IndraLab

Statements

OAZ1 inhibits USP28. 7 / 7
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"Prieto-Garcia et al demonstrated that AZ1 blocks USP28-dependent stabilization of ΔNp63, leading to a decrease in SCC transplanted tumor size and number (Prieto-Garcia et al, 2020)."
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"Inspired by the strong effect on viral replication, we explored USP25 as an antiviral drug target using the small molecule AZ1, which effectively inhibits USP25 and USP28 enzymatic activity ."
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"Differently substituted molecules (AZ1: -F/-CF ; AZ2: -O-CF ; AZ4: 3x-F) inhibited USP28/USP25 in a high nanomolar to low micromolar range, while potency was significantly diminished for the non-fluoro-substituted variant AZ3 (Wrigley et al, 2017)."
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"In addition to SGH, AZ1 is another inhibitor of USP28 that is quite significant for the treatment of lung cancer."
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"Kinetic analysis of full-length USP28 inhibition by AZ1 revealed a non-competitive mode of inhibition (Wrigley et al, 2017)."
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"The results showed that AZ1 could effectively inhibit USP28 in non-small cell lung cancer (Fig.S1A)."
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"AZ1 is the first reported inhibitor of USP28, demonstrating an ability to bind to and inhibit USP28, while also exhibiting dual activity against USP25 [60]."
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