Marco Macchia

University of Pisa

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Document Type

Co-Authors

Filippo Minutolo

University of Pisa

126

Simone Bertini

University of Pisa

107

Adriano Martinelli

University of Pisa

Tiziano Tuccinardi

University of Pisa

Clementina Manera

University of Pisa

Armando Rossello

University of Pisa

Carlotta Granchi

University of Pisa

Maria Digiacomo

University of Pisa

Elisabetta Orlandini

University of Pisa

Simona Rapposelli

University of Pisa

Cooperative Institutions

University of Pisa

336

University of Milan

160

Istituti di Ricovero e Cura a Carattere Scientifico

131

University of Rome Tor Vergata

Istituto Nazionale per le Malattie Infettive Lazzaro Spallanzani

University of Padua

University of Florence

National Research Council

University of Siena

University of Naples Federico II

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BACE-1 inhibitory activities of new substituted diphenyl-methylenyl-piperazines

V. Asso Elisa Ghilardi Simone Bertini Maria Digiacomo Carlotta Granchi

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Ultrastructural and Biochemical Evidence of Apoptosis Induced by a Novel Inhibitor of Protein Geranylgeranylation in Human MIA PaCa-2 Pancreatic Cancer Cells

Ultrastructural Pathology (1998)

Marco Gesi Antonio Pellegrini Paola Soldani Paola Lenzi Antonio Paparelli

Analogs of geranylgeranyl diphosphate (GGdP) have been demonstrated to inhibit the geranylgeranylation of proteins, producing cytotoxic activity in human prostate cancer cells. A detailed study is reported on the programmed cell death in vitro of human exocrine pancreas cancer cells (MIA PaCa-2) induced by the most active compound of this series of geranylgeranylation inhibitors, the dipotassium salt of (E,E,E)[2-oxo-2-[[(3,7,11,15-tetramethyl-2, 6,10,14-hexadecatetraenyl)-oxy]amino]ethyl] phosphonic acid (BAL 9504), using transmission and scanning electron microscopy (SEM). The results show that, after 72 h of treatment with BAL 9504, 25 microM, most MIA PaCa-2 cells display the typical morphological features of apoptosis, including condensation of nuclear chromatin, dilation of endoplasmic reticulum, and fragmentation of both nucleus and cytoplasm, giving rise to small membrane-bound vesicles (apoptotic bodies); surface protrusions and blebs are well demonstrated by SEM. The electrophoresis showed the presence of various bands corresponding to fragmented DNA of 180 base pairs, or multiples of this length, thus indicating that BAL 9504 effectively induces apoptosis. The present study provides the first evidence that inhibition of protein geranylgeranylation produces apoptosis in human MIA PaCa-2 exocrine pancreas cancer cells.

Geranylgeranylation

Fragmentation

Apoptotic body

10.3109/01913129809033477

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Citations (10)

La società turnaround, ossia per la patrimonializzazione e la ristrutturazione delle imprese in crisi

Rivista giuridica del Mezzogiorno (2015)

Marco Macchia

10.1444/82381

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New biphenylic derivatives as CB2 receptor selective ligands

Simone Bertini Chiara Arena S. Del Carlo Alessia Ligresti Giuseppe Saccomanni

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I rapporti tra burocrazia italiana e burocrazia europea

Analisi Giuridica dell'Economia (2020)

Marco Macchia

10.1433/98443

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Synthesis, platelet anti-aggregating activity and anti-inflammatory activity of a series of beta-aminoxypropionic acids.

PubMed (1994)

Marco Macchia Elisabetta Orlandini Armando Rossello Simone Bertini Giulio Soldani

Malondialdehyde

Anti-inflammatory

Carrageenan

Moiety

Adenosine diphosphate

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Citations (2)

Aminobenzothiazoles as beta-Selective Estrogen Receptor Ligands

Filippo Minutolo Simone Bertini Simona Rapposelli K.E. Carlson John A. Katzenellenbogen

BETA (programming language)

Estrogen receptor beta

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Synthesis of piperidine derivatives as potential anti Alzheimer agents

V. Asso Elisa Ghilardi Simone Bertini Filippo Minutolo Salvatore La Rosa

Piperidine

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Structural Evolutions of Salicylaldoximes as Selective Agonists for Estrogen Receptor β

Journal of Medicinal Chemistry (2009)

Filippo Minutolo Simone Bertini Carlotta Granchi T. Marchitiello Giovanni Prota

The bioisosteric replacement of the phenol ring, a signature functional group of most estrogen receptor (ER) ligands, with a hydrogen-bonded pseudocyclic ring, led to the development of a novel class of nonsteroidal ER-ligands based on a salicylaldoxime template. A series of structural modifications were applied to selected molecules belonging to the monoaryl-salicylaldoxime chemical class in an attempt to improve further their ERβ-selective receptor affinity and agonist properties. Among several modifications, the best results were obtained by the simultaneous introduction of a meta-fluorine atom into the para-hydroxyphenyl substituent present in the 4-position of salicylaldoxime, together with the insertion of a chloro group in the 3-position of the central scaffold. The resulting compound showed the best affinity (Ki = 7.1 nM) and selectivity for ERβ over ERα. Moreover, in transcription assays, it proved to be a selective and potent ERβ-full agonist with an EC50 of 4.8 nM.

10.1021/jm801458t

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Citations (41)

High performance liquid chromatographic determination of thalidomide in patients affected by hepatocellular carcinoma

Journal of Pharmaceutical and Biomedical Analysis (2008)

Giuseppe Saccomanni V. Turini Clementina Manera Giorgio Placanica Emanuela Omodeo Salè

Phenacetin

10.1016/j.jpba.2008.01.003

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Citations (6)