Target intelligence / Profile preview

D-luciferin

Molecular classification
Benzothiazole, Small molecule, Bioluminescent substrate
01

Overview

D-luciferin is a small molecule substrate primarily known for its role in the bioluminescent reaction catalyzed by the enzyme firefly luciferase (Source 1.1.1). In the presence of adenosine triphosphate (ATP), magnesium, and oxygen, luciferase converts D-luciferin into oxyluciferin, a process that releases visible light (Source 1.1.1, 1.3.2). This bioluminescent system is extensively utilized in biomedical research as a highly sensitive reporter to monitor gene expression, cell viability, and ATP levels (Source 1.1.4, 1.3.4). In vivo, D-luciferin is used for non-invasive imaging to track tumor progression, metastasis, and the efficacy of therapeutic interventions in animal models (Source 1.2.2, 1.2.4). Although it is not a therapeutic target, D-luciferin is a substrate for certain ATP-binding cassette (ABC) transporters, such as ABCG2 and MRP4, which can affect its tissue distribution and the resulting signal intensity (Source 1.2.1, 1.3.5). Its membrane permeability and lack of endogenous background make it an ideal tool for real-time visualization of biological processes (Source 1.3.2). Researchers also use D-luciferin derivatives to study specific enzyme activities or to improve brain penetration for neuroimaging (Source 1.2.1, 1.2.3).

Other names
Firefly luciferinBeetle luciferin(S)-2-(6-hydroxy-2-benzothiazolyl)-2-thiazoline-4-carboxylic acidD-(-)-Luciferin
02

Mechanism of action

Substrate for luciferase-catalyzed bioluminescence

03

Biological functions

BioluminescenceATP-dependent oxidationReporter substrate
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Disease associations

CancerInfectionInflammation
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Safety considerations

Interference with ABC transportersImaging artifacts from excipient interactionsBlood-brain barrier permeability limitations
06

Interacting drugs

Firefly luciferase

3 more in the full profile.

07

Biomarkers

Luciferase reporter activityATP concentration

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