FTase inhibitors and cancer: prospects for use in targeted therapies

M Xia, L Yu, Z Yan, Y Wang, L Zhang, G Miao… - Medicinal Chemistry …, 2024 - Springer
Farnesyltransferase (FTase) is a key enzyme that catalyzes the farnesylation of Ras protein.
It is used to bind RAS protein to plasma membrane to complete signal transduction. Ras has …

Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling

M Shen, P Pan, Y Li, D Li, H Yu, T Hou - Drug Discovery Today, 2015 - Elsevier
Highlights•Structures and therapeutic importance of FTase and GGTase-1 are briefly
outlined.•Available inhibitors of FTase and GGTase-1 are systematically …

Anticancer activity of farnesyltransferase and geranylgeranyltransferase I inhibitors: prospects for drug development

SM Sebti, AD Hamilton - Expert Opinion on Investigational Drugs, 1997 - Taylor & Francis
Inhibition of Farnesyltransferase (FTase) has been thoroughly investigated as a strategy to
discover novel anticancer drugs because the oncoprotein Ras, requires farnesylation for its …

The recent development of farnesyltransferase inhibitors as anticancer and antimalarial agents

Y Shen, S Qiang, S Ma - Mini Reviews in Medicinal Chemistry, 2015 - ingentaconnect.com
Cancer is a serious disease characterized by the uncontrolled growth division of cells, and
nowadays it remains a significant challenge for the medical field. Malaria is an infectious …

Farnesyltransferase inhibitors: potential role in the treatment of cancer

AD Cox - Drugs, 2001 - Springer
New targets for drug discovery have been identified rapidly as a result of the many recent
and rapid advances in the understanding of signal transduction pathways that contribute to …

An overview on natural farnesyltransferase inhibitors for efficient cancer therapy

X Dai, Y Sun, T Zhang, Y Ming… - Journal of Enzyme …, 2020 - Taylor & Francis
As one of the world's five terminally ills, tumours can cause important genetic dysfunction.
However, some current medicines for tumours usually have strong toxic side effects and are …

[HTML][HTML] A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics

G Porcu, C Wilson, D Di Giandomenico… - Molecular Cancer, 2010 - Springer
Abstract Background Farnesyltransferase inhibitors (FTIs) are anticancer agents developed
to inhibit Ras oncoprotein activities. FTIs of different chemical structure act via a conserved …

Farnesyltransferase inhibitors: a detailed chemical view on an elusive biological problem

SF Sousa, PA Fernandes… - Current medicinal …, 2008 - ingentaconnect.com
Farnesyltransferase (FTase) is a zinc enzyme that has been the subject of particular
attention in anti-cancer research. This enzyme promotes the addition of a farnesyl group …

Farnesyltransferase inhibitors: overview of their action and role in solid malignancy therapy

S Margaritora, A Cesario, V Porziella… - Letters in Drug …, 2005 - ingentaconnect.com
Nowadays, molecular targeted cancer therapies represent the core of translational research.
Protein prenylation [covalent binding of either a farnesyl (15-C) or a geranylgeranyl (20-C) …

Discovery of novel inhibitors for human farnesyltransferase (h FTase) via structure-based virtual screening

X Yu, X Zhao, L Zhu, C Zou, X Liu, Z Zhao, J Huang… - …, 2013 - pubs.rsc.org
In this study, 22 novel hFTase inhibitors containing 18 scaffolds were identified with IC50
values ranging from 0.0119 to 13.35 μM by structure-based virtual screening, and …