Target-Directed Self-Assembly of Homodimeric Drugs Against β‑Tryptase

Tryptase, a serine protease released from mast cells, is implicated in many allergic and inflammatory disorders. Human tryptase is a donut-shaped tetramer with the active sites facing inward forming a central pore. Bivalent ligands spanning two active sites potently inhibit this configuration, but t...

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Veröffentlicht in:ACS medicinal chemistry letters 2018-08, Vol.9 (8), p.827-831
Hauptverfasser: Giardina, Sarah F, Werner, Douglas S, Pingle, Maneesh, Foreman, Kenneth W, Bergstrom, Donald E, Arnold, Lee D, Barany, Francis
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Sprache:eng
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