What is DHFR gene?

Dihydrofolate reductase, or DHFR, is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as electron donor, which can be converted to the kinds of tetrahydrofolate cofactors used in 1-carbon transfer chemistry. In humans, the DHFR enzyme is encoded by the DHFR gene.

What is DHFR and why is it important?

Dihydrofolate reductase (DHFR) catalyzes the reduction of dihydrofolate to tetrahydrofolate (THF). The importance of this reaction is demonstrated by the effectiveness of antifolate medications used to treat cancer by inhibiting DHFR, thereby depleting THF and slowing DNA synthesis and cell proliferation.

What is the function of DHFR?

Dihydrofolate reductase is a small enzyme that plays a supporting role, but an essential role, in the building of DNA and other processes. It manages the state of folate, a snaky organic molecule that shuttles carbon atoms to enzymes that need them in their reactions.

How does trimethoprim inhibit dihydrofolate reductase?

Mechanism of Action Trimethoprim is 50,000 to 100,000 times more active against bacterial dihydrofolate reductase than against the human enzyme. Trimethoprim interferes with the conversion of dihydrofolate to tetrahydrofolate, the precursor of folinic acid and ultimately of purine and DNA synthesis (Fig. 33-3).

Is DHFR an inhibitor?

A substance that can build up in cancer cells and block them from using folate. Folate is a nutrient that rapidly dividing cells need to make DNA. Blocking folate use helps keep cancer cells from growing and may kill them.

What is the primary inhibitor of DHFR?

DHFR inhibitors used for antiparasitic therapy include pyrimethamine, trimethoprim, proguanil, and trimetrexate. The sulfonamides have various pharmacokinetic properties, which are taken advantage of in the formulations used for treatment of parasitic infections.

What reaction does DHFR catalyze include the reactants and products?

Dihydrofolate reductase (DHFR) catalyzes the NADPH-dependent reduction of dihydrofolate (DHF), yielding tetrahydrofolate (THF), an important reaction in the folate cycle, which supplies one-carbon units for the biosynthesis of deoxythymidine monophosphate (dTMP), and for reactions involved in the biosynthesis of …

What is the structure of trimethoprim?

C14H18N4O3
Trimethoprim/Formula

What is meant by DHFR inhibitors?

A dihydrofolate reductase inhibitor (DHFR inhibitor) is a molecule that inhibits the function of dihydrofolate reductase, and is a type of antifolate. Since folate is needed by rapidly dividing cells to make thymine, this effect may be used to therapeutic advantage.

Which of the drug is DHFR inhibitor?

The two main classical DHFR inhibitors are aminopterin (AM) and methotrexate (MTX, amethopterin), which were designed by replacing an enol-type OH group at C-4 of the natural substrate (DHF) by an amino group.

What reaction is catalyzed by dihydrofolate reductase?

What is the Iupac name of trimethoprim?

Trimethoprim hydrochloride

What does a data flow diagram ( DFD ) represent?

A Data Flow Diagram (DFD) is traditional visual representation of the information flows within a system. A neat and clear DFD can depict a good amount of the system requirements graphically. It can be manual, automated, or combination of both.

Why is DHFR important in the synthesis of tetrahydrofolate?

Tetrahydrofolate synthesis pathway. Found in all organisms, DHFR has a critical role in regulating the amount of tetrahydrofolate in the cell. Tetrahydrofolate and its derivatives are essential for purine and thymidylate synthesis, which are important for cell proliferation and cell growth.

How does the dihydrofolate reductase ( DHFR ) enzyme work?

Dihydrofolate reductase, or DHFR, is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as electron donor, which can be converted to the kinds of tetrahydrofolate cofactors used in 1-carbon transfer chemistry. In humans, the DHFR enzyme is encoded by the DHFR gene.

How is DHFR deficiency linked to megaloblastic anemia?

Dihydrofolate reductase deficiency has been linked to megaloblastic anemia. Treatment is with reduced forms of folic acid. Because tetrahydrofolate, the product of this reaction, is the active form of folate in humans, inhibition of DHFR can cause functional folate deficiency.