Abstract
Receptor tyrosine kinases (RTK) are transmembrane receptors regulating cellular proliferation, differentiation, apoptosis, motility and recruitment of the vasculature. Aberrant expression and/or function of RTK have been detected in many malignant tumors and are considered to be a part of the transformed phenotype. The action of several classes of anti-cancer drugs is based on specific recognition of RTK. Monoclonal antibodies target extracellular binding domains, while tyrosine kinase inhibitors (TKI) bind to intracellular kinase domains to suppress RTK signaling. The issues regarding the efficient use of RTK targeting are the inter- and intra-patient heterogeneity of RTK expression and the changes of expression levels during the course of disease and in response to therapy. Radionuclide molecular imaging of RTK expression may aid in selecting patients who would benefit from RTK-targeting therapy and in identifying non-responders. Therefore, the therapy would be more personalized. Currently, radiolabeled proteins (monoclonal antibodies and their fragments, natural peptides ligands to RTK and de novo selected affinity proteins) and TKI and their analogues are under development for the visualization of RTK. In this review, we discuss the advantages and disadvantages of these approaches.
Keywords: Radionuclide, molecular imaging, receptor tyrosine kinases, monoclonal antibodies, tyrosine kinase inhibitors, scaffold proteins.
Current Pharmaceutical Design
Title:Radiolabeled Probes Targeting Tyrosine-Kinase Receptors For Personalized Medicine
Volume: 20 Issue: 14
Author(s): Mohamed Altai, Anna Orlova and Vladimir Tolmachev
Affiliation:
Keywords: Radionuclide, molecular imaging, receptor tyrosine kinases, monoclonal antibodies, tyrosine kinase inhibitors, scaffold proteins.
Abstract: Receptor tyrosine kinases (RTK) are transmembrane receptors regulating cellular proliferation, differentiation, apoptosis, motility and recruitment of the vasculature. Aberrant expression and/or function of RTK have been detected in many malignant tumors and are considered to be a part of the transformed phenotype. The action of several classes of anti-cancer drugs is based on specific recognition of RTK. Monoclonal antibodies target extracellular binding domains, while tyrosine kinase inhibitors (TKI) bind to intracellular kinase domains to suppress RTK signaling. The issues regarding the efficient use of RTK targeting are the inter- and intra-patient heterogeneity of RTK expression and the changes of expression levels during the course of disease and in response to therapy. Radionuclide molecular imaging of RTK expression may aid in selecting patients who would benefit from RTK-targeting therapy and in identifying non-responders. Therefore, the therapy would be more personalized. Currently, radiolabeled proteins (monoclonal antibodies and their fragments, natural peptides ligands to RTK and de novo selected affinity proteins) and TKI and their analogues are under development for the visualization of RTK. In this review, we discuss the advantages and disadvantages of these approaches.
Export Options
About this article
Cite this article as:
Altai Mohamed, Orlova Anna and Tolmachev Vladimir, Radiolabeled Probes Targeting Tyrosine-Kinase Receptors For Personalized Medicine, Current Pharmaceutical Design 2014; 20 (14) . https://dx.doi.org/10.2174/13816128113196660667
DOI https://dx.doi.org/10.2174/13816128113196660667 |
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
-
Dealing with the Substance Abuse Epidemic and Infective Endocarditis:Clinical, Immunologic and Pathogenetic Aspects
Current Vascular Pharmacology Utility of γH2AX as a Molecular Marker of DNA Double-Strand Breaks in Nuclear Medicine: Applications to Radionuclide Therapy Employing Auger Electron-Emitting Isotopes
Current Radiopharmaceuticals Traditional Fruits of Kerala: Bioactive Compounds and their Curative Potential in Chronic Diseases
Current Nutrition & Food Science Chemoprotective Mechanism of the Natural Compounds, Epigallocatechin- 3-O-Gallate, Quercetin and Curcumin Against Cancer and Cardiovascular Diseases
Current Medicinal Chemistry Novel Ideas of Gene Therapy for Atherosclerosis: Modulation of Cellular Signal Transduction of TGF-β Family
Current Pharmaceutical Design The Targeted-liposome Delivery System of Antitumor Drugs
Current Drug Metabolism Fabry Disease and Cardiovascular Involvement
Current Pharmaceutical Design Tanshinone IIA: Pharmacology, Total Synthesis, and Progress in Structure-modifications
Current Medicinal Chemistry Basic and Clinical Research Against Advanced Glycation End Products (AGEs): New Compounds to Tackle Cardiovascular Disease and Diabetic Complications
Recent Advances in Cardiovascular Drug Discovery (Discontinued) Gold(III) Complexes in the Oncological Preclinical Arena: From Aminoderivatives to Peptidomimetics
Current Topics in Medicinal Chemistry Redox Signaling Pathways Involved in Neuronal Ischemic Preconditioning
Current Neuropharmacology Blockade of the Renin-Angiotensin-Aldosterone System: Effects on Hypertensive Target Organ Damage
Cardiovascular & Hematological Agents in Medicinal Chemistry Epicardial and Intramyocardial Adipose Tissue: The Enemy within
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Renin-Angiotensin-Aldosterone System in Autosomal Dominant Polycystic Kidney Disease
Current Hypertension Reviews Role of β 2-Adrenoceptor Activation in Sepsis-Induced Renal Inflammation
Current Immunology Reviews (Discontinued) Recent Advances in Targeted Anti-Vasculature Therapy: The Neuroblastoma Model
Current Drug Targets Synthesis and Inhibitory Effects of Some Novel 1,3-diarylprop-2-en-1-one Analogues in Foxp3 Expression: A Novel Class of Anti-cancer Candidates
Medicinal Chemistry Risk Models and Scores of Cardiovascular Disease in Patients with Diabetes Mellitus
Current Pharmaceutical Design Diabetic Cardiomyopathy: From Mechanism to Management in a Nutshell
Endocrine, Metabolic & Immune Disorders - Drug Targets Role of Endothelin in Diabetic Retinopathy
Current Vascular Pharmacology