Giuseppe La Regina

Pubblicazioni

Titolo Pubblicato in Anno
3-Aroyl-1,4-diarylpyrroles inhibit chronic myeloid leukemia cell growth through an interaction with tubulin ACS MEDICINAL CHEMISTRY LETTERS 2017
Violaceina: un pigmento prodotto dal batterio Janthinobacterium lividum ad attività antitumorale Natural Products: tecniche analitiche e nuove tendenze nel mondo dei prodotti naturali 2017
Chiral indolylarylsulfone non-nucleoside reverse transcriptase inhibitors as new potent and broad spectrum anti-HIV-1 agents JOURNAL OF MEDICINAL CHEMISTRY 2017
Inhibition of dengue virus replication by novel inhibitors of RNA-dependent RNA polymerase and protease activities JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 2017
Computer-aided identification and lead optimization of dual murine double minute 2 and 4 binders: structure-activity relationship studies and pharmacological activity JOURNAL OF MEDICINAL CHEMISTRY 2017
Inhibition of dengue virus by novel inhibitors of RNA-dependent RNA polymerase and protease activity Program and Abstracts 2017
Drug design and synthesis of new indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors Program and Abstracts 2017
Violacein, an indole-derived purple-colored natural pigment produced by Janthinobacterium lividum, inhibits the growth of head and neck carcinoma cell lines both in vitro and in vivo TUMOR BIOLOGY 2016
New Inhibitors of Dengue Virus Replication Abstract eBook 2016
New Inhibitors of indoleamine 2,3-dioxygenase 1: molecular modelling studies, synthesis and biological evaluation Abstract eBook 2016
New inhibitors of indoleamine 2,3-dioxygenase 1: molecular modeling studies, synthesis, and biological evaluation JOURNAL OF MEDICINAL CHEMISTRY 2016
Structure-based virtual screening to get new scaffold inhibitors of the Ser/Thr protein kinase PknB from Mycobacterium tuberculosis LETTERS IN DRUG DESIGN & DISCOVERY 2016
New 1-phenyl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides inhibit hepatitis C virus replication via suppression of cyclooxygenase-2 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 2015
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents JOURNAL OF MEDICINAL CHEMISTRY 2015
Pharmacological folding chaperones act as allosteric ligands of Frizzled4 NATURE CHEMICAL BIOLOGY 2015
Kinetic characterization of 4,4'-biphenylsulfonamides as selective non-zinc binding MMP inhibitors JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 2015
Discovery of 1,1'-biiphenyl-4-sulfonamides as a new class of potent and selective carbonic anhydrase XIV inhibitors JOURNAL OF MEDICINAL CHEMISTRY 2015
Endogenous vs exogenous allosteric modulators in GPCRs: a dispute for shuttling CB1 among different membrane microenvironments SCIENTIFIC REPORTS 2015
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer JOURNAL OF MEDICINAL CHEMISTRY 2015
Poster: "In vivo selection of JARID histone demethylases inhibitors and their use to enlighten the biological role of these enzymes in yeast and mammalian cells with focus on transcriptional regulation” Abstracts of the 27th International Conference on Yeast Genetics and Molecular Biology 2015

ERC

  • LS1_13
  • PE5_17
  • PE5_18

KET

  • Life-science technologies & biotechnologies

Interessi di ricerca

Progettazione, sintesi e sviluppo di agenti anti-infettivi (HIV-1, Rhinovirus, virus dell’epatite C, virus Dengue, Mycobacterium tuberculosis, Candida albicans), anti-tumorali (tubulina, apoptosi, istone demetilasi, metalloproteinasi di matrice, membri della famiglia BCL-2, Frizzled4, anidrasi carbonica, indolamina 2,3-diossigenasi 1, MDM2/MDM4, NHERF1, beta-catenina) e attivi sul sistema nervoso centrale (monoammino ossidasi, sistema endocannabinoide, glicogeno sintasi chinasi 3 beta); sintesi microonde-assistita; studi di modellistica molecolare.

Keywords

drug design and discovery
Anti-Infective Agents
anticancer agent

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