Targeted small molecule therapy and inhibitors for lymphoma

Zhong-Hui Wang1, Xiang Zheng1, Guo-Wu Rao1

  • 1College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, P. R. China.

PubMed

Insights

Targeted therapies, including inhibitors of Histone deacetylase (HDAC), Bruton

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Lymphoma is the ninth most common cancer globally as of 2020.
  • Targeted inhibition represents a key therapeutic strategy for lymphoma treatment.
  • Histone deacetylase (HDAC), Bruton's tyrosine kinase (BTK), and phosphoinositide 3-kinase (PI3K) are crucial in tumor development and are promising targets.

Purpose of the Study:

  • To review the role of HDAC, BTK, and PI3K in tumorigenesis.
  • To discuss the mechanism of action, structure-activity relationships, and clinical research of small molecule inhibitors targeting these proteins.
  • To offer novel therapeutic insights for lymphoma treatment.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Analysis of the molecular mechanisms of targeted inhibitors.
  • Synthesis of structure-activity relationship data for small molecule inhibitors.

Main Results:

  • HDAC, BTK, and PI3K are validated targets in various cancers, including lymphoma.
  • Several small molecule inhibitors targeting these pathways have demonstrated efficacy and safety in clinical studies.
  • Understanding structure-activity relationships aids in the development of more potent and selective inhibitors.

Conclusions:

  • Targeted inhibition of HDAC, BTK, and PI3K offers a promising avenue for lymphoma treatment.
  • Continued research into small molecule inhibitors is essential for advancing lymphoma therapy.
  • This review provides a foundation for developing new treatment strategies for lymphoma.

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...
7.5K
Tumor Immunotherapy01:27

Tumor Immunotherapy

Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
504
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
4.9K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
4.7K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
6.1K
Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
7.6K