Ubiquitination/ Proteasome - Multiple Myeloma - Colon Cancer - Lung Cancer - Glioma
Ubiquitination is a process in targeting proteins for degradation by the proteasome. Ubiquitin (Ub) is a 76 amino acid polypeptide which can be covalently attached to various cellular proteins by the ubiquitination process. This ubiquitin-proteasome system plays a vital role in cell division, growth, differentiation, transcriptional regulation, apoptosis and immunity etc. Three main types of enzymes are involved in the process of ubiquitination. In the first step, activation of ubiquitin is carried out by ubiquitin-activating enzyme (E1) through an ATP-dependent reaction. In the second step, the activated ubiquitin is transferred from E1 to ubiquitin-conjugating enzyme (E2). In the final step, the ubiquitin protein ligase (E3) is required for labeling the ubiquitin to target substrate protein. An isopeptide bond is formed between the carboxyl terminus of ubiquitin and the ε-amino group of a lysine residue in the target protein.
Once the substrate protein is labeled, proteasome will bind to a polyubiquitin chain, allowing the degradation of the labeled protein. The polyubiquitinated target protein is then recognized and degraded by the 26S proteasome. Deubiquitinating enzymes (DUBs) reverse the process of ubiquitination by removing ubiquitin from its substrate protein. Dysregulation of the ubiquitin-proteasome system has been linked to cancer, diabetes, cardiovascular and neurodegenerative diseases etc.
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- B6032 CB-5083Target: p97Summary: p97抑制剂
- A8715 SBI-02069652 CitationTarget: ULK1Summary: ULK1抑制剂
- B2168 NMS-8733 CitationTarget: Valosin-containing protein (VCP)Summary: VCP/p97抑制剂
- A8487 Nocodazole1 Citation中文名: 诺考达唑Target: Microtubules/TubulinsSummary: 微管蛋白产生抑制剂,抗肿瘤剂
- A2324 Dexamethasone (DHAP)中文名: 地塞米松Target: interleukin receptorSummary: 糖皮质激素,抗炎活性
- A4429 Vialinin ATarget: Deubiquitinating enzymes (DUBs)|IL Receptors|CCL2Summary: USP/IsoT/UCH-L1 DUB抑制剂
- A1933 Carfilzomib (PR-171)10 Citation中文名: 卡非佐米Target: ProteasomeSummary: 蛋白酶体抑制剂
- A4393 Paclitaxel (Taxol)4 Citation中文名: 紫杉醇Target: Microtubules/TubulinsSummary: 抗肿瘤药
- A2614 Bortezomib (PS-341)24 Citation中文名: 硼替佐米Target: ProteasomeSummary: 蛋白酶体抑制剂
- A4010 Salinosporamide A (NPI-0052, Marizomib)Target: ProteasomeSummary: 20S蛋白酶体抑制剂