Search Results - "Luisi, Grazia"
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Anti-Oxidant and Tyrosinase Inhibitory In Vitro Activity of Amino Acids and Small Peptides: New Hints for the Multifaceted Treatment of Neurologic and Metabolic Disfunctions
Published in Antioxidants (26-12-2018)“…Oxidative damage is among the factors associated with the onset of chronic pathologies, such as neurodegenerative and metabolic diseases. Several classes of…”
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Coumarin-Based Dual Inhibitors of Human Carbonic Anhydrases and Monoamine Oxidases Featuring Amino Acyl and ( Pseudo )-Dipeptidyl Appendages: In Vitro and Computational Studies
Published in Molecules (Basel, Switzerland) (01-11-2022)“…The involvement of human carbonic anhydrase (hCA) IX/XII in the pathogenesis and progression of many types of cancer is well acknowledged, and more recently…”
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3
Activation of β- and γ-carbonic anhydrases from pathogenic bacteria with tripeptides
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…Six tripeptides incorporating acidic amino acid residues were prepared for investigation as activators of β- and γ-carbonic anhydrases (CAs, EC 4.2.1.1) from…”
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4
Dual targeting of cancer-related human matrix metalloproteinases and carbonic anhydrases by chiral N-(biarylsulfonyl)-phosphonic acids
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2017)“…A series of nanomolar phosphonate matrix metalloproteinase (MPP) inhibitors was tested for inhibitory activity against a panel of selected human carbonic…”
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5
Biofilm and Quorum Sensing inhibitors: the road so far
Published in Expert opinion on therapeutic patents (01-12-2020)“…Biofilm is a complex aggregation of microorganisms characterized by the presence of a dynamic, adhesive and protective extracellular matrix composed of…”
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6
Discovery of arginine-containing tripeptides as a new class of pancreatic lipase inhibitors
Published in Future medicinal chemistry (01-01-2019)“…The inhibition of pancreatic lipase (PL) represents one of the most promising strategies in the search for novel antiobesity drugs. We propose here a…”
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7
Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors
Published in Bioorganic & medicinal chemistry (01-02-2020)“…[Display omitted] Matrix metalloproteinases (MMPs) are a large family of zinc-dependent endoproteases known to exert multiple regulatory roles in tumor…”
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8
Bioactive compounds of Crocus sativus L. and their semi-synthetic derivatives as promising anti-Helicobacter pylori, anti-malarial and anti-leishmanial agents
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2015)“…Crocus sativus L. is known in herbal medicine for the various pharmacological effects of its components, but no data are found in literature about its…”
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9
Nitrobenzoxadiazole-based GSTP1-1 inhibitors containing the full peptidyl moiety of (pseudo)glutathione
Published in Journal of enzyme inhibition and medicinal chemistry (01-11-2016)“…The inhibition of glutathione S-transferase P1-1 (GSTP1-1) is a sound strategy to overcome drug resistance in oncology practice. The nitrobenzoxadiazolyl (NBD)…”
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10
Fluorescent-labeled bioconjugates of the opioid peptides biphalin and DPDPE incorporating fluorescein-maleimide linkers
Published in Future medicinal chemistry (01-06-2017)“…The conjugation of fluorescent labels to opioid peptides is an extremely challenging task, which needs to be overcome to create new classes of probes for…”
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11
Hybrid peptides endomorphin-2/DAMGO: Design, synthesis and biological evaluation
Published in European journal of medicinal chemistry (01-10-2013)“…Endomorphin-2 [Tyr-Pro-Phe-Phe-NH2] and DAMGO [Tyr-D-Ala-Gly-(N–Me)Phe-Gly-ol] are natural (EM2) and synthetic (DAMGO) opioid peptides both selective for μ…”
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12
Biochemical and pharmacological investigation of novel nociceptin/OFQ analogues and N/OFQ-RYYRIK hybrid peptides
Published in Peptides (New York, N.Y. : 1980) (01-02-2019)“…•Hybrid peptides are research tools for GPCRs and their interacting complexes.•Nine new ligands were constructed from Dooley peptide RYYRIK and nociceptin…”
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13
Novel Cyclic Biphalin Analogues by Ruthenium-Catalyzed Ring Closing Metathesis: in Vivo and in Vitro Biological Profile
Published in ACS medicinal chemistry letters (11-04-2019)“…In this work we report the application of the ring-closing metathesis (RCM) to the preparation of two cyclic olefin-bridged analogues of biphalin…”
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14
Ac-tLeu-Asp-H is the minimal and highly effective human caspase-3 inhibitor: biological and in silico studies
Published in Amino acids (01-01-2015)“…Caspase-3 displays a pivotal role as an executioner of apoptosis, hydrolyzing several proteins including the nuclear enzyme poly(ADP-ribose)polymerase (PARP)…”
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15
Synthesis and neuromodulatory effects of TRH-related peptides: inhibitory activity on catecholamine release in vitro
Published in Pharmacological reports (2013)“…A detailed comprehension of central mechanisms underlying feeding behavior holds considerable promise for the treatment of alimentary disorders In order to…”
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16
Human caspase-3 inhibition by Z- tLeu-Asp-H: tLeu(P 2) counterbalances Asp(P 4) and Glu(P 3) specific inhibitor truncation
Published in Biochemical and biophysical research communications (19-12-2008)“…Caspase-3 is responsible for the cleavage of several proteins including the nuclear enzyme poly(ADP-ribose) polymerase (PARP). Designed on the cleavage site of…”
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17
Transition state isosteres of the gamma -glutamyl peptide bond hydrolysis: synthesis and characterization of the gradient [CH2NH] pseudopeptide analogue of glutathione
Published in Journal of peptide science (01-02-2004)“…The fully deprotected glutathione analogue containing the aminomethylene unit as transition state isostere of the -Glu-Cys peptide bond was synthesized for the…”
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18
Transition state isosteres of the γ-glutamyl peptide bond hydrolysis: synthesis and characterization of the ψ[CH2NH] pseudopeptide analogue of glutathione
Published in Journal of peptide science (01-02-2004)“…The fully deprotected glutathione analogue containing the aminomethylene unit as transition state isostere of the γ‐Glu‐Cys peptide bond was synthesized for…”
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Synthesis and preliminary pharmacological evaluation of 5-Hydroxy- and 5,6-dihydroxy-1,2,3,7,12,12a-hexahydrobenzo[5,6]cyclohepta[1,2,3- ij]isoquinoline derivatives as dopamine receptor ligands
Published in Bioorganic & medicinal chemistry (01-06-2001)“…A series of 5-hydroxy- and 5,6-dihydroxy-1,2,3,7,12,12a-hexahydrobenzo[5,6]cyclohepta[1,2,3- ij]isoquinoline derivatives ( 5a– e and 6a– e) were synthesized as…”
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20
Design and synthesis of glutathione analogues
Published in Farmaco (Società chimica italiana : 1989) (30-12-1998)“…This review reports recent structural modifications (since 1989) performed on the glutathione molecule both in the oxidized and reduced form. Relevant chemical…”
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