Abstract
The insulin-like growth factors (IGF) and their receptors play pivotal roles in cellular signaling transduction and thus regulate cell growth, differentiation, apoptosis, transformation and other important physiological progresses. The insulin-like growth factor 1 receptor (IGF-1R) mainly engages in the Ras/mitogen-activated protein kinase (MAPK) pathway and the phosphoinositide 3-kinase/protein kinase B (PI3K/AKT) pathway, and also forms cross-talk with the epidermal growth factor receptor (EGFR) pathway. Currently, it draws more attention since its overexpression has been demonstrated in various human cancers, such as colorectal cancer, breast cancer, prostate cancer and lung tumors, thus the strategy targeting the IGF-1R would be promising in treatment of these cancers. There are already dozens of agents developed for the inhibition of IGF-1R, which are categorized into monoclonal antibodies, small molecule inhibitors and so on. While in this review, small molecule inhibitors would be the focus for detailed discussion. Herein, we updated previously reported research papers and reviews in this field and summarized developments of small molecule inhibitors up to 2011. Finally, we proposed the application of network pharmacology methods to reconsider the clinical use of inhibitors with concomitant IR inhibition or other kinases inhibition, hoping that more optimal combinations would be obtained for cancer therapy.
Keywords: Receptor tyrosine kinase, IGF-1R, IR, EGFR, small molecule inhibitors, anticancer strategies, signaling transduction pathway, network pharmacology, cell growth, apoptosis
Current Pharmaceutical Design
Title:Insulin-like Growth Factor-1 Receptor (IGF-1R) Kinase Inhibitors in Cancer Therapy: Advances and Perspectives
Volume: 18 Issue: 20
Author(s): Mengzhu Xue, Xianwen Cao, Ye Zhong, Dong Kuang, Xiaofeng Liu, Zhenjiang Zhao and Honglin Li
Affiliation:
Keywords: Receptor tyrosine kinase, IGF-1R, IR, EGFR, small molecule inhibitors, anticancer strategies, signaling transduction pathway, network pharmacology, cell growth, apoptosis
Abstract: The insulin-like growth factors (IGF) and their receptors play pivotal roles in cellular signaling transduction and thus regulate cell growth, differentiation, apoptosis, transformation and other important physiological progresses. The insulin-like growth factor 1 receptor (IGF-1R) mainly engages in the Ras/mitogen-activated protein kinase (MAPK) pathway and the phosphoinositide 3-kinase/protein kinase B (PI3K/AKT) pathway, and also forms cross-talk with the epidermal growth factor receptor (EGFR) pathway. Currently, it draws more attention since its overexpression has been demonstrated in various human cancers, such as colorectal cancer, breast cancer, prostate cancer and lung tumors, thus the strategy targeting the IGF-1R would be promising in treatment of these cancers. There are already dozens of agents developed for the inhibition of IGF-1R, which are categorized into monoclonal antibodies, small molecule inhibitors and so on. While in this review, small molecule inhibitors would be the focus for detailed discussion. Herein, we updated previously reported research papers and reviews in this field and summarized developments of small molecule inhibitors up to 2011. Finally, we proposed the application of network pharmacology methods to reconsider the clinical use of inhibitors with concomitant IR inhibition or other kinases inhibition, hoping that more optimal combinations would be obtained for cancer therapy.
Export Options
About this article
Cite this article as:
Xue Mengzhu, Cao Xianwen, Zhong Ye, Kuang Dong, Liu Xiaofeng, Zhao Zhenjiang and Li Honglin, Insulin-like Growth Factor-1 Receptor (IGF-1R) Kinase Inhibitors in Cancer Therapy: Advances and Perspectives , Current Pharmaceutical Design 2012; 18 (20) . https://dx.doi.org/10.2174/138161212800672723
DOI https://dx.doi.org/10.2174/138161212800672723 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Immunotherapy of Cancer Based on DC-Tumor Fusion Vaccine
Current Immunology Reviews (Discontinued) Nanovehicle-based Small Interfering RNA (siRNA) Delivery for Therapeutic Purposes: A New Molecular Approach in Pharmacogenomics
Current Clinical Pharmacology A Review of Preclinical Experiments Toward Targeting M2 Macrophages in Prostate Cancer
Current Drug Targets Recent Applications of Triazolopyrimidine-Based Bioactive Compounds in Medicinal and Agrochemical Chemistry
Mini-Reviews in Medicinal Chemistry Extracellular Matrix and Aberrant Signaling in Lung Carcinoma: Role of Fibronectin in the Control of Human Lung Carcinoma Cell Growth,Apoptosis and Resistance to Therapy
Current Signal Transduction Therapy The Role of Non-coding Genome in Cancer-associated Fibroblasts; Stateof- the-Art and Perspectives in Cancer Targeted Therapy
Current Drug Targets Molecular Aspects of FKBP51 that Enable Melanoma Dissemination
Current Molecular Pharmacology Targeting Apoptosis Pathways in Cancer Therapy
Current Cancer Drug Targets Structural and Functional Organization of miRNAs
Current Pharmacogenomics Roles of Retinoic Acid in Induction of Immunity and Immune Tolerance
Endocrine, Metabolic & Immune Disorders - Drug Targets Hesperetin Liposomes for Cancer Therapy
Current Drug Delivery Cyclodepsipeptides - Potential Drugs and Lead Compounds in the Drug Development Process
Current Medicinal Chemistry Control of Copper Status for Cancer Therapy
Current Cancer Drug Targets 18F-FDG-PET/CT in Patients Affected by Differentiated Thyroid Carcinoma with Positive Thyroglobulin Level and Negative 131I Whole Body Scan. It's Value Confirmed by a Bicentric Experience
Current Radiopharmaceuticals Fibroblast Growth Factor 2: From Laboratory Evidence to Clinical Application
Current Vascular Pharmacology Antineoplastic Potential of Medicinal Plants
Recent Patents on Biotechnology Development of Selective Cyclin-Dependent Kinase 4 Inhibitors for Antineoplastic Therapies
Anti-Cancer Agents in Medicinal Chemistry Patent Selections
Recent Patents on Biomarkers Overview of Angiogenesis and the use of Bevacizumab in Patients with Malignant Gliomas
Current Signal Transduction Therapy New Molecular and Cellular Targets for Chemoprevention and Treatment of Skin Tumors by Plant Polyphenols: A Critical Review
Current Medicinal Chemistry