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Substrate Competitive Inhibitors of IGF-1 Receptor Kinase

Biochemistry, 2000
IGF-1 and its receptor play a pivotal role in many cancers, and therefore, IGF-1R is an attractive target for the design of inhibitors. In this communication, we report on a number of lead compounds for inhibitors of the isolated IGF-1R kinase. The search for these compounds utilized two novel in vitro assays and was aided by the knowledge of the three-
G, Blum, A, Gazit, A, Levitzki
openaire   +2 more sources

Insulin is a potent myeloma cell growth factor through insulin/IGF-1 hybrid receptor activation

open access: yesLeukemia, 2010
International audienceInsulin and insulin growth factor type 1 (IGF-1) and their receptors are closely related molecules, but both factors bind to the receptor of the other one with a weak affinity.
Laure Vincent   +2 more
exaly   +2 more sources

An Arrestin Role at the IGF-1 Receptor

Science's STKE, 2004
Povsic et al. investigated the role of β-arrestins in the activation of phosphatidylinositol 3-kinase (PI3K) by insulin-like growth factor 1 (IGF-1) and discovered that, unexpectedly, this involved a mechanism independent of the tyrosine kinase activity of the IGF-1 receptor.
openaire   +1 more source

IGF-1 levels and polymorphisms in the IGF-1 receptor are associated with response to antidepressant treatment

Experimental and Clinical Endocrinology & Diabetes, 2014
Objective: In psychiatric diseases such as depression, several neuroendocrine disturbances occur. Recent findings suggest that insulin like growth factor (IGF)-1 might be involved in depressive disorders1. In our study, we analyzed IGF-1 levels and polymorphisms in IGF-1 related genes for antidepressant response.
A Kopczak   +4 more
openaire   +1 more source

Insulin and IGF-1 receptor trafficking and signalling.

Novartis Foundation symposium, 2004
Receptor-mediated endocytosis governs the entry of receptors inside the cells. In the case of signalling receptors, e.g. tyrosine kinase receptors, the process is ligand-dependent and includes a series of surface events which determines the specificity of the internalization process and the activation of distinct signal transduction pathways.
Foti, Michelangelo   +3 more
openaire   +2 more sources

The IGF-1-IGF-1 Receptor System Modulates Myocyte Proliferation but Not Myocyte Cellular Hypertrophy in Vitro

Experimental Cell Research, 1994
In preliminary experiments it was established that the hypertrophic and hyperplastic responses of neonatal cardiac myocytes in culture were associated with enhanced expression of IGF-1 and IGF-1 receptors in these cells. Therefore, to determine the role of IGF-1 receptors on myocyte growth, cells were exposed to antisense oligodeoxynucleotides to IGF-1
J, Kajstura   +3 more
openaire   +2 more sources

Targeting the IGF-1 receptor: from rags to riches

European Journal of Cancer, 2004
The existence of the type 1 insulin-like growth factor receptor (IGF-IR) had been surmised for a number of years, before it was cloned in 1986 by Ullrich et al. [1]. At that time, the IGF-IR was considered a poor relative of the insulin receptor (IR), with which it has a 70% homology [1], a sort of redundant receptor that the cells used when the IR was
openaire   +2 more sources

Crosstalk between the extracellular domain of the ErbB2 receptor and IGF-1 receptor signaling

The Journal of Steroid Biochemistry and Molecular Biology, 2003
Insulin-like growth factor 1 receptor (IGF-1R) plays an important role in cell growth and malignant transformation. To investigate IGF-1R-dependent signaling events and its effects on apoptosis induction and cellular proliferation, we generated a constitutively active, ligand-independent IGF-1R variant.
Andrea, Belaus   +3 more
openaire   +2 more sources

Defects in IGF-1 receptor, insulin receptor and IRS-1/2 in Alzheimer's disease indicate possible resistance to IGF-1 and insulin signalling

Neurobiology of Aging, 2010
Insulin like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) signalling control vital growth, survival and metabolic functions in the brain. Here we describe specific and significant alterations in IGF-1R, IR, and their key substrate adaptor proteins IRS-1 and IRS-2 in Alzheimer's disease (AD). Western immunoblot analysis detected increased
Moloney, A.M.   +5 more
openaire   +3 more sources

Cell Cycle Control by the IGF-1 Receptor and Its Ligands

1994
The interaction of the IGF-1 receptor with its ligands (IGF-1, IGF-II and insulin at supraphysiological concentrations) plays a major role in normal development and in the control of both normal and abnormal growth (for reviews, see Werner et al., 1991 and Lowe, 1991).
R, Baserga, P, Porcu, M, Rubini, C, Sell
openaire   +2 more sources

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