Ac-Trp-Leu-Ala-AMC (Ac-WLA-AMC) Summary
The 20S Proteasome is the catalytic core component of the multi-complex 26S Proteasome that selectively degrades intracellular proteins.It is commonly associated with regulatory complexes, which include the 19S Proteasome, the PA28 alpha/beta complex, or the PA28 gamma complex.The 20S Proteasome is composed of 28 subunits arranged into four stacked rings.The outer rings, containing seven subunits each, are composed of closely-related but non-identical alpha subunits.The amino-terminal tails of the alpha subunits form a gate that restricts substrate entry into the catalytic core.The inner rings, also containing seven subunits each, are composed of closely-related but non-identical beta subunits.The amino-terminal tails of six of the beta subunits, three per ring, have proteolytic activity. Inhibition of 20S Proteasome proteolytic core activity using small molecule inhibitors is a valuable tool for the functional study of a variety of proteins and for therapeutic intervention.The 20S Proteasome can be activated chemically by the addition of detergent or by the proteinaceous activator PA28 Activator alpha.This fluorogenic tri-peptide substrate may be used to monitor Proteasome activity.It is hydrolyzed by the chymotrypsin-like activity of thebeta 5c (PSMB5) subunit.
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Citations for Ac-Trp-Leu-Ala-AMC (Ac-WLA-AMC)
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- H727 cells are inherently resistant to the proteasome inhibitor carfilzomib, yet require proteasome activity for cell survival and growthAuthors: MJ Lee, Z Miller, JE Park, D Bhattarai, W Lee, KB KimSci Rep, 2019;9(1):4089.2019
- Immunoproteasome functions explained by divergence in cleavage specificity and regulationAuthors: MB Winter, F La Greca, S Arastu-Kap, F Caiazza, P Cimermanci, TJ Buchholz, JL Anderl, M Ravalin, MF Bohn, A Sali, AJ O"Donoghue, CS CraikElife, 2017;6(0):.2017
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S-330 hydrolysis confirmation by LCMS-SRMS-330: 1 uMi20S: 15 nMPA28a: 150 nMReaction: 37 °C for 5 h1:S-330 Ac-WLA-AMC (588.20>342.15)2:Free AMC (176.25>120.00)3:S-330 Ac-WLA-COOH (431.25>342.15)