Abstract
Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with intresting results both in vitro and in vivo.
Keywords: Ser/Thr kinase inhibitors, ATP non-competitive, anticancer drugs, drug discovery
Anti-Cancer Agents in Medicinal Chemistry
Title: ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents
Volume: 9 Issue: 7
Author(s): Giorgio Cozza, Andrea Bortolato, Ernesto Menta, Ennio Cavalletti, Silvano Spinelli and Stefano Moro
Affiliation:
Keywords: Ser/Thr kinase inhibitors, ATP non-competitive, anticancer drugs, drug discovery
Abstract: Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with intresting results both in vitro and in vivo.
Export Options
About this article
Cite this article as:
Cozza Giorgio, Bortolato Andrea, Menta Ernesto, Cavalletti Ennio, Spinelli Silvano and Moro Stefano, ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (7) . https://dx.doi.org/10.2174/187152009789056930
DOI https://dx.doi.org/10.2174/187152009789056930 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- 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
-
Role of Curcumin in Modulating Plasma PON1 Arylesterase Activity and Susceptibility to LDL Oxidation in Oxidatively Challenged Wistar Rats
Letters in Drug Design & Discovery Antioxidative Activity, Polyphenolic Content and Anti-Glycation Effect of Some Thai Medicinal Plants Traditionally Used in Diabetic Patients
Medicinal Chemistry QT Prolongation and Anticancer Drugs: Is it a Cardiologist’s Worry? The Oncologist’s Point of View
Reviews on Recent Clinical Trials Cholesterol Ester Transfer Protein (CETP), Postprandial Lipemia and Hypolipidemic Drugs
Current Medicinal Chemistry Deciphering Role of Cytokines for Therapeutic Strategies Against Rheumatoid Arthritis
Current Drug Targets Inhibitors of Mammalian Acetyl-CoA Carboxylase
Recent Patents on Cardiovascular Drug Discovery Incretin-based Therapies for Type 2 Diabetes Mellitus: Effects on Insulin Resistance
Current Diabetes Reviews Role of Heme Oxygenases in Cardiovascular Syndromes and Co-morbidities
Current Pharmaceutical Design Vitamin A and Diabesity: New Insight for Drug Discovery
Mini-Reviews in Medicinal Chemistry Antihypertensive Drug Treatment and Circadian Blood Pressure Rhythm: A Review of the Role of Chronotherapy in Hypertension
Current Pharmaceutical Design Dual Modulation of Vascular Function by Perivascular Adipose Tissue and Its Potential Correlation with Adiposity/Lipoatrophy-Related Vascular Dysfunction
Current Pharmaceutical Design Evaluation of the Possible Contribution of Antioxidants Administration in Metabolic Syndrome
Current Pharmaceutical Design Association of Lower Adiponectin Plasma Levels, Increased Age and Smoking with Subclinical Atherosclerosis in Patients with HIV-1 Infection
Current HIV Research Dyslipidaemia Related to Insulin Resistance and Cardiovascular Disease in South Asian and West African Populations
Current Pharmaceutical Design Subject Index to Volume 3
Current Gene Therapy What Changes we may Expect in 2010 Hypertension Diagnosis and Management: Insights from the European Update Document
Current Vascular Pharmacology Mitochondrial Aldehyde Dehydrogenase, A Potential Drug Target for Protection of Heart and Brain from Ischemia/Reperfusion Injury
Current Drug Targets Metabolomic and Imaging: A Literature Review
Current Medical Imaging Post-stroke Depression Therapy: Where are we now?
Current Neurovascular Research Synthesis, Single Crystal Study, in silico Analysis, in vitro Antiinflammatory and Anticancer Activities of 7-hydroxy-14H-naphtho[2,3- a]phenothiazine-8,13-dione
Drug Delivery Letters