Armando Rossello
University of Pisa
Matrix metalloproteinaseChemical synthesisBiological activityDocking (molecular)EnzymeChemistryIn vitroIn vivoCombinatorial chemistryMatrix metalloproteinase inhibitorLactamHydroxamic acidMoietyEnzyme inhibitorArylAntimicrobialCancer researchBiochemistryMetalloproteinaseStereochemistryPharmacology
249Publications
28H-index
2,325Citations
Publications 233
Newest
#1Roberta Pece (UniGe: University of Genoa)H-Index: 2
#2Sara Tavella (UniGe: University of Genoa)H-Index: 17
Last. Cristina D'ArrigoH-Index: 19
view all 0 authors...
Shedding of A Disintegrin And Metalloproteinases (ADAM10) substrates, like TNFα or CD30, can affect both anti-tumor immune response and antibody-drug-conjugate (ADC)-based immunotherapy. We have published two new ADAM10 inhibitors, LT4 and MN8 able to prevent such shedding in Hodgkin lymphoma (HL). Since tumor tissue architecture deeply influence the outcome of anti-cancer treatments, we set up new three-dimensional (3D) culture systemsto verify whether ADAM10 inhibitors can contribute to, or en...
Source
#2Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
Last. Simone D. Scilabra (ISMETT)H-Index: 8
view all 7 authors...
For decades, disintegrin and metalloproteinase 17 (ADAM17) has been the object of deep investigation. Since its discovery as the tumor necrosis factor convertase, it has been considered a major drug target, especially in the context of inflammatory diseases and cancer. Nevertheless, the development of drugs targeting ADAM17 has been harder than expected. This has generally been due to its multifunctionality, with over 80 different transmembrane proteins other than tumor necrosis factor α (TNF) b...
Source
#1Salvatore Santamaria (Imperial College London)H-Index: 14
#2Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
Last. Josefin Ahnström (Imperial College London)H-Index: 16
view all 10 authors...
ADAMTS-5 is a major protease involved in the turnover of proteoglycans such as aggrecan and versican. Dysregulated aggrecanase activity of ADAMTS-5 has been directly linked to the etiology of osteoarthritis (OA). For this reason, ADAMTS-5 is a pharmaceutical target for the treatment of OA. ADAMTS-5 shares high structural and functional similarities with ADAMTS-4, which makes the design of selective inhibitors particularly challenging. Here we exploited the ADAMTS-5 binding capacity of β-N-acetyl...
1 CitationsSource
#1Susanna Nencetti (UniPi: University of Pisa)H-Index: 18
#2Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
Last. Elisabetta Orlandini (UniPi: University of Pisa)H-Index: 20
view all 14 authors...
Uveal melanoma (UM) represents an aggressive type of cancer and currently, there is no effective treatment for this metastatic disease. In the last years, histone deacetylase inhibitors (HDACIs) have been studied as a possible therapeutic treatment for UM, alone or in association with other chemotherapeutic agents. Here we synthesised a series of new HDACIs based on the SAHA scaffold bearing an (arylidene)aminoxy moiety. Their HDAC inhibitory activity was evaluated on isolated human HDAC1, 3, 6,...
Source
#1Anke Seifert (RWTH Aachen University)H-Index: 3
#2Stefan Düsterhöft (RWTH Aachen University)H-Index: 11
Last. Andreas Ludwig (RWTH Aachen University)H-Index: 63
view all 10 authors...
The metalloproteinase ADAM10 critically contributes to development, inflammation, and cancer and can be controlled by endogenous or synthetic inhibitors. Here, we demonstrate for the first time that loss of proteolytic activity of ADAM10 by either inhibition or loss of function mutations induces removal of the protease from the cell surface and the whole cell. This process is temperature dependent, restricted to mature ADAM10, and associated with an increased internalization, lysosomal degradati...
3 CitationsSource
#1Alessio Nocentini (UniFI: University of Florence)H-Index: 26
#2Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
Last. Claudiu T. Supuran (UniFI: University of Florence)H-Index: 152
view all 8 authors...
The synthesis and carbonic anhydrase (CA; EC 4.2.1.1) activating effects of a series of oxime ether-based amino alcohols towards four human (h) CA isoforms expressed in human brain, hCA I, II, IV a...
1 CitationsSource
#1Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
#2Elisa Nuti (UniPi: University of Pisa)H-Index: 25
Last. Armando Rossello (UniPi: University of Pisa)H-Index: 28
view all 4 authors...
Matrix metalloproteinases (MMPs) and A disintegrin and Metalloproteinase (ADAMs) are zinc-dependent endopeptidases belonging to the metzincin superfamily. Upregulation of metzincin activity is a major feature in many serious pathologies such as cancer, inflammations, and infections. In the last decades, many classes of small molecules have been developed directed to inhibit these enzymes. The principal shortcomings that have hindered clinical development of metzincin inhibitors are low selectivi...
Source
#1Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
#2Elisa Nuti (UniPi: University of Pisa)H-Index: 25
Last. Armando Rossello (UniPi: University of Pisa)H-Index: 28
view all 3 authors...
Carbonic anhydrases (CAs) are metalloenzymes responsible for the reversible hydration of carbon dioxide to bicarbonate, a fundamental reaction involved in various physiological and pathological pro...
1 CitationsSource
#1Doretta Cuffaro (UniPi: University of Pisa)H-Index: 5
#2Felicia D'Andrea (UniPi: University of Pisa)H-Index: 19
Last. Armando Rossello (UniPi: University of Pisa)H-Index: 28
view all 7 authors...
This study reports an ionic liquid (IL) promoted green method to obtain diaryl thioethers useful as key intermediates for the synthesis of matrix metalloproteinase (MMP) inhibitors. The synthetic p...
Source
#1Lidia Ciccone (UniPi: University of Pisa)H-Index: 9
#2Susanna Nencetti (UniPi: University of Pisa)H-Index: 18
Last. Elisabetta Orlandini (UniPi: University of Pisa)H-Index: 20
view all 9 authors...
Abstract Transthyretin (TTR) is a s-sheet-rich homotetrameric protein that transports thyroxine (T4) and retinol both in plasma and in cerebrospinal fluid. TTR also interacts with amyloid-β, playing a protective role in Alzheimer’s disease. Dissociation of the native transthyretin (TTR) tetramer is widely accepted as the critical step in TTR amyloids fibrillogenesis, and is responsible for extracellular deposition of amyloid fibrils. Small molecules, able to bind in T4 binding sites and stabiliz...
Source