Publications by authors named "Linda Blechschmidt"
Article Synopsis
- STAT family proteins play crucial roles in cell signaling and are potential targets for treating diseases; however, existing inhibitors often lack specificity.
- Recent research has introduced catechol bisphosphates as highly selective inhibitors for the STAT5b protein, distinguishing them from closely related STAT5a.
- The specificity is determined by a single amino acid position in the linker domain rather than the SH2 domain, suggesting new strategies for designing targeted STAT inhibitors and insights into their differing biological functions.
The transcription factor STAT5b is a target for tumour therapy. We recently reported catechol bisphosphate and derivatives such as Stafib-1 as the first selective inhibitors of the STAT5b SH2 domain. Here, we demonstrate STAT5b binding of catechol bisphosphate by solid-state nuclear magnetic resonance, and report on rational optimization of Stafib-1 (K = 44 nM) to Stafib-2 (K = 9 nM).
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