E1 enzymes
E1 enzymes (Ubiquitin-activating enzymes) catalyze the first step in the ubiquitination reaction, which (among other things) can target a protein for degradation via a proteasome. This covalent attachment of ubiquitin or ubiquitin-like proteins to targeted proteins is a major mechanism for regulating protein function in eukaryotic organisms. Many processes such as cell division, immune responses and embryonic development are also regulated by post-transcriptional modification by ubiquitin and ubiquitin-like proteins.
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NPS 2143 hydrochloride是calcium-sensing受体选择性拮抗剂， 口服有效的催化剂。
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PYR-41是特异的可渗透入细胞的泛素激活酶E1抑制剂，IC50< 10 uM，对E2几乎无活性。
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NPS-2143是一种新型有效的，选择性的Ca(2+)受体拮抗剂，IC50为43 nM。
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Ibrutinib (PCI-32765)是一种有效的，高选择性的Btk抑制剂，IC50为0.5 nM，能稍许微抑制Bmx， CSK， FGR， BRK及HCK，但对EGFR， Yes， ErbB2， JAK3等作用效果稍弱。
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Cinacalcet hydrochloride是口服活性的第二代拟钙剂，对甲状旁腺机能亢进有效。
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