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Figure 1: Lanosterol synthase mechanism. The discrete carbocation intermediates show the non-concerted nature of the mechanism. Though some data on the mechanism has been obtained by the use of suicide inhibitors, mutagenesis studies, and homology modeling, it is still not fully understood how the enzyme catalyzes the formation of lanosterol.
Minnich et al. dosed mongrel dogs subcutaneously with aminopterin and folic acid simultaneously to test whether folic acid can rescue animals from the lethality and toxicity of aminopterin [24] Dogs were given 0.020, 0.046, 0.044 escalated to 0.088, and 0.097 mg/kg aminopterin each day for 7 to 12 days. Folic acid was given in a weight ratio to ...
ATC code C10 Lipid modifying agents is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
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.
DON is a cytotoxic inhibitor of many enzymes of nucleotide synthesis. It could be shown in vitro that DON treatment led to apoptosis, or programmed cell death. Different pathways were investigated; it could be shown that the inner mitochondrial membrane was damaged, [14] and that single strand DNA breaks occurred. [15]
Image illustrates DNA, RNA, and protein synthesis. The first two are nucleic acids. A nucleic acid inhibitor is a type of antibacterial that acts by inhibiting the production of nucleic acids. There are two major classes: DNA inhibitors and RNA inhibitors. [1] The antifungal flucytosine acts in a similar manner.
Thymidine synthesis first requires reduction of the uridine to deoxyuridine (see next section), before the base can be methylated to produce thymidine. [1] [5] ATP, a purine nucleotide, is an activator of pyrimidine synthesis, while CTP, a pyrimidine nucleotide, is an inhibitor of pyrimidine synthesis. This regulation helps to keep the purine ...
Ezetimibe is a selective inhibitor of dietary cholesterol absorption. Lomitapide is a microsomal triglyceride transfer protein inhibitor. PCSK9 inhibitors [3] [4] are monoclonal antibodies for refractory cases. (e.g. Evolocumab, Inclisiran) They are used in combination with statins. Probucol (withdrawn in several countries)