2-Deoxy--glucose is a
glucose
Glucose is a simple sugar with the molecular formula . Glucose is overall the most abundant monosaccharide, a subcategory of carbohydrates. Glucose is mainly made by plants and most algae during photosynthesis from water and carbon dioxide, u ...
molecule
A molecule is a group of two or more atoms held together by attractive forces known as chemical bonds; depending on context, the term may or may not include ions which satisfy this criterion. In quantum physics, organic chemistry, and b ...
which has the 2-
hydroxyl
In chemistry, a hydroxy or hydroxyl group is a functional group with the chemical formula and composed of one oxygen atom covalently bonded to one hydrogen atom. In organic chemistry, alcohols and carboxylic acids contain one or more hydrox ...
group replaced by hydrogen, so that it cannot undergo further
glycolysis
Glycolysis is the metabolic pathway that converts glucose () into pyruvate (). The free energy released in this process is used to form the high-energy molecules adenosine triphosphate (ATP) and reduced nicotinamide adenine dinucleotide (NADH ...
. As such; it acts to competitively inhibit the production of
glucose-6-phosphate from glucose at the
phosphoglucoisomerase level (step 2 of glycolysis). 2-Deoxyglucose labeled with
tritium
Tritium ( or , ) or hydrogen-3 (symbol T or H) is a rare and radioactive isotope of hydrogen with half-life about 12 years. The nucleus of tritium (t, sometimes called a ''triton'') contains one proton and two neutrons, whereas the nucleus of ...
or
carbon-14
Carbon-14, C-14, or radiocarbon, is a radioactive isotope of carbon with an atomic nucleus containing 6 protons and 8 neutrons. Its presence in organic materials is the basis of the radiocarbon dating method pioneered by Willard Libby and co ...
has been a popular ligand for laboratory research in animal models, where distribution is assessed by tissue-slicing followed by
autoradiograph
An autoradiograph is an image on an X-ray film or nuclear emulsion produced by the pattern of decay emissions (e.g., beta particles or gamma rays) from a distribution of a radioactive substance. Alternatively, the autoradiograph is also available ...
y, sometimes in tandem with either conventional or
electron microscopy
An electron microscope is a microscope that uses a beam of accelerated electrons as a source of illumination. As the wavelength of an electron can be up to 100,000 times shorter than that of visible light photons, electron microscopes have a hi ...
.
2-DG is up taken by the
glucose transporters of the cell. Therefore, cells with higher glucose uptake, for example tumor cells, have also a higher uptake of 2-DG. Since 2-DG hampers cell growth, its use as a
tumor
A neoplasm () is a type of abnormal and excessive growth of tissue. The process that occurs to form or produce a neoplasm is called neoplasia. The growth of a neoplasm is uncoordinated with that of the normal surrounding tissue, and persists ...
therapeutic has been suggested, and in fact, 2-DG is in clinical trials. It is not completely clear how 2-DG inhibits cell growth. The fact that glycolysis is inhibited by 2-DG, seems not to be sufficient to explain why 2-DG treated cells stop growing. Because of its structural similarity to mannose, 2DG has the potential to inhibit N-glycosylation in mammalian cells and other systems, and as such induces ER stress and the Unfolded Protein Response (UPR) pathway.
Use in optical imaging
2-DG has been used as a targeted optical imaging agent for fluorescent ''in vivo'' imaging. In clinical medical imaging (
PET scan
Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in metabolic processes, and in other physiological activities including blood flo ...
ning),
fluorodeoxyglucose
18F.html" ;"title="sup>18F">sup>18Fluorodeoxyglucose ( INN), or fluorodeoxyglucose F 18 (USAN and USP), also commonly called fluorodeoxyglucose and abbreviated 18F.html" ;"title="sup>18F">sup>18FDG, 2- 18F.html" ;"title="sup>18F">sup>18FDG or ...
is used, where one of the 2-hydrogens of 2-deoxy-D-glucose is replaced with the positron-emitting isotope
fluorine-18
Fluorine-18 (18F) is a fluorine radioisotope which is an important source of positrons. It has a mass of 18.0009380(6) u and its half-life is 109.771(20) minutes. It decays by positron emission 96% of the time and electron capture 4% of the time ...
, which emits paired
gamma ray
A gamma ray, also known as gamma radiation (symbol γ or \gamma), is a penetrating form of electromagnetic radiation arising from the radioactive decay of atomic nuclei. It consists of the shortest wavelength electromagnetic waves, typically ...
s, allowing distribution of the tracer to be imaged by external gamma camera(s). This is increasingly done in tandem with a
CT function which is part of the same PET/CT machine, to allow better localization of small-volume tissue glucose-uptake differences.
Indian adoption for COVID-19 treatment
On May 8, 2021, the
Drugs Controller General of India
Drugs Controller General of India (DCGI) is the head of department of the Central Drugs Standard Control Organization of the Government of India responsible for approval of licences of specified categories of drugs such as blood and blood pr ...
approved an oral formulation of 2-deoxy-D-glucose for emergency use as adjunct therapy in moderate to severe coronavirus patients.
What is 2-deoxy-D-glucose (2-DG) and is it effective against Covid?
The Economic Times, 17 May 2021.DRDO
The Defence Research and Development Organisation (DRDO) (IAST: ''Raksā Anūsandhān Evam Vikās Sangaṭhan'') is the premier agency under the Department of Defence Research and Development in Ministry of Defence of the Government of India, ...
along with Dr. Reddy's Laboratories, who jointly claimed via a press release, that the drug "helps in faster recovery of hospitalised patients and reduces supplemental oxygen dependence".The Wire
''The Wire'' is an American crime drama television series created and primarily written by author and former police reporter David Simon. The series was broadcast by the cable network HBO in the United States. ''The Wire'' premiered on June 2 ...
as well as The Hindu
''The Hindu'' is an Indian English-language daily newspaper owned by The Hindu Group, headquartered in Chennai, Tamil Nadu. It began as a weekly in 1878 and became a daily in 1889. It is one of the Indian newspapers of record and the sec ...
noted that the approval was based on poor evidence; no journal publication (or preprint
In academic publishing, a preprint is a version of a scholarly or scientific paper that precedes formal peer review and publication in a peer-reviewed scholarly or scientific journal. The preprint may be available, often as a non-typeset versi ...
) concerning efficacy and safety are yet available.
See also
* COVID-19 misinformation
False information, including intentional disinformation and conspiracy theories, about the scale of the COVID-19 pandemic and the origin, prevention, diagnosis, and treatment of the disease has been spread through social media, text messagin ...
* Fluorouracil
Fluorouracil (5-FU), sold under the brand name Adrucil among others, is a cytotoxic chemotherapy medication used to treat cancer. By intravenous injection it is used for treatment of colorectal cancer, oesophageal cancer, stomach cancer, panc ...
References
{{DEFAULTSORT:Deoxy-D-Glucose, 2-
Deoxy sugars
Aldohexoses