A5087351584- Enzyme function and inhibition
- Synthesis and Catalytic Reactions
- Cholinesterase and Neurodegenerative Diseases
- Phenothiazines and Benzothiazines Synthesis and Activities
- Chemical Reactions and Mechanisms
- Advanced Glycation End Products research
- Insect Resistance and Genetics
- Enzyme Catalysis and Immobilization
- Insect and Pesticide Research
- Mycotoxins in Agriculture and Food
- Plant-Microbe Interactions and Immunity
- Insect behavior and control techniques
- Polyamine Metabolism and Applications
- Biochemical effects in animals
- Phytochemicals and Antioxidant Activities
- Electrochemical sensors and biosensors
- Insect-Plant Interactions and Control
- Essential Oils and Antimicrobial Activity
- Protein Hydrolysis and Bioactive Peptides
- Glycosylation and Glycoproteins Research
- Chemical synthesis and alkaloids
- Plant tissue culture and regeneration
- Melanoma and MAPK Pathways
- Pancreatic function and diabetes
- NF-κB Signaling Pathways
Institute of Biostructure and Bioimaging
2015-2024
National Research Council
2008-2024
National Academies of Sciences, Engineering, and Medicine
2012-2024
Istituto Nazionale di Fisica Nucleare, Sezione di Napoli
2020
Naples Anesthesia & Physician Associates
2014-2020
University of Buenos Aires
2017
Centro Interuniversitario di Ricerca sui Peptidi Bioattivi
2013
Tampere University
2008
Balboa Nephrology Medical Group
2008
University of Naples Federico II
1997-2006
Carbonic anhydrase (CA) IX is a plasma membrane-associated member of the α-CA enzyme family, which involved in solid tumor acidification. It marker hypoxia and prognostic factor several human cancers. An aberrant increase CA expression chronic during development various carcinomas contributes to tumorigenesis through at least two mechanisms: pH regulation cell adhesion control. Here we report X-ray structure catalytic domain complex with classical, clinically used sulfonamide inhibitor,...
Carbonic anhydrase IX (CA IX) is an exceptional member of the CA protein family; in addition to its classical role pH regulation, it has also been proposed participate cell proliferation, adhesion, and tumorigenic processes. To characterize biochemical properties this membrane protein, two soluble recombinant forms were produced using baculovirus-insect expression system. The proteins consisted either catalytic domain only form) or extracellular domain, which included both proteoglycan...
The X-ray crystal structure of the fluorescent antitumor sulfonamide carbonic anhydrase (CA, EC, 4.2.1.1) inhibitor (4-sulfamoylphenylethyl)thioureido fluorescein (1) in complex with cytosolic isoform hCA II is reported, together a modeling study adduct 1 tumor-associated IX. Its binding to similar that other benzesulfonamides, ionized coordinated Zn2+ ion within enzyme active site, and also participating network hydrogen bonds residues Thr199 Glu106. scaffold did not establish polar...
A structural study of the adduct which 2-benzylsulfinylbenzoic acid forms with human carbonic anhydrase II is reported, showing a binding mode completely different from any other class inhibitors investigated so far; this carboxylate binds in pocket situated out enzyme active site.
Making males in a fruit fly pest The Mediterranean or Medfly ( Ceratitis capitata ) is global and highly destructive pest. Meccariello et al. identified the master gene for male sex determination on Y chromosome of named it Maleness-on-the-Y MoY (see Perspective by Makki Meller). Flies each were transformed into other genetic manipulation, crosses files generated female progeny. functionally conserved olive invasive oriental fly. This discovery has potential insect control based mass release...
SspCA, a novel `extremo-α-carbonic anhydrase' isolated from the thermophilic bacterium Sulfurihydrogenibium yellowstonense YO3AOP1, is an efficient catalyst for hydration of CO2 and presents exceptional thermostability. Indeed, SspCA retains high catalytic activity even after being heated to 343-373 K several hours. Here, crystallographic structure this α-carbonic anhydrase (α-CA) reported factors responsible its function at temperature are elucidated. In particular, study suggests that...
Abstract The cytosolic isoform XIII is a recently discovered member of the human carbonic anhydrase (hCA, EC 4.2.1.1) family. It selectively expressed among other tissues in reproductive organs, where it may control pH and ion balance regulation, ensuring thus proper fertilization conditions. authors report here X‐ray crystallographic structure this isozyme unbound state complex with classical sulfonamide inhibitor, namely acetazolamide. A detailed comparison obtained structural data those...
A series of nitroimidazoles incorporating sulfonamide/sulfamide/sulfamate moieties were designed and synthesized as radio/chemosensitizing agent targeting the tumor-associated carbonic anhydrase (CA) isoforms IX XII. Most new compounds nanomolar inhibitors these isoforms. Crystallographic studies on complex hCA II with lead sulfamide derivative this clarified binding mode type in enzyme active site cavity. Some best nitroimidazole CA showed significant activity vitro by reducing...
In this paper we report the synthesis of a series benzoxaborole derivatives, their inhibition properties against some carbonic anhydrases (CAs), recognized as important drug targets, and characterization binding mode these molecules to CA active site. Our data provide first experimental evidence that benzoxaboroles can be efficiently used inhibitors.
The multi-component fingerprint and the biological evaluation of plant-derived material are indispensable for pharmaceutical field, in food quality control procedures, all plant-based products. We investigated quantitative content biologically active compounds (anthocyanins chlorogenic acid) microwave-assisted blueberry extracts from 14 different Italian cultivars, using validated high-performance liquid chromatography-photodiode array detector (HPLC-PDA) method routinely instrument...
The Mediterranean fruitfly Ceratitis capitata (medfly) is an invasive agricultural pest of high economic impact and has become emerging model for developing new genetic control strategies as alternative to insecticides. Here, we report the successful adaptation CRISPR-Cas9-based gene disruption in medfly by injecting vitro pre-assembled, solubilized Cas9 ribonucleoprotein complexes (RNPs) loaded with gene-specific single guide RNAs (sgRNA) into early embryos. When targeting eye pigmentation...
The occurrence of fusaproliferin (FP) was investigated in 22 samples preharvest maize ears Fusarium rot, collected 1994 Italy. most frequently recovered species were moniliforme and proliferatum. Chemical analysis by high-perfomance liquid chromatography gas chromatography/mass spectrometry identified FP (up to 500 mg/kg) nine mostly infected F. often found be associated with fumonisin B1 (FB1) 300 beauvericin (BEA) 520 mg/kg). as a natural contaminant its co-occurrence FB1 BEA is reported...
We report two series of novel benzenesulfonamide derivatives acting as effective carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The synthesized compounds were tested against human (h) isoforms hCA I, II, VII, and XII. first compounds, 4-(3-(2-(4-substitued piperazin-1-yl)ethyl)ureido)benzenesulfonamides, showed low nanomolar inhibitory action being less the other isoforms. second series, 2-(4-substitued piperazin-1-yl)-N-(4-sulfamoylphenyl)acetamide derivatives, activity II involved in...