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Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Cancer02:18

Cancer

Cancers arise due to mutations in genes involved in the regulation of cell division, which leads to unrestricted cell proliferation. Modern science and medicine have made great strides in the understanding and treatment of cancer, including eradicating cancer in some patients. However, there is still no cure for cancer. This is largely due to the fact that cancer is a large group of many diseases.
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
Treatment Resistent Cancers02:56

Treatment Resistent Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...

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Related Experiment Video

Updated: Jul 12, 2026

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation
15:04

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation

Published on: January 19, 2019

An update on DOT1LWT/MUT modulators as a promising anticancer strategy.

Xue Fan1, Shuyu Liu1, Luyao Wang1

  • 1Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.

Bioorganic & Medicinal Chemistry
|July 9, 2026
PubMed
Summary

Disruptor of telomeric silencing 1-like (DOT1L) is a key enzyme in diseases like leukemia and lung cancer. This review covers DOT1L inhibitors and novel strategies for developing targeted cancer therapies.

Keywords:
Allosteric inhibitorAnticancerDOT1LOrthosteric inhibitor“Induced-fit” allosteric model

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Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence
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Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence

Published on: January 7, 2019

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Last Updated: Jul 12, 2026

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation
15:04

Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation

Published on: January 19, 2019

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence
10:09

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence

Published on: January 7, 2019

Area of Science:

  • Biochemistry and Molecular Biology
  • Cancer Research
  • Drug Discovery

Background:

  • Disruptor of telomeric silencing 1-like (DOT1L) is the sole H3K79 methyltransferase, crucial in various disease pathologies.
  • DOT1L dysregulation is implicated in leukemogenesis and lung carcinogenesis, making it a significant therapeutic target.

Purpose of the Study:

  • To provide a comprehensive overview of DOT1L structure, signaling pathways, and associated diseases.
  • To summarize recent advancements in DOT1L inhibitor development, including orthosteric and allosteric strategies.
  • To introduce emerging therapeutic modalities targeting DOT1L, such as PPI inhibitors and PROTACs.

Main Methods:

  • Structural analysis of wild-type (WT) and mutant DOT1L.
  • Review of signaling pathways and disease associations.
  • Analysis of inhibitor design strategies based on the "Induced-fit" allosteric model.

Main Results:

  • Detailed examination of DOT1L structural features and their implications in disease.
  • Summary of current orthosteric and allosteric DOT1L inhibitors.
  • Introduction to novel therapeutic approaches like PPI inhibitors and PROTACs.

Conclusions:

  • DOT1L remains a promising target for cancer therapy.
  • Advances in inhibitor design and emerging strategies offer new avenues for drug development.
  • Further research is needed to overcome challenges and develop next-generation DOT1L-targeted therapeutics.