Below the Surface: IGF-1R Therapeutic Targeting and Its Endocytic Journey

Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations

(2019) Laura M. Wingler et al.   CELL

New Binding Sites, New Opportunities for GPCR Drug Discovery

(2019) H.C. Stephen Chan et al.   TRENDS IN BIOCHEMICAL SCIENCES

GPCR Signaling Regulation: The Role of GRKs and Arrestins

(2019) Vsevolod V. Gurevich et al.   Frontiers in Pharmacology

Therapeutic Targeting of the IGF Axis

(2019) Eliot Osher et al.   Cells

The Neglected Insulin: IGF-II, a Metabolic Regulator with Implications for Diabetes, Obesity, and Cancer

(2019) Holly et al.   Cells

Aiming for the Insulin-like Growth Factor-1 system in breast cancer therapeutics

(2018) Panagiotis F. Christopoulos et al.   CANCER TREATMENT REVIEWS

GPCR signaling: conformational activation of arrestins

(2018) Alem W. Kahsai et al.   CELL RESEARCH

GPCR desensitization: Acute and prolonged phases

(2018) Sudarshan Rajagopal et al.   CELLULAR SIGNALLING

Blocking of autocrine IGF-1 reduces viability of human umbilical cord mesenchymal stem cells via inhibition of the Akt/Gsk-3β signaling pathway

(2018) Qi Wang et al.   Molecular Medicine Reports

FES-related tyrosine kinase activates the insulin-like growth factor-1 receptor at sites of cell adhesion

(2018) Joanna Stanicka et al.   ONCOGENE

AGC kinases, mechanisms of regulation ‎and innovative drug development

(2018) Alejandro E. Leroux et al.   SEMINARS IN CANCER BIOLOGY

G protein-coupled receptor kinases (GRKs) in tumorigenesis and cancer progression: GPCR regulators and signaling hubs

(2018) Laura Nogués et al.   SEMINARS IN CANCER BIOLOGY

A novel functional crosstalk between DDR1 and the IGF axis and its relevance for breast cancer

(2018) Antonino Belfiore et al.   Cell Adhesion & Migration

Annexin A1 regulates EGFR activity and alters EGFR-containing tumour-derived exosomes in head and neck cancers

(2018) N. Raulf et al.   EUROPEAN JOURNAL OF CANCER

Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9

(2018) Louis M. Luttrell et al.   Science Signaling

G protein–coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor

(2018) Minjung Choi et al.   Science Signaling

Is there potential for the approval of monoclonal antibodies to treat thyroid-associated ophthalmopathy?

(2018) Terry J. Smith   Expert Opinion on Orphan Drugs

Insulin Receptor Isoforms in Physiology and Disease: An Updated View

(2017) Antonino Belfiore et al.   ENDOCRINE REVIEWS

Trends in GPCR drug discovery: new agents, targets and indications

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

Detection of wild-type EGFR amplification and EGFRvIII mutation in CSF-derived extracellular vesicles of glioblastoma patients

(2017) Javier M Figueroa et al.   NEURO-ONCOLOGY

Functional antagonism of β-arrestin isoforms balance IGF-1R expression and signalling with distinct cancer-related biological outcomes

(2017) N Suleymanova et al.   ONCOGENE

Unbalancing p53/Mdm2/IGF-1R axis by Mdm2 activation restrains the IGF-1-dependent invasive phenotype of skin melanoma

(2017) C Worrall et al.   ONCOGENE

Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

(2017) Thomas J. Cahill et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GPCR Signaling and Trafficking: The Long and Short of It

(2017) Nathan J. Pavlos et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Enhanced response of melanoma cells to MEK inhibitors following unbiased IGF-1R down-regulation

(2017) Naida Suleymanova et al.   Oncotarget

Preclinical and first-in-human phase I studies of KW-2450, an oral tyrosine kinase inhibitor with insulin-like growth factor receptor-1/insulin receptor selectivity

(2016) Gary K. Schwartz et al.   CANCER SCIENCE

Small-molecule kinase inhibitors: an analysis of FDA-approved drugs

(2016) Peng Wu et al.   DRUG DISCOVERY TODAY

c-Src, Insulin-Like Growth Factor I Receptor, G-Protein-Coupled Receptor Kinases and Focal Adhesion Kinase are Enriched Into Prostate Cancer Cell Exosomes

(2016) Rachel M. DeRita et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Epidermal Growth Factor Receptor in Prostate Cancer Derived Exosomes

(2016) Geetanjali Kharmate et al.   PLoS One

Insulin-like Growth Factor 1 Signaling Axis Meets p53 Genome Protection Pathways

(2016) Haim Werner et al.   Frontiers in Oncology

The dichotomy of the Insulin-like growth factor 1 receptor: RTK and GPCR: friend or foe for cancer treatment?

(2015) Caitrin Crudden et al.   GROWTH HORMONE & IGF RESEARCH

NEDD4 ubiquitin ligase is a putative oncogene in endometrial cancer that activates IGF-1R/PI3K/Akt signaling

(2015) Yuping Zhang et al.   GYNECOLOGIC ONCOLOGY

Minireview: Were the IGF Signaling Inhibitors All Bad?

