Heparanase: a rainbow pharmacological target associated to multiple pathologies including rare diseases

S Rivara, FM Milazzo, G Giannini - Future medicinal chemistry, 2016 - Future Science
In recent years, heparanase has attracted considerable attention as a promising target for
innovative pharmacological applications. Heparanase is a multifaceted protein endowed with …

Kinetic analysis and molecular modeling of the inhibition mechanism of roneparstat (SST0001) on human heparanase

D Pala, S Rivara, M Mor, FM Milazzo, G Roscilli… - …, 2016 - academic.oup.com
Heparanase is a β-d-glucuronidase which cleaves heparan sulfate chains in the extracellular
matrix and on cellular membranes. A dysregulated heparanase activity is intimately …

Synthesis and evaluation of new Hsp90 inhibitors based on a 1, 4, 5-trisubstituted 1, 2, 3-triazole scaffold

…, G Giannini, L Vesci, FM Milazzo… - Journal of Medicinal …, 2014 - ACS Publications
Ruthenium catalyzed 1,3-cycloaddition (click chemistry) of an azido moiety installed on
dihydroxycumene scaffold with differently substituted aryl propiolates gave a new family of 1,4,5-…

[HTML][HTML] Human inhalable antibody fragments neutralizing SARS-CoV-2 variants for COVID-19 therapy

O Minenkova, D Santapaola, FM Milazzo, AM Anastasi… - Molecular Therapy, 2022 - cell.com
As of December 2021, coronavirus disease 2019 (COVID-19), caused by the severe acute
respiratory syndrome coronavirus 2 (SARS-CoV-2), remains a global emergency, and novel …

7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors

…, L Merlini, G Giannini, L Vesci, FM Milazzo… - Bioorganic & Medicinal …, 2014 - Elsevier
7-Azaindole-1-carboxamides were designed as a new class of PARP-1 inhibitors. The
compounds displayed a variable pattern of target inhibition profile that, in part, paralleled the …

ST7612AA1, a thioacetate-ω (γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors

…, G Battistuzzi, D Vignola, FM Milazzo… - Journal of Medicinal …, 2014 - ACS Publications
A systematic study of medicinal chemistry aimed at identifying a new generation of HDAC
inhibitors, through the introduction of a thiol zinc-binding group (ZBG) and of an amide-lactam …

Novel benzazole derivatives endowed with potent antiheparanase activity

…, G Roscilli, G Cassinelli, FM Milazzo… - Journal of medicinal …, 2018 - ACS Publications
Heparanase is the sole mammalian enzyme capable of cleaving glycosaminoglycan
heparan sulfate side chains of heparan sulfate proteoglycans. Its altered activity is intimately …

Novel symmetrical benzazolyl derivatives endowed with potent anti-heparanase activity

…, G Roscilli, G Cassinelli, FM Milazzo… - Journal of medicinal …, 2018 - ACS Publications
Heparanase is the only mammalian endo-β-d-glucuronidase involved in a variety of major
diseases. The up-regulation of heparanase expression increases tumor size, angiogenesis, …

Novel 3, 4-isoxazolediamides as potent inhibitors of chaperone heat shock protein 90

…, L Vesci, M Castorina, FM Milazzo… - Journal of medicinal …, 2011 - ACS Publications
A structural investigation on the isoxazole scaffold led to the discovery of 3,4-isoxazolediamide
compounds endowed with potent Hsp90 inhibitory properties. We have found that …

Isoxazolo (aza) naphthoquinones: A new class of cytotoxic Hsp90 inhibitors

…, S Penco, L Vesci, M Castorina, FM Milazzo… - European journal of …, 2012 - Elsevier
A series of 3-aryl-naphtho[2,3–d]isoxazole-4,9-diones and some of their 6-aza analogues
were synthesized and found to inhibit the heat shock protein 90 (Hsp90). The compounds …