Work

Discovery of First-in-Class Carbonic Anhydrase/Histone Deacetylase Dual Inhibitors with Antiproliferative Activity in Cancer Cells

Year: 2025

Type: article

Abstract: evidence supporting a new class of compounds capable of independently targeting the tumor-associated human (h) carbonic anhydrase (CA; EC 4.2.1.1) and histone deacetylase (HDAC; EC 3.5.1.98) isoforms as first-in-class agents endowed with enhanced antiproliferative effects and safety profiles when compared to their constitutive counterparts as well as to clinically used drugs. The binding modes of both the CA- and HDAC-directed moieties were investigated through X-ray and molecular modeling experiments, respectively, thus delivering detailed Structure-Activity Relationship (SAR) knowledge.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.5c01788

Authors: Murat Bozdag, Nabil Mroweh, Alessia Raucci, Andrea Angeli, Silvia Peppicelli, Alessio Biagioni, Lido Calorini, Daniela Trisciuoglio, Rino Ragno, Roberta Astolfi, Lidia Giuliani, Clemens Zwergel, Sergio Valente, Elena Andreucci, Fabrizio Carta, Antonello Mai, Claudiu T. Supuran

Institutions: University of Florence, Sapienza University of Rome, Institute of Molecular Biology and Pathology, National Research Council, Istituto Pasteur

Language: English

Topic: Enzyme function and inhibition

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,500

Funders: European Commission, Ministero dell’Istruzione, dell’Università e della Ricerca, Fondazione Umberto Veronesi, Associazione Italiana per la Ricerca sul Cancro, Accademia Nazionale dei Lincei, NextGenerationEU

Awards: G3157763019, G4917008562, G5023805214, G8076786994, G850769058

OpenAlex ID: W4415629191

FWCI: 1.278

Cites: 77

Cited by: 5

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