Correlating drug–target kinetics and in vivo pharmacodynamics: long residence time inhibitors of the FabI enoyl-ACP reductase

Author:

Daryaee Fereidoon12345,Chang Andrew12345,Schiebel Johannes678910,Lu Yang12345,Zhang Zhuo12345,Kapilashrami Kanishk12345,Walker Stephen G.111345,Kisker Caroline678910,Sotriffer Christoph A.1281310,Fisher Stewart L.14155,Tonge Peter J.12345

Affiliation:

1. Institute for Chemical Biology & Drug Discovery

2. Department of Chemistry

3. Stony Brook University

4. Stony Brook

5. USA

6. Rudolf Virchow Center for Experimental Biomedicine

7. Institute for Structural Biology

8. University of Würzburg

9. D-97080 Würzburg

10. Germany

11. Department of Oral Biology and Pathology

12. Institute of Pharmacy and Food Chemistry

13. D-97074 Würzburg

14. The Broad Institute

15. Cambridge

Abstract

A mechanistic PK/PD model that enables predictions ofin vivodrug activity and an assessment of target vulnerability.

Funder

National Institute of General Medical Sciences

National Institutes of Health

Deutsche Forschungsgemeinschaft

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

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