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Antifolates act primarily as inhibitors of both RNA and DNA, and are often grouped with nucleic acid inhibitors in textbooks. However, they also act indirectly as protein synthesis inhibitors (because tetrahydrofolate is also involved in the synthesis of amino acids serine and methionine), so they are sometimes considered as their own category, antimetabolites. [6]
As a nucleoside inhibitor, the guanosine analog prodrug is used to stop viral RNA synthesis and viral mRNA capping by incorporating into RNA and pairing to uracil or cytosine. Branaplam is currently in phase I/II clinical trial for the treatment of Spinal Muscular Atrophy (SMA). This molecule is from a class of pyridazine small molecules and ...
They are related to nucleic acid analogues. Nucleoside and nucleotide analogues can be used in therapeutic drugs, including a range of antiviral products used to prevent viral replication in infected cells. The most commonly used is acyclovir. Nucleotide and nucleoside analogues can also be found naturally.
Purine synthesis inhibitor. Acute lymphoblastic leukaemia, acute promyelocytic leukaemia, lymphoblastic lymphoma and inflammatory bowel disease. [12] Myelosuppression, hepatotoxicity, GI ulceration (rare), pancreatitis (rare) and secondary leukaemia (rare) or myelodysplasia (rare). Nelarabine [13] IV: Purine synthesis inhibitor.
Antimetabolites may also be antibiotics, such as sulfanilamide drugs, which inhibit dihydrofolate synthesis in bacteria by competing with para-aminobenzoic acid (PABA). [8] PABA is needed in enzymatic reactions that produce folic acid, which acts as a coenzyme in the synthesis of purines and pyrimidines, the building-blocks of DNA.
Dihydropteroate synthase inhibitors are drugs that inhibit the action of dihydropteroate synthase. They include sulfonamides, dapsone, and para-aminosalicylic acid. [1] Tetrahydrofolate synthesis pathway. In bacteria, antibacterial sulfonamides act as competitive inhibitors of the enzyme dihydropteroate synthase, DHPS.
Decitabine (i.e., 5-aza-2′-deoxycytidine), sold under the brand name Dacogen among others, acts as a nucleic acid synthesis inhibitor. [4] It is a medication for the treatment of myelodysplastic syndromes, a class of conditions where certain blood cells are dysfunctional, and for acute myeloid leukemia (AML). [5] Chemically, it is a cytidine ...
It is nonenzymatically cleaved to mercaptopurine, a purine analogue that inhibits DNA synthesis. By preventing the clonal expansion of lymphocytes in the induction phase of the immune response, it affects both cell immunity and humoral immunity .