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Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
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Recent advances in cancer therapeutics
Nicola Chessum1, Keith Jones1, Elisa Pasqua1
1Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom.
Progress in Medicinal Chemistry
|March 3, 2015
Summary
Cancer treatment is shifting from cytotoxic drugs to targeted therapies like imatinib, aiming for efficacy with lower toxicity. Medicinal chemistry advances drive novel oncology drug discovery in areas such as kinase and chaperone inhibitors.
Area of Science:
- Oncology
- Medicinal Chemistry
- Drug Discovery
Background:
- Cancer therapeutics have shifted from traditional cytotoxic drugs to targeted therapies.
- Imatinib, a kinase inhibitor, exemplifies this paradigm shift, targeting specific cancer-driving proteins.
- The goal is to achieve high efficacy with reduced toxicity.
Purpose of the Study:
- To review advancements in targeted cancer therapeutics.
- To highlight novel approaches in medicinal chemistry for oncology drug discovery.
- To focus on four key areas: chaperone inhibitors, kinase inhibitors, histone deacetylase inhibitors, and protein-protein interaction inhibitors.
Main Methods:
- Review of approved drugs and clinical trials in selected therapeutic areas.
- Emphasis on high-throughput screening, fragment-based screening, and structure-based design.
- Exploration of selectivity, pharmacokinetic optimization, and pharmacodynamic biomarker modulation.
Main Results:
- Imatinib demonstrates impressive survival improvements in chronic myeloid leukemia patients.
- Selected areas showcase newer approaches and novel aspects of medicinal chemistry in cancer treatment.
- Compounds in these areas are either approved drugs or in clinical trials.
Conclusions:
- Targeted therapies represent a significant advancement in cancer treatment.
- Medicinal chemistry plays a crucial role in developing effective and less toxic cancer drugs.
- Continued innovation in drug discovery is essential for improving patient outcomes.
Keywords:
Cancer therapeuticsChaperonesEpigeneticsHistone deacetylasesKinase inhibitorsPersonalised medicineProtein–protein interactionsMore Related Videos
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