Related Experiment Video

Updated: Sep 25, 2025

Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures
07:48

Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures

Published on: December 26, 2016

11.5K

Targeting allosteric regulation of cancer metabolism

Daniel M Kremer1,2,3, Costas A Lyssiotis4,5,6

  • 1Department of Molecular & Integrative Physiology, University of Michigan, Ann Arbor, MI, USA.

Nature Chemical Biology
|April 28, 2022
PubMed

Insights

Cancer cells reprogram metabolism, offering therapeutic targets. Allosteric modulation of metabolic enzymes with small molecules presents a promising strategy for developing novel cancer drugs by exploiting these tumor-specific vulnerabilities.

Area of Science:

  • Oncology
  • Biochemistry
  • Pharmacology

Background:

  • Metabolic reprogramming is a hallmark of all cancer types.
  • Targeting cancer metabolism is a validated strategy for chemotherapy.
  • Recent research has elucidated tumor-specific metabolic pathways and vulnerabilities.

Purpose of the Study:

  • To highlight allosteric modulation of metabolic enzymes as a key mechanism for small-molecule cancer drugs.
  • To discuss mechanistic insights and achievements in targeting cancer metabolism using this approach.
  • To review technological advancements in discovering allosteric modulators.

Main Methods:

  • Review of contemporary research on cancer metabolism and small-molecule drug development.
  • Focus on allosteric modulation as a mechanism of action for targeting metabolic enzymes.
  • Discussion of mechanistic studies and technological advances in drug discovery.

Main Results:

  • Allosteric modulation offers an attractive mechanism for developing selective small-molecule inhibitors of metabolic enzymes.
  • Application of allosteric modulators has yielded significant insights into cancer metabolism and therapeutic strategies.
  • Technological progress is enhancing the discovery of novel allosteric modulators for cancer treatment.

Conclusions:

  • Targeting metabolic reprogramming via allosteric modulation of enzymes is a viable strategy in oncology.
  • Continued advancements in drug discovery technologies will accelerate the development of these targeted therapies.
  • Exploiting tumor-specific metabolic vulnerabilities through allosteric modulators holds promise for future cancer treatments.

More Related Videos

Assessment of the Metabolic Profile of Primary Leukemia Cells06:21

Assessment of the Metabolic Profile of Primary Leukemia Cells

Published on: November 21, 2018

10.6K
Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer06:51

Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer

Published on: July 21, 2018

18.1K

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...
7.9K
Regulation of Metabolism01:19

Regulation of Metabolism

Cellular needs and conditions vary from cell to cell and change within individual cells over time. For example, the required enzymes and energetic demands of stomach cells are different from those of fat storage cells, skin cells, blood cells, and nerve cells. Furthermore, a digestive cell works much harder to process and break down nutrients during the time that closely follows a meal compared with many hours after a meal. As these cellular demands and conditions vary, so do the amounts and...
10.0K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
3.9K
Adaptive Mechanisms in Cancer Cells02:53

Adaptive Mechanisms in Cancer Cells

Cancer cells accumulate genetic changes at an abnormally rapid rate due to the defects in the DNA repair mechanisms. From an evolutionary perspective, such genetic instability is advantageous for cancer development. Mutant cell lines accumulate a series of beneficial mutations that contribute to their progression into cancer.
Some of the advantages that cancer cells have on normal cells include - enhanced ability to divide without terminally differentiating, induce new blood vessel formation,...
6.0K
Allosteric Regulation01:08

Allosteric Regulation

Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
59.5K
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...
5.1K