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The p53 upregulated modulator of apoptosis (PUMA) also known as Bcl-2-binding component 3 (BBC3), is a pro-apoptotic protein, member of the Bcl-2 protein family. [5] [6] In humans, the Bcl-2-binding component 3 protein is encoded by the BBC3 gene. [5] [6] The expression of PUMA is regulated by the tumor suppressor p53.
Most competitive inhibitors function by binding reversibly to the active site of the enzyme. [1] As a result, many sources state that this is the defining feature of competitive inhibitors. [ 7 ] This, however, is a misleading oversimplification , as there are many possible mechanisms by which an enzyme may bind either the inhibitor or the ...
Histamine N-methyltransferase is encoded by a single gene, called HNMT, which has been mapped to chromosome 2 in humans. [5]Three transcript variants have been identified for this gene in humans, which produce different protein isoforms [6] [5] due to alternative splicing, which allows a single gene to code for multiple proteins by including or excluding particular exons of a gene in the final ...
Irreversible inhibitors covalently bind to an enzyme, and this type of inhibition can therefore not be readily reversed. [51] Irreversible inhibitors often contain reactive functional groups such as nitrogen mustards, aldehydes, haloalkanes, alkenes, Michael acceptors, phenyl sulfonates, or fluorophosphonates. [52]
15874 Ensembl ENSG00000121351 ENSMUSG00000041681 UniProt P10997 P12968 RefSeq (mRNA) NM_000415 NM_001329201 NM_010491 RefSeq (protein) NP_000406 NP_001316130 NP_034621 Location (UCSC) Chr 12: 21.35 – 21.38 Mb Chr 6: 142.24 – 142.25 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Amino acid sequence of amylin with disulfide bridge and cleavage sites of insulin degrading enzyme ...
These inhibitors bind through two phosphonate oxygen atoms. Phosphonate inhibitors have been developed that exhibit selectivity for MMP-8 over other MMPs. Selective MMP-8 inhibitors could be useful in the treatment of acute liver disease and multiple sclerosis [15] Phosphinic MMP inhibitors have been reported to target MMP-11 and MMP-13.
Inosine 5′-monophosphate dehydrogenase (IMPDH) is a purine biosynthetic enzyme that catalyzes the nicotinamide adenine dinucleotide (NAD +)-dependent oxidation of inosine monophosphate (IMP) to xanthosine monophosphate (XMP), the first committed and rate-limiting step towards the de novo biosynthesis of guanine nucleotides from IMP.
Index inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug-drug interaction studies. [2]Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by ≥80%, ≥50% to <80%, and ≥20% to <50%, respectively.