DGUOK Inhibitors
Chemical inhibitors of DGUOK can achieve functional inhibition through various mechanisms, primarily by resembling its natural substrates and competing for the active site of the enzyme. Deoxyguanosine, a natural nucleoside, can competitively inhibit DGUOK by acting as an alternative substrate. When present in excess, it can outcompete the natural substrate, leading to the functional inhibition of DGUOK's kinase activity. Similarly, nucleoside analogs like Ribavirin and Didanosine are designed to mimic the natural substrates of the enzyme. Their incorporation by DGUOK leads to halting of the polymerization processes, directly inhibiting the kinase activity of DGUOK. Cladribine and Fludarabine, both synthetic nucleosides, get phosphorylated by DGUOK and act as chain terminators during DNA synthesis, which disrupts the normal enzymatic cycle of DGUOK, effectively halting its function.
Other chemicals such as Clofarabine and Penciclovir are phosphorylated by the kinase activity of DGUOK. Once incorporated into DNA, they terminate the DNA chain elongation, which is a critical step where DGUOK normally functions, thereby inhibiting it. Ganciclovir, after being phosphorylated by DGUOK, inhibits DNA polymerization, thus preventing DGUOK from fulfilling its role in generating nucleotides for DNA synthesis. Cidofovir also undergoes phosphorylation by DGUOK and inhibits the enzyme by competitive inhibition, resembling the natural substrates of the enzyme. Entecavir and Tenofovir, both nucleoside analogs, are metabolized and phosphorylated to active forms that inhibit DGUOK by competing with the natural substrates for the active site, thereby blocking the normal enzymatic activity. Sofosbuvir, another nucleotide analog, once metabolized, can be erroneously utilized by DGUOK, leading to its functional inhibition as a defective substrate, which disrupts the normal enzymatic process of the protein. These chemical inhibitors employ substrate competition, defective substrate incorporation, and termination of the enzymatic cycle to achieve the functional inhibition of DGUOK.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Ribavirin | 36791-04-5 | sc-203238 sc-203238A sc-203238B | 10 mg 100 mg 5 g | $62.00 $108.00 $210.00 | 1 | |
Ribavirin is a nucleoside analogue that can inhibit DGUOK by resembling its natural substrates. Once incorporated, it can halt the further polymerization processes that DGUOK is involved in, leading to its functional inhibition. | ||||||
2-Chloro-2′-deoxyadenosine | 4291-63-8 | sc-202399 | 10 mg | $144.00 | 1 | |
Cladribine, a synthetic nucleoside, can be phosphorylated by DGUOK. The phosphorylated form acts as a chain terminator during DNA synthesis, which in turn can functionally inhibit the action of DGUOK by preventing its normal activity in DNA synthesis. | ||||||
Fludarabine | 21679-14-1 | sc-204755 sc-204755A | 5 mg 25 mg | $57.00 $200.00 | 15 | |
Fludarabine is phosphorylated by DGUOK and the triphosphate form incorporates into DNA, inhibiting DNA synthesis and functionally inhibiting DGUOK by blocking its physiological role in generating nucleotides for DNA synthesis. | ||||||
Clofarabine | 123318-82-1 | sc-278864 sc-278864A | 10 mg 50 mg | $185.00 $781.00 | ||
Clofarabine, a purine nucleoside analog, is phosphorylated by DGUOK and disrupts DNA replication and repair, which leads to a functional inhibition of DGUOK as it impedes the enzyme's role in nucleotide synthesis for DNA replication. | ||||||
Penciclovir | 39809-25-1 | sc-203183 | 100 mg | $255.00 | ||
Penciclovir, an acyclic guanine derivative, can be phosphorylated by DGUOK and once incorporated into DNA, it can terminate the DNA chain, thereby inhibiting the enzymatic activity of DGUOK in DNA synthesis. | ||||||
Ganciclovir | 82410-32-0 | sc-203963 sc-203963A | 50 mg 250 mg | $228.00 $413.00 | 1 | |
Ganciclovir, a synthetic nucleoside analog of guanine, is phosphorylated by DGUOK. The phosphorylated ganciclovir inhibits DNA polymerization, thereby functionally inhibiting DGUOK by interfering with its natural nucleotide synthesis activity. | ||||||
Cidofovir | 113852-37-2 | sc-482141 | 50 mg | $135.00 | ||
Cidofovir is phosphorylated by DGUOK and subsequently inhibits viral DNA polymerases more than cellular polymerases, leading to the inhibition of DGUOK's enzymatic activity by competitive inhibition through substrate resemblance. | ||||||
Entecavir | 142217-69-4 | sc-204738 sc-204738A sc-204738B | 1 mg 5 mg 25 mg | $75.00 $210.00 $620.00 | 11 | |
Entecavir is another guanine nucleoside analog that can be phosphorylated by DGUOK. Once phosphorylated, it competes with the natural substrate, resulting in the functional inhibition of DGUOK by preventing its normal enzymatic action. | ||||||
Sofosbuvir | 1190307-88-0 | sc-482362 | 25 mg | $143.00 | 1 | |
Sofosbuvir, a nucleotide analog, is metabolized to the active triphosphate form, which can then be mistakenly utilized by DGUOK, leading to the functional inhibition of the enzyme by acting as a defective substrate. | ||||||
Tenofovir | 147127-20-6 | sc-204335 sc-204335A | 10 mg 50 mg | $154.00 $633.00 | 11 | |
Tenofovir, once metabolized to its active form, can inhibit DGUOK by mimicking its natural substrates. This can lead to a functional inhibition of DGUOK as it would interfere with the enzyme's ability to catalyze the phosphorylation of nucleotides. | ||||||