Research Topics
| Luca GentilucciSummaryAffiliation: University of Bologna Country: Italy Publications
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Detail Information
Publications
Cyclopeptide analogs for generating new molecular and 3D diversityLuca Gentilucci
Department of Chemistry G Ciamician, University of Bologna, 40126 Bologna, Italy
Comb Chem High Throughput Screen 12:929-39. 2009..Finally, we discuss the conformational features of such molecules as turn mimics. The comparison suggests that the retro-inverso modification allows a higher degree of three-dimensional diversity than normal peptides...- Molecular docking of opiates and opioid peptides, a tool for the design of selective agonists and antagonists, and for the investigation of atypical ligand-receptor interactionsL Gentilucci
Department of Chemistry G Ciamician, University of Bologna, Via Selmi 2, 40126, Bologna, Italy
Curr Med Chem 19:1587-601. 2012..For the atypical structure of these compounds, the docking proved to be essential to disclose how they interact with and activate the receptors... - Re-discussion of the importance of ionic interactions in stabilizing ligand-opioid receptor complex and in activating signal transductionLuca Gentilucci
Dipartimento di Chimica G Ciamician, Universita degli Studi di Bologna, Via Selmi 2, 40126 Bologna, Italy
Curr Drug Targets 8:185-96. 2007..In particular, they strengthen the evidence that ORs can bind ligands via diverse binding modes, and in some cases an electrostatic interaction is not an absolute requirement... - Peptides and peptidomimetics in medicine, surgery and biotechnologyLuca Gentilucci
Dept of Chemistry G Ciamician, Universita degli Studi di Bologna, Via Selmi 2, 40126, Bologna, Italy
Curr Med Chem 13:2449-66. 2006..Finally, peptide-based biomaterials can find applications in bio-nanotechnology for bio-microchips, peptide nanorods and nanotubes, bio-sensors, bio-electronic devices, and peptide-metal wires... - A novel family of minimal PMRI cyclic peptides as versatile scaffolds for generating new molecular topologyLuca Gentilucci
Department of Chemistry G Ciamician, Universita degli Studi di Bologna, Via Selmi 2, 40126 Bologna, Italy
Med Chem 2:395-400. 2006..These scaffolds have been designed to permit easy introduction in a combinatorial fashion of a range of pharmacophores that possess a diversity of structure, function, and 3D disposition... - Investigation of the interaction between the atypical agonist c[YpwFG] and MORLuca Gentilucci
Dipartimento di Chimica G Ciamician, Universita degli Studi di Bologna, Italy
FEBS J 275:2315-37. 2008.... - Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimeticsLuca Gentilucci
Department of Chemistry G Ciamician, Universita degli Studi di Bologna, Via Selmi 2, 40126 Bologna, Italy
J Med Chem 53:106-18. 2010.... - Chemical modifications designed to improve peptide stability: incorporation of non-natural amino acids, pseudo-peptide bonds, and cyclizationLuca Gentilucci
Department of Chemistry G Ciamician, Universita degli Studi di Bologna, Via Selmi 2, 40126 Bologna, Italy
Curr Pharm Des 16:3185-203. 2010..This review focuses on modified peptides in which the peptide character is still preponderant, with particular emphasis on the chemical methodologies utilized to introduce the modifications... - The inverse type?II ?-turn on D-Trp-Phe, a pharmacophoric motif for MOR agonistsLuca Gentilucci
Department of Chemistry G Ciamician, University of Bologna, Via Selmi 2, 40126 Bologna, Italy
ChemMedChem 6:1640-53. 2011.... - Topological exploration of cyclic endomorphin-1 analogues, structurally defined models for investigating the bioactive conformation of MOR agonistsLuca Gentilucci
Dipartimento di Chimica G Ciamician, Via Selmi 2, Universita degli Studi di Bologna, 40126 Bologna, Italy
Protein Pept Lett 14:51-6. 2007.... - Development of isoxazoline-containing peptidomimetics as dual ?v?3 and ?5?1 integrin ligandsAlessandra Tolomelli
Department of Chemistry G Ciamician, University of Bologna, Via Selmi 2, 40126 Bologna, Italy
ChemMedChem 6:2264-72. 2011..The molecular basis of the observed inhibitory activity was suggested on the results of docking experiments... - Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffoldsFides Benfatti
Dipartimento di Chimica G Ciamician, Universita di Bologna, Via Selmi 2, 40126 Bologna, Italy
Bioorg Med Chem 15:7380-90. 2007..The synthesis and the antiadhesion activity of a small library of peptidomimetics capable to recognize alpha(v)beta(3) and alpha(5)beta(1) integrins has been herein reported... - Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimeticsLuca Gentilucci
Department of Chemistry G Ciamician, Universita degli Studi di Bologna, Via Selmi 2, 40126 Bologna, Italy
Bioorg Med Chem Lett 17:2329-33. 2007..In particular, peptides 4 and 8 showed an IC(50) in the 10(-8)M range. Despite the linear structure, the peptides tend to adopt a folded conformation in a polar environment... - Stability against enzymatic hydrolysis of endomorphin-1 analogues containing beta-prolineGiuliana Cardillo
Dipartimento di Chimica G Ciamician, Universita di Bologna, Via Selmi 2, 40126 Bologna, Italy
