Enzymes/transporters

Regine Garcia Boy1, Eva-Maria Knapp, Michael Eisenhut

  • 1Abteilung für Nuklearmedizin, Universitätsklinikum Heidelberg, Im Neuenheimer Feld 400, 69120 Heidelberg, Germany. r.garcia@med.uni-heidelberg.de

Insights

Developing targeted tracers is crucial for cancer diagnosis and monitoring treatment response. Researchers are focusing on enzymes and transporters, which are often altered in tumors, for effective molecular imaging strategies.

Area of Science:

  • Oncology
  • Molecular Imaging
  • Biochemistry

Background:

  • Tumor-specific targets for diagnostic tracers are rare due to similarities between cancer and normal cells.
  • Malignant transformation involves altered expression of enzymes and transporters critical for tumor growth.
  • Molecular imaging relies on tracers targeting these over-expressed enzymes and transporters.

Purpose of the Study:

  • To highlight the importance of developing specific tracers for cancer diagnosis and chemotherapy monitoring.
  • To discuss the potential of targeting enzymes and transporters for molecular imaging in oncology.

Main Methods:

  • Review of current strategies in molecular imaging for cancer.
  • Identification of key enzymes and transporters as potential targets for tracer development.

Main Results:

  • Enzymes and transporters are frequently dysregulated during cancer development.
  • Targeting these dysregulated molecules offers a promising avenue for tumor-specific imaging.

Conclusions:

  • Targeted tracers exploiting altered enzyme and transporter expression are essential for advancing cancer diagnosis and treatment assessment.
  • Glucose transporters, multi-drug resistance transporters (MDRPs), kinases, and cathepsins represent key targets for developing novel molecular imaging agents.

Related Concept Videos

Membrane Transporters01:31

Membrane Transporters

Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
The Significance of Membrane Transport01:44

The Significance of Membrane Transport

The transport of solutes across the cell membrane is essential for metabolic processes, like maintaining cell size and volume, generating the action potential, exchanging nutrients and gases, etc. Membrane transport can be either passive or active. It can be simple diffusion, facilitated, or mediated transport aided by transport proteins such as transporters and channels.
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
The Significance of Membrane Transport01:44

The Significance of Membrane Transport

The transport of solutes across the cell membrane is essential for metabolic processes, like maintaining cell size and volume, generating the action potential, exchanging nutrients and gases, etc. Membrane transport can be either passive or active. It can be simple diffusion, facilitated, or mediated transport aided by transport proteins such as transporters and channels.
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
Active Transport01:14

Active Transport

Active transport is a critical biological process that allows cells to move solutes against an electrochemical gradient. This process requires direct energy input and is characterized by its selectivity, saturability, and susceptibility to competitive inhibition.
Primary active transporters, like Na+, K+ and -ATPase, directly utilize ATP to move ions across the membrane. These transporters play significant roles in various physiological processes. For instance, Na+, K+ and -ATPase maintain...
Facilitated Diffusion01:16

Facilitated Diffusion

The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
Carrier-Mediated Transport01:06

Carrier-Mediated Transport

Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...