Abstract
This review mainly covers last five year literature on CCK1R agonists and antagonists. These CCK1R ligands have been found following the two usual and complementary strategies for drug discovery: rational design based on structure activity relationships on the CCK-7 and CCK-4 peptide sequences of the endogenous ligands and random screening of diverse compounds, followed by hit optimization. The first group includes: chimeric bifunctional opioid/CCK peptides, designed as opioid agonists with balanced CCK1R/CCK2R antagonist activity for the treatment of neuropathic pain, antagonist and agonist dipeptoids, and 1,3-dioxoperhydropyrido[1,2-c]pyrimidine- and anthranilic acidbased antagonists. Among the ligands derived from random screening, a few new 1,4-benzodiazepine-, 1,5- benzodiazepine-, and five member ring heterocycle-based CCK1R ligands have been reported. Finally, taking into account the importance of receptor mapping studies for ligand optimization and future precise de novo receptor structurebased design of new selective and more effective ligands, the most significant conclusions of these studies have also been reviewed.
Keywords: CCK1R ligands, peptidomimetics, Dipeptoids, Anthranilic Acid, 1,5-benzodiazepine
Current Topics in Medicinal Chemistry
Title: Strategies for Design of Non Peptide CCK1R Agonist/Antagonist Ligands
Volume: 7 Issue: 12
Author(s): M. Teresa Garcia-Lopez, Rosario Gonzalez-Muniz, Mercedes Martin-Martinez and Rosario Herranz
Affiliation:
Keywords: CCK1R ligands, peptidomimetics, Dipeptoids, Anthranilic Acid, 1,5-benzodiazepine
Abstract: This review mainly covers last five year literature on CCK1R agonists and antagonists. These CCK1R ligands have been found following the two usual and complementary strategies for drug discovery: rational design based on structure activity relationships on the CCK-7 and CCK-4 peptide sequences of the endogenous ligands and random screening of diverse compounds, followed by hit optimization. The first group includes: chimeric bifunctional opioid/CCK peptides, designed as opioid agonists with balanced CCK1R/CCK2R antagonist activity for the treatment of neuropathic pain, antagonist and agonist dipeptoids, and 1,3-dioxoperhydropyrido[1,2-c]pyrimidine- and anthranilic acidbased antagonists. Among the ligands derived from random screening, a few new 1,4-benzodiazepine-, 1,5- benzodiazepine-, and five member ring heterocycle-based CCK1R ligands have been reported. Finally, taking into account the importance of receptor mapping studies for ligand optimization and future precise de novo receptor structurebased design of new selective and more effective ligands, the most significant conclusions of these studies have also been reviewed.
Export Options
About this article
Cite this article as:
M. Teresa Garcia-Lopez , Rosario Gonzalez-Muniz , Mercedes Martin-Martinez and Rosario Herranz , Strategies for Design of Non Peptide CCK1R Agonist/Antagonist Ligands, Current Topics in Medicinal Chemistry 2007; 7 (12) . https://dx.doi.org/10.2174/156802607780960537
DOI https://dx.doi.org/10.2174/156802607780960537 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
- Announcements
Related Articles
-
Modulation of Doxorubicin Mediated Growth Inhibition of Hepatocellular Carcinoma Cells by Platelet Lysates
Anti-Cancer Agents in Medicinal Chemistry Bioactive Cyclohexenones: A Mini Review
Current Bioactive Compounds Multiple Myeloma and the Immune Microenvironment
Current Cancer Drug Targets Functionalized Nanocarriers for Enhanced Bioactive Delivery to Squamous Cell Carcinomas: Targeting Approaches and Related Biopharmaceutical Aspects
Current Pharmaceutical Design Recent Advances in the Synthesis of 1,3-Azoles
Current Topics in Medicinal Chemistry Antigenic Differences Between Normal and Malignant Cells as a Basis for Treatment of Intracerebral Neoplasms Using a DNA-Based Vaccine
Current Genomics Antibody Engineering for Targeted Therapy of Cancer Recombinant Fv-Immunotoxins
Current Pharmaceutical Biotechnology Natural Products Derived from Traditional Chinese Medicine as Novel Inhibitors of the Epidermal Growth Factor Receptor
Combinatorial Chemistry & High Throughput Screening Strategies for Increasing the Solubility and Bioavailability of Anticancer Compounds: β-Lapachone and Other Naphthoquinones
Current Pharmaceutical Design ADAM Metalloproteinases as Potential Drug Targets
Current Medicinal Chemistry Micro-RNA in Disease and Gene Therapy
Current Drug Discovery Technologies CETUXIMAB: From Bench to Bedside
Current Cancer Drug Targets Alternative Splicing in Chronic Myeloid Leukemia (CML): A Novel Therapeutic Target?
Current Cancer Drug Targets Mammalian Cell Competitions, Cell-in-Cell Phenomena and Their Biomedical Implications.
Current Molecular Medicine Magnetic Resonance Imaging of the Cervix, and its Relevance to the Revised International Federation of Gynecology and Obstetrics (FIGO) Staging
Current Medical Imaging NCRNA Combined Therapy as Future Treatment Option for Cancer
Current Pharmaceutical Design Preface [ Hot Topic: Radiation Oncology as Mainstay of Modern Cancer Medicine (Guest Editors: Claus Belka & Verena Jendrossek)]
Current Medicinal Chemistry - Anti-Cancer Agents Neuropilin and Neuropilin Associated Molecules as New Molecular Targets in Pancreatic Adenocarcinoma
Anti-Cancer Agents in Medicinal Chemistry Genetics of Cancer Susceptibility
Current Genomics Single-cell Sequencing in the Field of Stem Cells
Current Genomics