Targeting RAS signalling pathways in cancer therapy

J Downward - Nature reviews cancer, 2003 - nature.com
The RAS proteins control signalling pathways that are key regulators of several aspects of
normal cell growth and malignant transformation. They are aberrant in most human tumours …

Targeting the MAPK pathway in melanoma: why some approaches succeed and other fail

GS Inamdar, SRV Madhunapantula… - Biochemical …, 2010 - Elsevier
The Mitogen Activated Protein Kinase (MAPK) pathway plays a key role in melanoma
development making it an important therapeutic target. In normal cells, the tightly regulated …

Structural basis for the autoinhibition of c-Abl tyrosine kinase

B Nagar, O Hantschel, MA Young, K Scheffzek… - Cell, 2003 - cell.com
Abstract c-Abl is normally regulated by an autoinhibitory mechanism, the disruption of which
leads to chronic myelogenous leukemia. The details of this mechanism have been elusive …

Thematic review series: lipid posttranslational modifications. Farnesyl transferase inhibitors

AD Basso, P Kirschmeier, WR Bishop - Journal of lipid research, 2006 - ASBMB
Some proteins undergo posttranslational modification by the addition of an isoprenyl lipid
(farnesyl-or geranylgeranyl-isoprenoid) to a cysteine residue proximal to the C terminus …

Isoprenoids and protein prenylation: implications in the pathogenesis and therapeutic intervention of Alzheimer's disease

A Jeong, KF Suazo, WG Wood… - Critical reviews in …, 2018 - Taylor & Francis
The mevalonate–isoprenoid–cholesterol biosynthesis pathway plays a key role in human
health and disease. The importance of this pathway is underscored by the discovery that two …

Development of farnesyl transferase inhibitors: a review

NMGM Appels, JH Beijnen, JHM Schellens - The oncologist, 2005 - academic.oup.com
Abstract Learning Objectives After completing this course, the reader will be able to:
Describe the potential mechanisms by which farnesyl transferases inhibit tumor growth …

Effects of statins and farnesyltransferase inhibitors on the development and progression of cancer

MR Graaf, DJ Richel, CJF van Noorden… - Cancer treatment …, 2004 - Elsevier
Statins (3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors–HMG-CoA reductase
inhibitors) have been approved for the treatment of lipid disorders. Recently, in vivo studies …

Targeting the RAS oncogene

A Takashima, DV Faller - Expert opinion on therapeutic targets, 2013 - Taylor & Francis
Introduction: The Ras proteins (K-Ras, N-Ras, and H-Ras) are GTPases that function as
molecular switches for a variety of critical cellular activities and their function is tightly and …

Targeting mutant KRAS for anticancer therapeutics: a review of novel small molecule modulators

Y Wang, CE Kaiser, B Frett, H Li - Journal of medicinal chemistry, 2013 - ACS Publications
The RAS proteins play a role in cell differentiation, proliferation, and survival. Aberrant RAS
signaling has been found to play a role in 30% of all cancers. KRAS, a key member of the …

Searching for the elusive targets of farnesyltransferase inhibitors

SM Sebti, CJ Der - Nature Reviews Cancer, 2003 - nature.com
Abstract Farnesyltransferase (FTase) inhibitors (FTIs) were developed originally as anti-RAS
compounds and novel target-based drugs for cancer treatment. The analyses of FTIs …