(2015) Heather Beckwith et al.   MOLECULAR ENDOCRINOLOGY

HRD1 suppresses the growth and metastasis of breast cancer cells by promoting IGF-1R degradation

(2015) Yue-Mei Xu et al.   Oncotarget

Targeting the IGF-1R: The Tale of the Tortoise and the Hare

(2015) Caitrin Crudden et al.   Frontiers in Endocrinology

Arrestin-dependent Angiotensin AT1Receptor Signaling Regulates Akt and mTor-mediated Protein Synthesis

(2014) Ryan T. Kendall et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Something old, something new and something borrowed: emerging paradigm of insulin-like growth factor type 1 receptor (IGF-1R) signaling regulation

(2013) Leonard Girnita et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Designing Novel Therapies Against Sarcomas in the Era of Personalized Medicine and Economic Crisis

(2013) Maria Manara et al.   CURRENT PHARMACEUTICAL DESIGN

Targeting Non-Small Cell Lung Cancer Cells by Dual Inhibition of the Insulin Receptor and the Insulin-Like Growth Factor-1 Receptor

(2013) Emma E. Vincent et al.   PLoS One

Endocytosis of Receptor Tyrosine Kinases

(2013) L. K. Goh et al.   Cold Spring Harbor Perspectives in Biology

IGF-1R as an anti-cancer target--trials and tribulations

(2013) Helen X. Chen et al.   Chinese Journal of Cancer

Insulin/insulin-like growth factor (IGF) stimulation abrogates an association between a deubiquitinating enzyme USP7 and insulin receptor substrates (IRSs) followed by proteasomal degradation of IRSs

(2012) Hidehito Yoshihara et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

CSF-1 receptor signalling from endosomes mediates the sustained activation of Erk1/2 and Akt in macrophages

(2012) Jennifer Huynh et al.   CELLULAR SIGNALLING

Targeting the insulin-like growth factor 1 receptor (IGF1R) signaling pathway for cancer therapy

(2012) Cristina E Tognon et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

The decline and fall of the IGF-I receptor

(2012) Renato Baserga   JOURNAL OF CELLULAR PHYSIOLOGY

Effect of a Low-Fat Diet Combined with IGF-1 Receptor Blockade on 22Rv1 Prostate Cancer Xenografts

(2012) R. Konijeti et al.   MOLECULAR CANCER THERAPEUTICS

Melanoma exosomes educate bone marrow progenitor cells toward a pro-metastatic phenotype through MET

(2012) Héctor Peinado et al.   NATURE MEDICINE

Atypical ubiquitylation — the unexplored world of polyubiquitin beyond Lys48 and Lys63 linkages

(2012) Yogesh Kulathu et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The Origin and Evolution of G Protein-Coupled Receptor Kinases

(2012) Arcady Mushegian et al.   PLoS One

Heterodimerization of Glycosylated Insulin-Like Growth Factor-1 Receptors and Insulin Receptors in Cancer Cells Sensitive to Anti-IGF1R Antibody

(2012) Jun Gyu Kim et al.   PLoS One

 -Arrestin-biased agonism as the central mechanism of action for insulin-like growth factor 1 receptor-targeting antibodies in Ewing's sarcoma

(2012) H. Zheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective recruitment of G protein-coupled receptor kinases (GRKs) controls signaling of the insulin-like growth factor 1 receptor

(2012) H. Zheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Transfer of Growth Factor Receptor mRNA Via Exosomes Unravels the Regenerative Effect of Mesenchymal Stem Cells

(2012) Susanna Tomasoni et al.   STEM CELLS AND DEVELOPMENT

A Single Mutation in Arrestin-2 Prevents ERK1/2 Activation by Reducing c-Raf1 Binding

(2011) Sergio Coffa et al.   BIOCHEMISTRY

Dual IGF-1R/InsR Inhibitor BMS-754807 Synergizes with Hormonal Agents in Treatment of Estrogen-Dependent Breast Cancer

(2011) X. Hou et al.   CANCER RESEARCH

The role of endocytosis in activating and regulating signal transduction

(2011) Emma R. Andersson   CELLULAR AND MOLECULAR LIFE SCIENCES

18FDG-PET Predicts Pharmacodynamic Response to OSI-906, a Dual IGF-1R/IR Inhibitor, in Preclinical Mouse Models of Lung Cancer

(2011) E. T. McKinley et al.   CLINICAL CANCER RESEARCH

Reading the ubiquitin postal code

(2011) Jean-François Trempe   CURRENT OPINION IN STRUCTURAL BIOLOGY

Polyubiquitination of Insulin-like Growth Factor I Receptor (IGF-IR) Activation Loop Promotes Antibody-induced Receptor Internalization and Down-regulation

(2011) Yifan Mao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterization of soluble and exosomal forms of the EGFR released from pancreatic cancer cells

