Highly Diverse Heparan Sulfate Analogue Libraries: Providing Access to Expanded Areas of Sequence Space for Bioactivity Screening

Structurally diverse heparan sulfate analogue libraries were produced chemicoenzymatically from heparin. They possess vastly more heterogeneity than tissue heparan sulfates, expand the sequence space available for screening, and can help identify minimal structural features associated with activity. Library components are likely to exhibit fewer nonspecific interactions and side-effects than heparin or simple chemically modified heparin. A strategy for their use is illustrated for the fibroblast growth factor-receptor tyrosine kinase signaling system.