Related Experiment Video

Updated: Jan 15, 2026

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
09:19

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo

Published on: February 6, 2015

9.1K

BRITE-338733: From RecA inhibition to cancer treatment

Tiyyaba Furqan1, Amira Bekdash1, Jisha Chalissery1

  • 1Department of Biochemistry and Molecular Biology, College of Medicine and Health Sciences, United Arab Emirates University, P.O. Box: 15551, Al Ain, United Arab Emirates.

European Journal of Medicinal Chemistry
|October 11, 2025
PubMed

Insights

Researchers identified BRITE-338733 as a novel inhibitor of the RSC chromatin remodeler. This compound shows potential as an anticancer therapeutic due to its DNA binding and cancer cell cytotoxicity.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • ATP-dependent chromatin remodelers regulate cellular processes by altering chromatin structure.
  • The ATPase domains of these remodelers are underexplored therapeutic targets.

Purpose of the Study:

  • To computationally identify and experimentally validate novel inhibitors of the RSC chromatin remodeler's ATP hydrolysis activity.
  • To target the ATP binding pocket and/or DNA interaction sites.

Main Methods:

  • Computational screening using docking studies.
  • Molecular dynamics simulations to analyze compound behavior.
  • Experimental validation using ATP hydrolysis assays.
  • DNA binding affinity assessment.
  • In vitro cytotoxicity assays against breast cancer cells.

Main Results:

  • BRITE-338733 was identified as the most promising inhibitor candidate through computational analysis.
  • Experimental assays confirmed significant inhibition of ATP hydrolysis by BRITE-338733.
  • BRITE-338733 demonstrated strong binding to DNA.
  • The compound exhibited cytotoxicity against breast cancer cells.

Conclusions:

  • BRITE-338733 is a potent inhibitor of the RSC chromatin remodeler.
  • BRITE-338733's ability to bind DNA and its cytotoxicity suggest potential as an anticancer therapeutic.
Keywords:
ATPase activityCancerChromatin remodelerCytotoxicityDNA bindingEnsemble molecular dynamics simulationsIntercalationMolecular dockingRSCSWI/SNF

More Related Videos

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics06:00

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics

Published on: May 14, 2016

11.4K
Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down08:59

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down

Published on: December 11, 2017

7.6K

Related Concept Videos

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...
5.5K
Treatment Resistant Cancers02:56

Treatment Resistant 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...
3.7K
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...
8.6K
Receptor Downregulation in MVBs01:15

Receptor Downregulation in MVBs

Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that  lead to cell proliferation, migration, and differentiation. Overexpression of EGFR  stimulates cells to proliferate. Excessive  EGFR...
2.8K
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...
9.8K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
7.7K