Abstract
Over the past decade, fragment-based drug discovery has developed significantly and has gained increasing popularity in the pharmaceutical industry as a powerful alternative and complement to traditional high-throughput screening approaches for hit identification. Fragment-based methods are capable of rapidly identifying starting points for structure-based drug design from relatively small libraries of low molecular weight compounds. The main constraints are the need for sensitive methods that can reliably detect the typically weak interactions between fragments and the target protein, and strategies for transforming fragments into higher molecular weight drug candidates. This approach has recently been validated as series of compounds from various programs have entered clinical trials.
Keywords: Fragment screening, Ligand efficiency, Drug discovery, Cancer, high-throughput screening (HTS), Crystallography, fluorimetry, Phosphoinositide-Dependent Kinase-1 (PDK1), Anti-cancer, Cyclindependent kinase (CDK)
Anti-Cancer Agents in Medicinal Chemistry
Title: Targeting Cancer Using Fragment Based Drug Discovery
Volume: 12 Issue: 1
Author(s): Andrew P. Turnbull and Susan M. Boyd
Affiliation:
Keywords: Fragment screening, Ligand efficiency, Drug discovery, Cancer, high-throughput screening (HTS), Crystallography, fluorimetry, Phosphoinositide-Dependent Kinase-1 (PDK1), Anti-cancer, Cyclindependent kinase (CDK)
Abstract: Over the past decade, fragment-based drug discovery has developed significantly and has gained increasing popularity in the pharmaceutical industry as a powerful alternative and complement to traditional high-throughput screening approaches for hit identification. Fragment-based methods are capable of rapidly identifying starting points for structure-based drug design from relatively small libraries of low molecular weight compounds. The main constraints are the need for sensitive methods that can reliably detect the typically weak interactions between fragments and the target protein, and strategies for transforming fragments into higher molecular weight drug candidates. This approach has recently been validated as series of compounds from various programs have entered clinical trials.
Export Options
About this article
Cite this article as:
P. Turnbull Andrew and M. Boyd Susan, Targeting Cancer Using Fragment Based Drug Discovery, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (1) . https://dx.doi.org/10.2174/187152012798764660
DOI https://dx.doi.org/10.2174/187152012798764660 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Aluminum Vaccine Adjuvants: Are they Safe?
Current Medicinal Chemistry Stem Cell Transplant and Idiotypic Vaccination for B-Cell Malignancies
Current Topics in Medicinal Chemistry Substance Abuse, HIV-1 and Hepatitis
Current HIV Research Recent Clinical Trials of mTOR-Targeted Cancer Therapies
Reviews on Recent Clinical Trials Recent Advances in the Design and Synthesis of Prednisolone and Methylprednisolone Conjugates
Current Pharmaceutical Design Targeting CREB for Cancer Therapy: Friend or Foe
Current Cancer Drug Targets Resistance to Crizotinib in Advanced Non-Small Cell Lung Cancer (NSCLC) with ALK Rearrangement: Mechanisms, Treatment Strategies and New Targeted Therapies
Current Clinical Pharmacology Editorial:
Current Immunology Reviews (Discontinued) Antiangiogenic Therapies in Non-Hodgkin's Lymphoma
Current Cancer Drug Targets Towards Improved Therapies Using Nanopharmaceuticals: Recent Patents on Pharmaceutical Nanoformulations
Recent Patents on Food, Nutrition & Agriculture CXCR4 and Glioblastoma
Anti-Cancer Agents in Medicinal Chemistry Targeting Heme for the Identification of Cytotoxic Agents
Anti-Cancer Agents in Medicinal Chemistry Rheb/mTOR Activation and Regulation in Cancer: Novel Treatment Strategies beyond Rapamycin
Current Drug Targets Bladder Cancer: A Simple Model Becomes Complex
Current Genomics Mechanism of Action of Flavonoids in Prevention of Inflammation- Associated Skin Cancer
Current Medicinal Chemistry Pleiotropic Effect of Mahanine and Girinimbine Analogs: Anticancer Mechanism and its Therapeutic Versatility
Anti-Cancer Agents in Medicinal Chemistry Epigenetics in Vascular Disease – Therapeutic Potential of New Agents
Current Vascular Pharmacology Mechanism of Cancer Drug Resistance and the Involvement of Noncoding RNAs
Current Medicinal Chemistry Resveratrol and Cancer Treatment: Is Hormesis a Yet Unsolved Matter?
Current Pharmaceutical Design The Role of Hesperidin in Cell Signal Transduction Pathway for the Prevention or Treatment of Cancer
Current Medicinal Chemistry