Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics

Margarete Von Wantoch Rekowski, Vijay Kumar, Zongmin Zhou, Johann Moschner, Antonia Marazioti, Marina Bantzi, Georgios A. Spyroulias, Focco Van Den Akker, Athanassios Giannis, Andreas Papapetropoulos

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Recently, the structure of BAY 58-2667 bound to the Nostoc sp. H-NOX domain was published. On the basis of this structural information, we designed BAY 58-2667 derivatives and tested their effects on soluble guanylyl cyclase (sGC) activity. Derivative 20 activated sGC 4.8-fold more than BAY 58-2667. Co-crystallization of 20 with the Ns H-NOX domain revealed that the increased conformational distortion at the C-terminal region of αF helix containing 110-114 residues contributes to the higher activation triggered by 20.

Original languageEnglish (US)
Pages (from-to)8948-8952
Number of pages5
JournalJournal of Medicinal Chemistry
Volume56
Issue number21
DOIs
StatePublished - Nov 14 2013
Externally publishedYes

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Heme
Nostoc
Crystallization
BAY 58-2667
Soluble Guanylyl Cyclase

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Von Wantoch Rekowski, M., Kumar, V., Zhou, Z., Moschner, J., Marazioti, A., Bantzi, M., ... Papapetropoulos, A. (2013). Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics. Journal of Medicinal Chemistry, 56(21), 8948-8952. https://doi.org/10.1021/jm400539d

Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics. / Von Wantoch Rekowski, Margarete; Kumar, Vijay; Zhou, Zongmin; Moschner, Johann; Marazioti, Antonia; Bantzi, Marina; Spyroulias, Georgios A.; Van Den Akker, Focco; Giannis, Athanassios; Papapetropoulos, Andreas.

In: Journal of Medicinal Chemistry, Vol. 56, No. 21, 14.11.2013, p. 8948-8952.

Research output: Contribution to journalArticle

Von Wantoch Rekowski, M, Kumar, V, Zhou, Z, Moschner, J, Marazioti, A, Bantzi, M, Spyroulias, GA, Van Den Akker, F, Giannis, A & Papapetropoulos, A 2013, 'Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics', Journal of Medicinal Chemistry, vol. 56, no. 21, pp. 8948-8952. https://doi.org/10.1021/jm400539d
Von Wantoch Rekowski M, Kumar V, Zhou Z, Moschner J, Marazioti A, Bantzi M et al. Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics. Journal of Medicinal Chemistry. 2013 Nov 14;56(21):8948-8952. https://doi.org/10.1021/jm400539d
Von Wantoch Rekowski, Margarete ; Kumar, Vijay ; Zhou, Zongmin ; Moschner, Johann ; Marazioti, Antonia ; Bantzi, Marina ; Spyroulias, Georgios A. ; Van Den Akker, Focco ; Giannis, Athanassios ; Papapetropoulos, Andreas. / Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics. In: Journal of Medicinal Chemistry. 2013 ; Vol. 56, No. 21. pp. 8948-8952.
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