Abstract
A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.
Keywords: Tri-peptides, pTyr mimetics, PTP1B inhibitors, TCPTP, Type 2 diabetes, Metabolic disorders.
Medicinal Chemistry
Title:Peptidomimetics as Potent and Selective PTP1B Inhibitors
Volume: 9 Issue: 5
Author(s): Dipam Patel, Mukul Jain, Shailesh R. Shah, Rajesh Bahekar, Pradip Jadav, Kiran Shah, Amit Joharapurkar, Mubeen Shaikh and Kalapatapu V.V.M. Sairam
Affiliation:
Keywords: Tri-peptides, pTyr mimetics, PTP1B inhibitors, TCPTP, Type 2 diabetes, Metabolic disorders.
Abstract: A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.
Export Options
About this article
Cite this article as:
Patel Dipam, Jain Mukul, Shah R. Shailesh, Bahekar Rajesh, Jadav Pradip, Shah Kiran, Joharapurkar Amit, Shaikh Mubeen and Sairam V.V.M. Kalapatapu, Peptidomimetics as Potent and Selective PTP1B Inhibitors, Medicinal Chemistry 2013; 9 (5) . https://dx.doi.org/10.2174/1573406411309050005
DOI https://dx.doi.org/10.2174/1573406411309050005 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
-
Proteomic Analysis of Early Phosphorylated Proteins in Acute Pancreatitis
Model
Current Proteomics Computational Advances in Chronic Diseases Diagnostics and Therapy - II
Current Drug Targets Impact of the CD40-CD40L Dyad in Alzheimers Disease
CNS & Neurological Disorders - Drug Targets Significant Correlation between Cystatin C, Cerebral Infarction, and Potential Biomarker for Increased Risk of Stroke
Current Neurovascular Research Role of Renin Angiotensin System Inhibitors in Cardiovascular and Renal Protection: A Lesson from Clinical Trials
Current Pharmaceutical Design Age-Related Neurodegeneration Prevention Through mTOR Inhibition: Potential Mechanisms and Remaining Questions
Current Topics in Medicinal Chemistry An Approach to Diabetic Ketoacidosis in an Emergency Setting
Reviews on Recent Clinical Trials Metastatic Breast Cancer, Organotropism and Therapeutics: A Review
Current Cancer Drug Targets Current State of Development of Genome Analysis in Livestock
Current Genomics Poly(ADP-Ribose) Polymerase Inhibitors: New Pharmacological Functions and Potential Clinical Implications
Current Pharmaceutical Design Recent Patents on the Upgrading of Fish by-Products
Recent Patents on Chemical Engineering Biomaterials and Supercritical Fluid Technologies: Which Perspectives to Fabricate Artificial Extracellular Matrix?
Current Pharmaceutical Design Biological Activities of Yarrow Species (Achillea spp.)
Current Pharmaceutical Design New Applications of Oleanolic Acid and its Derivatives as Cardioprotective Agents: A Review of their Therapeutic Perspectives
Current Pharmaceutical Design The Role of Inflammatory and Cytokine Biomarkers in the Pathogenesis of Frailty Syndrome
Endocrine, Metabolic & Immune Disorders - Drug Targets Development and Validation of a Fluorescence-Based HTS Assay for the Identification of P/Q-Type Calcium Channel Blockers
Combinatorial Chemistry & High Throughput Screening Purification and Characterization of a Novel Anti-Proliferative Lectin from Morus alba L. Leaves
Protein & Peptide Letters Gastrointestinal Immune System and Brain Dialogue Implicated in Neuroinflammatory and Neurodegenerative Diseases
Current Molecular Medicine Long-Chain Omega-3 Fatty Acid Deficiency in Mood Disorders: Rationale for Treatment and Prevention
Current Drug Discovery Technologies COVID Tarnish Lung: Residual Radiological Lung Consequences of Infection with COVID-19
Current Respiratory Medicine Reviews