Abstract
In the current review, we discuss the role of NF-κB and JAK/STAT signaling pathways and their small molecule regulators in the therapy of inflammatory diseases. Considering potential harmful effects directly assigned to the COX-2 inhibition, novel therapeutically-relevant biological targets such as NF-κB and JAK/STAT signaling pathways have received a growing attention. Here we summarize recent progress in the identification and development of novel, clinically approved or evaluated small molecule regulators of these signaling cascades as promising anti-inflammatory therapeutics. In addition, we illustrate key structural modifications and bioisosteric transformations among these inhibitors to provide a helpful basis for further development of novel small molecule anti-inflammatory agents.
Keywords: NF-κB, JAK/STAT, signalling, inhibitors, anti-inflammatory, therapy, Chronic inflammation, rheumatoid arthritis, ischaemic heart disease, atherosclerosis, cancer, fibrosis, Hayfever, Alzheimer's diseases, MAPKs, STAT, NSAIDs, Valdecoxib, leukemia, inflammatory bowel disease, arthritis, sepsis, asthma, multiple sclerosis, colitis, diabetic neuropathy, AIDS, GPCR, TNFR, NEMO, oxycodone/ibuprofen, Oxycodone, Bortezomib, RS-411, Fumaderm, Gabexate, MK-231, Silibinin, ST-1482, RK-0202, Salazosulfapyridine, Curaxin CBLC-102, NGX-3781, Hydrocodone, NSC-49171, Pseudoephedrine, T-614, Curcumin, MPC-7869, Dimethyl fumarate, Famotidine, Fluasterone, Tepoxalin, E-3330, EGCG, Declopramide, Resveratrol, Tranexamic acid, RTA-402, Orazipone, RTA-401, ALS-357, IMD-0354, SIM-688, ENMD-1198, Parthenolide, Cepharanthine, Taxifolin, SC-514, TPCA-1, BMS-345541, ML120B, HUVECs, RHEC, HMGB1, lung lavage, neutrophil influx, lung edema, SOCS, PIAS, Lestaurtinib, MHCII, HWA-486, CP-690550, MK-0457, TG-101348, LS-104, SKI-606, Atiprimod, ABT-869, mixed lymphocyte reaction, mycophenolate mofetil
Mini-Reviews in Medicinal Chemistry
Title: Small Molecule Inhibitors of NF-κB and JAK/STAT Signal Transduction Pathways as Promising Anti-Inflammatory Therapeutics
Volume: 11 Issue: 1
Author(s): Y. A. Ivanenkov, K. V. Balakin and Y. Lavrovsky
Affiliation:
Keywords: NF-κB, JAK/STAT, signalling, inhibitors, anti-inflammatory, therapy, Chronic inflammation, rheumatoid arthritis, ischaemic heart disease, atherosclerosis, cancer, fibrosis, Hayfever, Alzheimer's diseases, MAPKs, STAT, NSAIDs, Valdecoxib, leukemia, inflammatory bowel disease, arthritis, sepsis, asthma, multiple sclerosis, colitis, diabetic neuropathy, AIDS, GPCR, TNFR, NEMO, oxycodone/ibuprofen, Oxycodone, Bortezomib, RS-411, Fumaderm, Gabexate, MK-231, Silibinin, ST-1482, RK-0202, Salazosulfapyridine, Curaxin CBLC-102, NGX-3781, Hydrocodone, NSC-49171, Pseudoephedrine, T-614, Curcumin, MPC-7869, Dimethyl fumarate, Famotidine, Fluasterone, Tepoxalin, E-3330, EGCG, Declopramide, Resveratrol, Tranexamic acid, RTA-402, Orazipone, RTA-401, ALS-357, IMD-0354, SIM-688, ENMD-1198, Parthenolide, Cepharanthine, Taxifolin, SC-514, TPCA-1, BMS-345541, ML120B, HUVECs, RHEC, HMGB1, lung lavage, neutrophil influx, lung edema, SOCS, PIAS, Lestaurtinib, MHCII, HWA-486, CP-690550, MK-0457, TG-101348, LS-104, SKI-606, Atiprimod, ABT-869, mixed lymphocyte reaction, mycophenolate mofetil
Abstract: In the current review, we discuss the role of NF-κB and JAK/STAT signaling pathways and their small molecule regulators in the therapy of inflammatory diseases. Considering potential harmful effects directly assigned to the COX-2 inhibition, novel therapeutically-relevant biological targets such as NF-κB and JAK/STAT signaling pathways have received a growing attention. Here we summarize recent progress in the identification and development of novel, clinically approved or evaluated small molecule regulators of these signaling cascades as promising anti-inflammatory therapeutics. In addition, we illustrate key structural modifications and bioisosteric transformations among these inhibitors to provide a helpful basis for further development of novel small molecule anti-inflammatory agents.
Export Options
About this article
Cite this article as:
A. Ivanenkov Y., V. Balakin K. and Lavrovsky Y., Small Molecule Inhibitors of NF-κB and JAK/STAT Signal Transduction Pathways as Promising Anti-Inflammatory Therapeutics, Mini-Reviews in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/138955711793564079
DOI https://dx.doi.org/10.2174/138955711793564079 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Vitamin E and All-Cause Mortality: A Meta-Analysis
Current Aging Science Antibacterial and Antioxidant Property of Streptomyces cinnamonensis VITNS1 Isolated from Serkadu Region, Vellore, Tamil Nadu, India
Anti-Infective Agents Endothelial Dysfunction and Atherosclerosis: Focus on Novel Therapeutic Approaches
Recent Patents on Cardiovascular Drug Discovery NPY and Cardiac Diseases
Current Topics in Medicinal Chemistry Modifier Gene Studies to Identify New Therapeutic Targets in Cystic Fibrosis
Current Pharmaceutical Design Editorial
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents MicroRNAs as Potential Therapeutic Agents in the Treatment of Myocardial Infarction
Current Vascular Pharmacology The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases – Part I
Current Medicinal Chemistry Advances in Antithrombotic Agents
Cardiovascular & Hematological Agents in Medicinal Chemistry Filling the Gaps between the In Vivo and In Vitro Microenvironment: Engineering of Spheroids for Stem Cell Technology
Current Stem Cell Research & Therapy Plasma Steroid Level Measured Using Modern Separation Techniques as Biomarkers in Biological Diagnostics
Current Pharmaceutical Analysis Review of Endocrine Manifestations of Antiphospholid Syndrome
Current Rheumatology Reviews Microparticles: From Biogenesis to Biomarkers and Diagnostic Tools in Cardiovascular Disease
Current Stem Cell Research & Therapy Herbal Medicines for Diabetes Management and its Secondary Complications
Current Diabetes Reviews Nitric Oxide Synthase Function in Exercise
Current Enzyme Inhibition Salvaging the Ischemic Heart: Gi-Coupled Receptors in Mast Cells Activate a PKCε/ALDH2 Pathway Providing Anti-RAS Cardioprotection
Current Medicinal Chemistry Therapeutic Potential of Targeting Protease Activated Receptors in Cardiovascular Diseases
Current Pharmaceutical Design A Comprehensive Review on Phytochemistry and Pharmacological Effects of Stinging Nettle (Urtica dioica)
Current Traditional Medicine Cardiovascular Disease in Systemic Lupus Erythematosus: The Role of Traditional and Lupus Related Risk Factors
Current Cardiology Reviews Anti-apoptotic Serpins as Therapeutics in Cardiovascular Diseases
Cardiovascular & Hematological Disorders-Drug Targets