Abstract
Farnesyl Protein Transferase as a target for therapeutic intervention is currently under investigation in human clinical trials. Sch-66336 (sarasar®), a benzocycloheptapyridyl Farnesyl Transferase Inhibitor (FTI), has been found to be effective in cellular proliferation assays and in in vivo oncology models both as a single agent and in combination with other anti-cancer agents. Clinically, early evidence is being generated that suggests efficacy in humans, particularly in patients with leukemia. Herein, we review the biology of FPT, the discovery of Sch-66336 and other benzocycloheptapyridyl FTIs, and the clinical evaluation of Sch-66336 for the treatment of leukemia and solid tumors.
Keywords: Sch-66336, Benzocycloheptapyridyl Farnesyl Protein, anti-cancer agents
Current Topics in Medicinal Chemistry
Title: Sch-66336 (Sarasar®) and Other Benzocycloheptapyridyl Farnesyl Protein Transferase Inhibitors: Discovery, Biology and Clinical Observations
Volume: 3 Issue: 10
Author(s): Arthur G. Taveras, Paul Kirschmeier and Charles M. Baum
Affiliation:
Keywords: Sch-66336, Benzocycloheptapyridyl Farnesyl Protein, anti-cancer agents
Abstract: Farnesyl Protein Transferase as a target for therapeutic intervention is currently under investigation in human clinical trials. Sch-66336 (sarasar®), a benzocycloheptapyridyl Farnesyl Transferase Inhibitor (FTI), has been found to be effective in cellular proliferation assays and in in vivo oncology models both as a single agent and in combination with other anti-cancer agents. Clinically, early evidence is being generated that suggests efficacy in humans, particularly in patients with leukemia. Herein, we review the biology of FPT, the discovery of Sch-66336 and other benzocycloheptapyridyl FTIs, and the clinical evaluation of Sch-66336 for the treatment of leukemia and solid tumors.
Export Options
About this article
Cite this article as:
Taveras G. Arthur, Kirschmeier Paul and Baum M. Charles, Sch-66336 (Sarasar®) and Other Benzocycloheptapyridyl Farnesyl Protein Transferase Inhibitors: Discovery, Biology and Clinical Observations, Current Topics in Medicinal Chemistry 2003; 3 (10) . https://dx.doi.org/10.2174/1568026033452104
DOI https://dx.doi.org/10.2174/1568026033452104 |
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
-
New and Highly Potent Antitumor Natural Products from Marine-Derived Fungi: Covering the Period from 2003 to 2012
Current Topics in Medicinal Chemistry Proton Ion-Microbeam Elemental Analysis for Inhaled Particle-Induced Pulmonary Diseases: Application for Diagnosis and Assessment of Progression
Current Medicinal Chemistry The Rational Design of Anticancer Platinum Complexes: The Importance of the Structure-Activity Relationship
Current Medicinal Chemistry Cancer Gene Therapy by Adenovirus-Mediated Gene Transfer
Current Gene Therapy The Medical Potential of Antimicrobial Peptides from Insects
Current Topics in Medicinal Chemistry Gefitinib Targets EGFR Dimerization and ERK1/2 Phosphorylation to Inhibit Pleural Mesothelioma Cell Proliferation
Current Cancer Drug Targets Aptamers: Molecular Tools for Medical Diagnosis
Current Topics in Medicinal Chemistry Predicting Targeted Polypharmacology for Drug Repositioning and Multi- Target Drug Discovery
Current Medicinal Chemistry Epigenetics of Virus-Induced Tumors: Perspectives for Therapeutic Targeting
Current Pharmaceutical Design The Chemistry and Bio-Medicinal Significance of Pyrimidines & Condensed Pyrimidines
Current Topics in Medicinal Chemistry Novel Marine-Derived Anti-Cancer Agents
Current Pharmaceutical Design Phosphoinositide-3-kinases as the Novel Therapeutic Targets for the Inflammatory Diseases: Current and Future Perspectives
Current Drug Targets The Role of Pemetrexed in Lung Adenocarcinoma, Mixed Subtype with Bronchioloalveolar Carcinoma Features
Current Drug Targets Gene Silencing in the Development of Personalized Cancer Treatment: The Targets, the Agents and the Delivery Systems
Current Gene Therapy Circulating Levels of Soluble Angiogenic Factors in Multiple Myeloma: Correlation with Parameters of Disease Activity and Prognosis
Current Angiogenesis (Discontinued) C-KIT Signaling in Cancer Treatment
Current Pharmaceutical Design Interferon Therapy in Lung Cancer: Current Perspectives
Current Cancer Therapy Reviews TEM8 Targeted Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Investigating the In Vivo Expression Patterns of miR-7 microRNA Family Members in the Adult Mouse Brain
MicroRNA Potential Applications of FDG-PET/CT in COPD: A Review of the Literature
Current Molecular Imaging (Discontinued)