Abstract
Osteoclasts are one of the key therapeutic targets for a variety of orthopedic diseases such as osteoporosis and osteoarthritis. In this study, we synthesized a novel compound N-(3-(cyclohexylcarbamoyl) phenyl)-1H-indole-2- carboxamide (termed as OA-4) and investigated the effects of OA-4 on the differentiation and function of osteoclasts. OA-4 markedly diminished osteoclast differentiation and osteoclast specific gene expression in a dose-dependent manner. In addition, OA-4 dose-dependently suppressed osteoclastic bone resorption. Furthermore, we found OA-4 attenuated RANKL-induced p38 phosphorylation without affecting JNK or NF-κB signaling pathways. Collectively, we synthesized a novel compound OA-4 which can inhibit osteoclast formation and functions via the suppression of p38 signaling pathway.
Keywords: OA-4, osteoclast formation, osteoclastic bone resorption, osteoporosis, P38 signaling pathway.
Current Medicinal Chemistry
Title:OA-4 Inhibits Osteoclast Formation and Bone Resorption via Suppressing RANKL Induced P38 Signaling Pathway
Volume: 21 Issue: 5
Author(s): B. Tian, A. Qin, Z.Y. Shao, T. Jiang, Z.J. Zhai, H.W. Li, T.T. Tang, Q. Jiang, K.R. Dai, M.H. Zheng, Y.P. Yu and Z.A. Zhu
Affiliation:
Keywords: OA-4, osteoclast formation, osteoclastic bone resorption, osteoporosis, P38 signaling pathway.
Abstract: Osteoclasts are one of the key therapeutic targets for a variety of orthopedic diseases such as osteoporosis and osteoarthritis. In this study, we synthesized a novel compound N-(3-(cyclohexylcarbamoyl) phenyl)-1H-indole-2- carboxamide (termed as OA-4) and investigated the effects of OA-4 on the differentiation and function of osteoclasts. OA-4 markedly diminished osteoclast differentiation and osteoclast specific gene expression in a dose-dependent manner. In addition, OA-4 dose-dependently suppressed osteoclastic bone resorption. Furthermore, we found OA-4 attenuated RANKL-induced p38 phosphorylation without affecting JNK or NF-κB signaling pathways. Collectively, we synthesized a novel compound OA-4 which can inhibit osteoclast formation and functions via the suppression of p38 signaling pathway.
Export Options
About this article
Cite this article as:
Tian B., Qin A., Shao Z.Y., Jiang T., Zhai Z.J., Li H.W., Tang T.T., Jiang Q., Dai K.R., Zheng M.H., Yu Y.P. and Zhu Z.A., OA-4 Inhibits Osteoclast Formation and Bone Resorption via Suppressing RANKL Induced P38 Signaling Pathway, Current Medicinal Chemistry 2014; 21 (5) . https://dx.doi.org/10.2174/09298673113209990190
DOI https://dx.doi.org/10.2174/09298673113209990190 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
Regulation of MET Receptor Signaling by SOCS1 and its Implications for Hepatocellular Carcinoma
Current Pharmaceutical Design Theranostic Applications of Lutetium-177 in Radionuclide Therapy
Current Radiopharmaceuticals Functional Antagonism between NF-κB and Nuclear Receptors: Implications in Carcinogenesis and Strategies for Optimal Cancer Chemopreventive Interventions
Current Cancer Drug Targets Prevalence of Breast Complaints in Women with Mastopathy in Khorramabad
Current Women`s Health Reviews Emergence of Nanomedicine as Cancer Targeted Magic Bullets: Recent Development and Need to Address the Toxicity Apprehension
Current Drug Discovery Technologies Chemistry and Pharmacological Properties of Some Natural and Synthetic Antioxidants for Heavy Metal Toxicity
Current Medicinal Chemistry Technology Whitespaces India Should Focus: A Comparative Anti-Cancer Patent Rational Analysis of Indian and International Public Funded Universities
Recent Patents on Anti-Cancer Drug Discovery Design of New Oxazaphosphorine Anticancer Drugs
Current Pharmaceutical Design Protease-Activated Receptor 2: Are Common Functions in Glial and Immune Cells Linked to Inflammation-Related CNS Disorders?
Current Drug Targets Chemotherapy-Induced Modifications to Gastrointestinal Microflora: Evidence and Implications of Change
Current Drug Metabolism N-substituted Pyrrole-based Scaffolds as Potential Anticancer and Antiviral Lead Structures
Medicinal Chemistry Patent Selections
Recent Patents on Inflammation & Allergy Drug Discovery Targeted Cancer Therapy: The Next Generation of Cancer Treatment
Current Drug Discovery Technologies Novel Approaches Towards Designing of Isoform-Selective Inhibitors Against Class II Histone Deacetylases: The Acute Requirement for Targetted Anticancer Therapy
Current Topics in Medicinal Chemistry Design and Synthesis of Mannich bases as Benzimidazole Derivatives as Analgesic Agents
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry MicroRNAs: Potential Diagnostic and Therapeutic Targets for Breast Cancer
Epigenetic Diagnosis & Therapy (Discontinued) Actions of the Anti-Angiogenic Compound Angiostatin in an Animal Model of Alzheimer’s Disease
Current Alzheimer Research Regulation of HIF-1α at the Transcriptional Level
Current Pharmaceutical Design Synthetic Lethality and PARP-Inhibitors in Oral and Head & Neck Cancer
Current Pharmaceutical Design Glioma: Tryptophan Catabolite and Melatoninergic Pathways Link microRNA, 14-3- 3, Chromosome 4q35, Epigenetic Processes and other Glioma Biochemical Changes
Current Pharmaceutical Design