(2011) Kamila A. Adamczyk et al.   LIFE SCIENCES

Potent Inhibition of Angiogenesis by the IGF-1 Receptor-Targeting Antibody SCH717454 Is Reversed by IGF-2

(2011) H. K. Bid et al.   MOLECULAR CANCER THERAPEUTICS

Identification of the cathelicidin peptide LL-37 as agonist for the type I insulin-like growth factor receptor

(2011) A Girnita et al.   ONCOGENE

G protein-coupled receptor kinases: More than just kinases and not only for GPCRs

(2011) Eugenia V. Gurevich et al.   PHARMACOLOGY & THERAPEUTICS

Distinct Phosphorylation Sites on the  2-Adrenergic Receptor Establish a Barcode That Encodes Differential Functions of  -Arrestin

(2011) K. N. Nobles et al.   Science Signaling

β-arrestin-mediated receptor trafficking and signal transduction

(2011) Sudha K. Shenoy et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Receptor tyrosine kinase–G-protein-coupled receptor signalling platforms: out of the shadow?

(2011) Nigel J. Pyne et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Endosomal signalling of epidermal growth factor receptors contributes to EGF-stimulated cell cycle progression in primary hepatocytes

(2010) Yi Luo et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Differential G-protein-coupled Receptor Phosphorylation Provides Evidence for a Signaling Bar Code

(2010) Adrian J. Butcher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting the insulin-like growth factor I receptor inhibits proliferation and VEGF production of non-small cell lung cancer cells and enhances paclitaxel-mediated anti-tumor effect

(2010) Maria Spiliotaki et al.   LUNG CANCER

Molecular mechanism of multivesicular body biogenesis by ESCRT complexes

(2010) Thomas Wollert et al.   NATURE

IGF-IR Internalizes with Caveolin-1 and PTRF/Cavin in Hacat Cells

(2010) Barbara Salani et al.   PLoS One

Insulin Receptor Isoforms and Insulin Receptor/Insulin-Like Growth Factor Receptor Hybrids in Physiology and Disease

(2009) Antonino Belfiore et al.   ENDOCRINE REVIEWS

Targeting the IGF1 axis in cancer proliferation

(2009) Ilan Bruchim et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Oligomerized Tie2 localizes to clathrin-coated pits in response to angiopoietin-1

(2009) Elena Bogdanovic et al.   HISTOCHEMISTRY AND CELL BIOLOGY

β-Arrestin-2 Mediates Anti-apoptotic Signaling through Regulation of BAD Phosphorylation

(2009) Seungkirl Ahn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

AMG 479, a fully human anti-insulin-like growth factor receptor type I monoclonal antibody, inhibits the growth and survival of pancreatic carcinoma cells

(2009) P. J. Beltran et al.   MOLECULAR CANCER THERAPEUTICS

BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR

(2009) J. M. Carboni et al.   MOLECULAR CANCER THERAPEUTICS

Pathways and mechanisms of endocytic recycling

(2009) Barth D. Grant et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Emerging role of insulin-like growth factor receptor inhibitors in oncology: early clinical trial results and future directions

(2009) A Gualberto et al.   ONCOGENE

High Expression Levels of Total IGF-1R and Sensitivity of NSCLC Cells In Vitro to an Anti-IGF-1R Antibody (R1507)

(2009) Yixuan Gong et al.   PLoS One

 -Arrestin-dependent signaling and trafficking of 7-transmembrane receptors is reciprocally regulated by the deubiquitinase USP33 and the E3 ligase Mdm2

(2009) S. K. Shenoy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Addiction to Elevated Insulin-like Growth Factor I Receptor and Initial Modulation of the AKT Pathway Define the Responsiveness of Rhabdomyosarcoma to the Targeting Antibody

(2008) L. Cao et al.   CANCER RESEARCH

Identification of c-Cbl as a New Ligase for Insulin-like Growth Factor-I Receptor with Distinct Roles from Mdm2 in Receptor Ubiquitination and Endocytosis

(2008) B. Sehat et al.   CANCER RESEARCH

Grb10/Nedd4-mediated multiubiquitination of the insulin-like growth factor receptor regulates receptor internalization

(2008) Giada Monami et al.   JOURNAL OF CELLULAR PHYSIOLOGY

New Picropodophyllin Analogs via Palladium-Catalyzed Allylic Alkylation−Hiyama Cross-Coupling Sequences

(2008) Maxime Vitale et al.   JOURNAL OF ORGANIC CHEMISTRY

Evolution of the Insulin Receptor Family and Receptor Isoform Expression in Vertebrates

(2008) C. Hernandez-Sanchez et al.   MOLECULAR BIOLOGY AND EVOLUTION

IGF1 Is a Common Target Gene of Ewing's Sarcoma Fusion Proteins in Mesenchymal Progenitor Cells

(2008) Luisa Cironi et al.   PLoS One

Heterotrimeric G protein activation by G-protein-coupled receptors

(2007) William M. Oldham et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY