomyces argillaceus that has been used for the treatment of several types tumors and hypercalcaemia processes. However, its use in humans limited because side effects. Using combinatorial biosynthesis approaches, we have generated seven new mithramycin derivatives, which differ from parental sugar profile or both 3-side chain. From these studies three novel derivatives were identified, demycarosyl-3D-β-d-digitoxosylmithramycin SK,...
The development of cell-free and self-sufficient biocatalytic systems represents an emerging approach to address more complex synthetic schemes under nonphysiological conditions. Herein, we report the a heterogeneous biocatalyst for synthesis chiral alcohols without need add exogenous cofactor. In this work, NADPH-dependent ketoreductase was primarily stabilized further co-immobilized with NADPH catalyze asymmetric reductions addition As result, immobilized cofactor is accessible, thus, it...
Abstract Purpose: The goal of this study was to identify second-generation mithramycin analogues that better target the EWS-FLI1 transcription factor for Ewing sarcoma. We previously established as an inhibitor, but compound's toxicity prevented its use at effective concentrations in patients. Experimental Design: screened a panel mithralogs establish their ability inhibit compared IC50 with MTD mice determine relationship between efficacy and toxicity. confirmed suppression promoter, mRNA,...
The first application of Deep Eutectic Solvents (DESs) in asymmetric bioamination ketones has been accomplished. amine transaminases (ATAs) turned out to be particularly stable DES-buffer mixtures at a percentage up 75% (w/w) neoteric solvent. Moreover, this reaction medium was used perform chemoenzymatic cascade toward biaryl amines by coupling Suzuki sequentially with an enantioselective catalyzed the recently discovered ATA from Exophiala xenobiotica (EX-ωTA). solubilizing properties DESs...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA useful and versatile procedure for the acylation of nucleosides through an enzymic reactionFrancisco Moris Vicente GotorCite this: J. Org. Chem. 1993, 58, 3, 653–660Publication Date (Print):January 1, 1993Publication History Published online1 May 2002Published inissue 1 January 1993https://pubs.acs.org/doi/10.1021/jo00055a018https://doi.org/10.1021/jo00055a018research-articleACS PublicationsRequest reuse permissionsArticle...
Abstract The ruthenium‐catalyzed redox isomerization of allylic alcohols was successfully coupled with the enantioselective enzymatic ketone reduction (mediated by KREDs) in a concurrent process aqueous medium. overall transformation, formally asymmetric alcohols, took place excellent conversions and enantioselectivities, under mild reaction conditions, employing commercially readily available catalytic systems, without external coenzymes or cofactors. Optimization resulted multistep...
This study investigates for the first time crosstalk between stromal fibroblasts and cancer stem cell (CSC) biology in head neck squamous carcinomas (HNSCC), with ultimate goal of identifying effective therapeutic targets. The effects conditioned media from cancer-associated (CAFs) normal (NFs) on CSC phenotype were assessed by combining functional expression analyses HNSCC-derived lines. Further characterization CAFs NFs secretomes mass spectrometry was followed pharmacologic target...
Phenolic acid decarboxylase from Bacillus subtilis (BsPAD) converts several p-hydroxycinnamic derivatives into the corresponding p-hydroxystyrenes, which are considered to be promising bio-based aromatic chemicals. Despite enzyme's high activity and stability, low solubility of its substrates presents severe limitations for establishment industrial processes. Accordingly, deep eutectic solvents (DESs) have emerged as interesting alternatives aqueous or organic biphasic systems they offer...
The ruthenium-catalysed isomerisation of allylic alcohols was coupled, for the first time, with asymmetric bioamination in a one-pot process an aqueous medium.
The combination of the metal-catalyzed cycloisomerization alkynes containing a tethered nucleophile as substituent in aqueous media (followed by spontaneous hydrolysis, hydroalkoxylation, or aminolysis transiently formed five-membered heterocycles) with subsequent enantioselective ketone bioreduction (mediated KREDs) has been achieved. overall transformations, which formally involve three-step one-pot reaction, provide variety enantiopure valuable molecules (e.g., 1,4-diols, lactones, and...
