| Autor: |
Eunsun Park, Kyung-Hee Song, Darong Kim, Minyoung Lee, Nguyen Van Manh, Hee Kim, Ki Bum Hong, Jeewoo Lee, Jie-Young Song, Soosung Kang |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
ACS medicinal chemistry letters. 13(9) |
| ISSN: |
1948-5875 |
| Popis: |
Glutaminyl cyclases (QC, isoQC) convert N-terminal glutamine or glutamate into pyroglutamate (pGlu) on substrates. IsoQC has recently been demonstrated to promote pGlu formation on the N-terminus of CD47, the SIRPα binding site, contributing to the "don't eat me" cancer immune signaling of CD47-SIRPα. We developed new QC inhibitors by applying a structure-based optimization approach starting from fragments identified through library screening. Screening of metal binding fragments identified 5-(1 |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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