Org Biomol Chem 1:1498-502. 2003..The presence of beta-proline alone is sufficient to confer good resistance against the hydrolysis of the biologically strategic Pro-Trp bond... - Synthesis and conformational analysis of cyclotetrapeptide mimetic beta-turn templates and validation as 3D scaffoldsLuca Gentilucci
Department of Chemistry G Ciamician, University of Bologna, Italy
ChemMedChem 4:517-23. 2009..The peptide mimetics can be regarded as 3D scaffolds for designing molecules with a predictable display of the pharmacophores. We used the models for testing novel RGD analogues as alpha(v)beta(3)-integrin receptor antagonists... - Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-]Giuliana Cardillo
Dipartimento di Chimica G Ciamician and CSFM, Via Selmi 2, Universita di Bologna, 40126 Bologna, Italy
J Med Chem 47:5198-203. 2004.... - Conformational analysis and mu-opioid receptor affinity of short peptides, endomorphin models in a low polarity solventGiuliana Cardillo
Dipartimento di Chimica G Ciamician, C S F M, Universita di Bologna, Via Selmi 2, 40126 Bologna, Italy
Org Biomol Chem 1:3010-4. 2003..To test the reliability of the peptides as endomorphin conformational models, we measured the affinities for mu-receptors labelled with [3H]-DAMGO. In particular, Cbz-Pro-Trp-PheNH2 displayed a nanomolar affinity... - Synthesis and biological evaluation of unprecedented classes of spiro-beta-lactams and azido-beta-lactams as acyl-CoA:cholesterol acyltransferase inhibitorsFides Benfatti
Dipartimento di Chimica G Ciamician, Universita di Bologna, Via Selmi 2, 40126 Bologna, Italy
Bioorg Med Chem Lett 17:1946-50. 2007..The potential of these particular beta-lactams as biologically active compounds has been confirmed by the results obtained in ACAT inhibition assays... - A straightforward route to enantiopure 2-substituted-3,4-dehydro-?-proline via ring closing metathesisAlessandra Tolomelli
Department of Chemistry, G Ciamician, University of Bologna, Via Selmi 2, 40126, Bologna, Italy
Amino Acids 41:575-86. 2011..Moreover, in view of a future application of these dehydro-?-amino acids as central core of peptidomimetics, the malonate chain was also used to protect nitrogen prior to RCM... - Peripheral antinociceptive effects of the cyclic endomorphin-1 analog c[YpwFG] in a mouse visceral pain modelAndrea Bedini
Department of Pharmacology, University of Bologna, Irnerio 48, 4126 Bologna, Italy
Peptides 31:2135-40. 2010..In conclusion, c[YpwFG] displays sufficient metabolic stability to be effective after peripheral administration and demonstrates the therapeutic potential of endomorphin derivatives as novel analgesic agents to control visceral pain... - New trends in the development of opioid peptide analogues as advanced remedies for pain reliefLuca Gentilucci
Dipartimento di Chimica G Ciamician, Via Selmi 2, Universita degli Studi di Bologna, 40126 Bologna, Italy
Curr Top Med Chem 4:19-38. 2004.... - Recent advances in the investigation of the bioactive conformation of peptides active at the micro-opioid receptor. conformational analysis of endomorphinsLuca Gentilucci
Dipartimento di Chimica G Ciamician, Via Selmi 2, Universita degli Studi di Bologna, 40126 Bologna, Italy
Curr Top Med Chem 4:105-21. 2004.... - Synthesis of dehydro-beta-amino esters via highly regioselective amination of allylic carbonatesFides Benfatti
Department of Chemistry G Ciamician, University of Bologna, Bologna, Italy
Org Lett 10:2425-8. 2008.... - Antinociception by a peripherally administered novel endomorphin-1 analogue containing beta-prolineSanti Spampinato
Department of Pharmacology, University of Bologna, Irnerio 48, 40126 Bologna, Italy
Eur J Pharmacol 469:89-95. 2003..This compound will be extremely useful for exploring the pharmacological profile of endomorphins in vivo and confirms the potential therapeutic interest of endomorphin derivatives as novel analgesic agents... - Synthesis and biological evaluation of azido- and aziridino-hydroxyl-beta-lactams through stereo- and regioselective epoxide ring openingFides Benfatti
Department of Chemistry G. Ciamician, University of Bologna, Via Selmi 2, 40126 Bologna, Italy
J Org Chem 71:9229-32. 2006..The straightforwardness of the procedure makes this strategy useful for the synthesis of potentially bioactive compounds. Some selected examples showed promising activity in acyl CoA-cholesterol acyltransferase inhibition assays... - Highly diastereoselective allylic azide formation and isomerization. Synthesis of 3(2'-amino)-beta-lactamsGiuliana Cardillo
Department of Chemistry G Ciamician, University of Bologna, Via Selmi 2, 40126 Bologna, Italy
Org Lett 7:533-6. 2005..reaction: see text].. - Endomorphin-1 analogues containing beta-proline are mu-opioid receptor agonists and display enhanced enzymatic hydrolysis resistanceGiuliana Cardillo
Dipartimento di Chimica G. Ciamician, Via Selmi 2, , 40126-Bologna, Italy
J Med Chem 45:2571-8. 2002..These features suggest that this novel class of endomorphin-1 analogues may represent suitable candidates for the in vivo investigation as potential mu-opioid receptor agonists... - Expedient synthesis of pseudo-Pro-containing peptides: towards constrained peptidomimetics and foldamersRossella De Marco
Department of Chemistry G Ciamician, University of Bologna, Via Selmi 2, 40126 Bologna, Italy
Org Biomol Chem 10:2307-17. 2012....