Abstract
Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are highly prevalent gastrointestinal disorders. Traditional symptoms based therapies had somewhat limited success and efficacy in addressing the disorders. Recently, linaclotide emerged as novel peptide capable of improving abdominal symptoms in patients suffering from IBS-C and CIC. Guanylate cyclase C (GC-C) receptor a multi domain protein, found to be molecular target for linaclotide which acts by activating GC-C receptor on the apical surface of intestinal epithelial cells. Binding of linaclotide to GC-C receptor triggers the elevation of second messenger cGMP that elicits fluid secretion into intestinal cells which play a critical role in maintaining homeostasis through cystic fibrosis transmembrane conductance regulator (CFTR). Data from Phase and clinical trials demonstrated that linaclotide seems to produce a statistically significant increase in stool frequency, improved straining, decreased abdominal pain and discomfort.
Keywords: CIC, cGMP, guanylate cyclase C, homeostasis, IBS-C, Linaclotide.
Mini-Reviews in Medicinal Chemistry
Title:Linaclotide-a Novel Secretagogue in the Treatment of Irritable Bowel Syndrome with Constipation and Chronic Idiopathic Constipation
Volume: 13 Issue: 11
Author(s): Shivani Sharma, Tina Sharma, Richa Dhingra, Prince Tomar, Sukhminder Singh, Manav Malhotra and T. R. Bhardwaj
Affiliation:
Keywords: CIC, cGMP, guanylate cyclase C, homeostasis, IBS-C, Linaclotide.
Abstract: Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are highly prevalent gastrointestinal disorders. Traditional symptoms based therapies had somewhat limited success and efficacy in addressing the disorders. Recently, linaclotide emerged as novel peptide capable of improving abdominal symptoms in patients suffering from IBS-C and CIC. Guanylate cyclase C (GC-C) receptor a multi domain protein, found to be molecular target for linaclotide which acts by activating GC-C receptor on the apical surface of intestinal epithelial cells. Binding of linaclotide to GC-C receptor triggers the elevation of second messenger cGMP that elicits fluid secretion into intestinal cells which play a critical role in maintaining homeostasis through cystic fibrosis transmembrane conductance regulator (CFTR). Data from Phase and clinical trials demonstrated that linaclotide seems to produce a statistically significant increase in stool frequency, improved straining, decreased abdominal pain and discomfort.
Export Options
About this article
Cite this article as:
Sharma Shivani, Sharma Tina, Dhingra Richa, Tomar Prince, Singh Sukhminder, Malhotra Manav and Bhardwaj R. T., Linaclotide-a Novel Secretagogue in the Treatment of Irritable Bowel Syndrome with Constipation and Chronic Idiopathic Constipation, Mini-Reviews in Medicinal Chemistry 2013; 13 (11) . https://dx.doi.org/10.2174/1389557511313110011
DOI https://dx.doi.org/10.2174/1389557511313110011 |
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
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...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
- 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
-
Lipid Nanocarriers and Molecular Targets for Malaria Chemotherapy
Current Drug Targets A System Pharmacology Study for Deciphering Anti Depression Activity of Nardostachys jatamansi
Current Drug Metabolism The Role of CO-RADS Scoring System in the Diagnosis of COVID-19 Infection and its Correlation with Clinical Signs
Current Medical Imaging Appropriate Use of Antibiotics for the Management of Respiratory Tract Infections
Infectious Disorders - Drug Targets Intrathecal Enzyme Replacement Therapy for Mucopolysaccharidosis I: Translating Success in Animal Models to Patients
Current Pharmaceutical Biotechnology Efficacy of Fluoroquinolones Against Pathogenic Oral Bacteria
Mini-Reviews in Medicinal Chemistry Pain Perception and Management: Where do We Stand?
Current Molecular Pharmacology Safety and Efficacy of Setarud (IMOD TM ) Among People Living with HIV/AIDS: A Review
Recent Patents on Anti-Infective Drug Discovery Acne and Its Treatment Options - A Review
Current Drug Delivery Practical Lessons from Amyloid Immunotherapy Trials in Alzheimer Disease
Current Alzheimer Research New Uses of Melatonin as a Drug; A Review
Current Medicinal Chemistry Clinical, Genetic, and Neuroimaging Features of Early Onset Alzheimer Disease: The Challenges of Diagnosis and Treatment
Current Alzheimer Research The Therapeutic Potential of Melatonin in Neurological Disorders
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Calcium Channel Blockers in Obesity-Related Hypertension
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) The Use of Carvedilol in Pediatric Heart Failure
Cardiovascular & Hematological Disorders-Drug Targets Postpartum Psychiatric Disorders: What Do We Know And Where Do We Go?
Current Psychiatry Reviews Efficacy and Adverse Effects of Venlafaxine in Children and Adolescents with ADHD: A Systematic Review of Non-controlled and Controlled Trials
Reviews on Recent Clinical Trials Melatonin and Melatoninergic Drugs as Therapeutic Agents: Ramelteon and Agomelatine, the Two Most Promising Melatonin Receptor Agonists
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery An Overview on Different Classes of Viral Entry and Respiratory Syncitial Virus (RSV) Fusion Inhibitors
Current Medicinal Chemistry Sleep Disordered Breathing: Alternatives to CPAP Therapy
Current Respiratory Medicine Reviews