Abstract
The synthesis and proteolytic inhibitor function of two new tetrapeptides, MeOSuc-Ala-Pro-Ala-Val-CH2Cl (APAV) and MeOSuc-Ala-Pro-Ala-Leu-CH2Cl (APAL) are described. An examination of inhibitory activity using a realtime reverse transcription-polymerase chain reaction (RT-PCR) assay in the presence of proteinase K reveals that the APAL at a concentration of 0.5 mM allows a signal to be obtained for an exogenous target (“Xeno RNA”) at 29 cycles (i.e Ct = 29), whereas the MeOSuc-Ala-Ala-Pro-Val-CH2Cl (AAPV) control requires a 2-fold lower concentration (0.25 mM) to produce the same Ct. The other new analog APAV does not provide proteinase K inhibition under the same experimental conditions.
Keywords: Chloromethyl ketones, tetrapeptides, proteinase K inhibitor, serine protease, real-time RT-PCR
Letters in Organic Chemistry
Title: Synthesis and Application of New Rearranged Tetrapeptidyl Chloromethyl Ketones as Potent Proteinase K Inhibitor
Volume: 8 Issue: 1
Author(s): Anilkumar R. Kore, Muthian Shanmugasundaram and Irudaya Charles
Affiliation:
Keywords: Chloromethyl ketones, tetrapeptides, proteinase K inhibitor, serine protease, real-time RT-PCR
Abstract: The synthesis and proteolytic inhibitor function of two new tetrapeptides, MeOSuc-Ala-Pro-Ala-Val-CH2Cl (APAV) and MeOSuc-Ala-Pro-Ala-Leu-CH2Cl (APAL) are described. An examination of inhibitory activity using a realtime reverse transcription-polymerase chain reaction (RT-PCR) assay in the presence of proteinase K reveals that the APAL at a concentration of 0.5 mM allows a signal to be obtained for an exogenous target (“Xeno RNA”) at 29 cycles (i.e Ct = 29), whereas the MeOSuc-Ala-Ala-Pro-Val-CH2Cl (AAPV) control requires a 2-fold lower concentration (0.25 mM) to produce the same Ct. The other new analog APAV does not provide proteinase K inhibition under the same experimental conditions.
Export Options
About this article
Cite this article as:
R. Kore Anilkumar, Shanmugasundaram Muthian and Charles Irudaya, Synthesis and Application of New Rearranged Tetrapeptidyl Chloromethyl Ketones as Potent Proteinase K Inhibitor, Letters in Organic Chemistry 2011; 8 (1) . https://dx.doi.org/10.2174/157017811794557895
DOI https://dx.doi.org/10.2174/157017811794557895 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Oxidative Stress and Cardiovascular Aging: Interaction Between NRF-2 and ADMA
Current Cardiology Reviews Editorial (Thematic Issue: “Heterocycle and Hydrocarbon Compounds from Natural Sources in Medicinal Chemistry: From Synthesis to Computational Design in Pharmacological Applications” – Part 1)
Current Topics in Medicinal Chemistry Melatonin in Cardiac Ischemia/Reperfusion-Induced Mitochondrial Adaptive Changes
Cardiovascular & Hematological Disorders-Drug Targets Endocannabinoid System: Emerging Role from Neurodevelopment to Neurodegeneration
Mini-Reviews in Medicinal Chemistry Mitochondrion of Protozoan Parasite Emerges as Potent Therapeutic Target:Exciting Drugs are on the Horizon
Current Pharmaceutical Design TakoTsubo Cardiomyopathy A Short Review
Current Cardiology Reviews A Review of Cilostazol, a Phosphodiesterase Inhibitor, and its Role in Preventing Both Coronary and Peripheral Arterial Restenosis Following Endovascular Therapy
Recent Patents on Cardiovascular Drug Discovery Somatostatin: A Hormone for the Heart?
Current Vascular Pharmacology Hemolysis-Associated Pulmonary Hypertension in Sickle Cell Disease: Global Disruption of the Arginine-Nitric Oxide Pathway
Current Hypertension Reviews Editorial [Hot Topic:Active and Passive Aβ-Immunotherapy: Preclinical and Clinical Studies and Future Directions: Part I (Guest Editors: Michael G. Agadjanyan and David H. Cribbs)]
CNS & Neurological Disorders - Drug Targets Beyond Physical Exercise: The Role of Nutrition, Gut Microbiota and Nutraceutical Supplementation in Reducing Age-Related Sarcopenia
Current Aging Science Colchicine: An Old Wine in a New Bottle?
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Effect of Aluminium Chloride Concentration on Diltiazem Hydrochloride Release from pH-sensitive Hydrogel Beads Composed of Hydrolyzed Grafted k-Carrageenan and Sodium Alginate
Current Chemical Biology WITHDRAWN: Current Trends in the Detection of Biological Proteins and Immunological Assays using Graphene Quantum Dots
Current Analytical Chemistry Defective Insulin Signalling, Mediated by Inflammation, Connects Obesity to Alzheimer Disease; Relevant Pharmacological Therapies and Preventive Dietary Interventions
Current Alzheimer Research Apolipoprotein A-I Mimetic Peptides for the Treatment of Coronary Artery Disease
Current Cardiology Reviews Recent Advances in Progressive Supranuclear Palsy: A Review
Current Alzheimer Research The Metabolism of Methazolamide in Immortalized Human Keratinocytes, HaCaT Cells
Drug Metabolism Letters Models for the Study of Angiogenesis
Current Pharmaceutical Design Pathophysiology of Hypertension During Preeclampsia: Role of Inflammatory Cytokines
Current Hypertension Reviews