Abstract One of the pioneering examples chemoenzymatic cascades in water such as palladium‐catalysed Suzuki‐cross coupling followed by an enzymatic reduction has been revisited employment a medium containing Deep Eutectic Solvents ( DESs ) for catalytic performance. Thus, unique properties these neoteric solvents enabled to reach high substrate concentration overall process. Moreover, both isolated enzymes and whole cells exhibited excellent activities which allowed obtain set chiral biaryl...
We report the generation of novel glycosylated indolocarbazoles by combinatorial biosynthesis, and identification two potent selective compounds inhibitors JAK2 Ikkb kinases.
Deregulated activity of transcription factors (TFs) the Sp/KLF family, like Sp1, Sp3 and Sp4, consequent over-expression Sp-regulated genes occur frequently in human cancers. This provides rationale for development inhibitors Sp TFs as cancer therapeutics. Mithramycin A (MTM-A) is a natural polyketide that binds GC-rich DNA sequences, inhibits exhibits potent antitumor experimental systems. However, clinical use MTM-A limited by severe toxicity compound. Here, we studied two analogues, which...
Abstract Tumors evolve from initial tumorigenic events into increasingly aggressive behaviors in a process usually driven by subpopulations of cancer stem cells (CSCs). Mesenchymal stromal/stem (MSCs) may act as the cell-of-origin for sarcomas and CSCs that present MSC features have been identified due to their ability grow self-renewed floating spheres (tumorspheres). Accordingly, we previously developed sarcoma models using human MSCs transformed with relevant oncogenic events. To study...
// Juan Tornin 1 , Lucia Martinez-Cruzado Laura Santos Aida Rodriguez Luz-Elena Núñez 2 Patricia Oro Maria Ana Hermosilla Eva Allonca Teresa Fernández-García 3 Aurora Astudillo 4 Carlos Suarez Francisco Morís Rene Hospital Universitario Central de Asturias and Instituto Oncología del Principado Asturias, Oviedo, Spain EntreChem SL, Unidad Histopatología Molecular en Modelos Animales Cáncer, IUOPA, Universidad Servicio Anatomía Patológica, Correspondence to: Rodriguez, e-mail: renerg@ficyt.es...
A hybrid organo- and biocatalytic system for the asymmetric conversion of racemic alcohols into amines was developed. Combining an organocatalyst, AZADO, oxidant, NaOCl, enzyme, ω-transaminase, we implemented a one-pot oxidation–transamination sequential process in aqueous medium. The method showed broad substrate scope successfully applied to conventional secondary sterically hindered β-substituted cycloalkanols, where highly stereoselective dynamic bioamination enabled us set up both...
Abstract Cancer stem cells (CSC) contribute to disease progression and treatment failure in prostate cancer because of their intrinsic resistance current therapies. The transcription factors NF-κB STAT3 are frequently activated advanced sustain expansion CSCs. EC-70124 is a novel chimeric indolocarbazole compound generated by metabolic engineering the biosynthetic pathways glycosylated indolocarbazoles, such as staurosporine rebeccamycin. In vitro kinome analyses revealed that acted...
Abstract Background MiT-Renal Cell Carcinoma (RCC) is characterized by genomic translocations involving microphthalmia-associated transcription factor (MiT) family members TFE3 , TFEB or MITF . MiT-RCC represents a specific subtype of sporadic RCC that predominantly seen in young patients and can present with heterogeneous histological features making diagnosis challenging. Moreover, the disease biology this aggressive cancer poorly understood there no accepted standard care therapy for...
ABSTRACT Fungal infections are a growing global health concern due to the limited number of available antifungal therapies as well emergence fungi that resistant first-line antimicrobials, particularly azoles and echinocandins. Development novel, selective is challenging similarities between fungal mammalian cells. An attractive source potential treatments provided by ecological niches co-inhabited bacteria, fungi, multicellular organisms, where complex relationships multiple organisms have...