ACS Medicinal Chemistry Letters
Letter
Authors
NAD, nicotinamide adenine dinucleotide; SAR, structure−
activity relationship
Osamu Kurasawa − Pharmaceutical Research Division, Takeda
Pharmaceutical Company Limited, Fujisawa, Kanagawa 251-
8555, Japan
Akihiro Yokota − Pharmaceutical Research Division, Takeda
Pharmaceutical Company Limited, Fujisawa, Kanagawa 251-
8555, Japan
Michael G. Klein − Department of Structural Biology, Takeda
California, San Diego, California 92121, United States
Bunnai Saito − Pharmaceutical Research Division, Takeda
Pharmaceutical Company Limited, Fujisawa, Kanagawa 251-
8555, Japan
Shigemitsu Matsumoto − Pharmaceutical Research Division,
Takeda Pharmaceutical Company Limited, Fujisawa,
Kanagawa 251-8555, Japan
Masanori Okaniwa − Pharmaceutical Research Division,
Takeda Pharmaceutical Company Limited, Fujisawa,
Kanagawa 251-8555, Japan
Geza Ambrus-Aikelin − Department of Structural Biology,
Takeda California, San Diego, California 92121, United States
Noriko Uchiyama − Pharmaceutical Research Division, Takeda
Pharmaceutical Company Limited, Fujisawa, Kanagawa 251-
8555, Japan
Daisuke Morishita − Pharmaceutical Research Division, Takeda
Pharmaceutical Company Limited, Fujisawa, Kanagawa 251-
8555, Japan
Hiromichi Kimura − Pharmaceutical Research Division,
Takeda Pharmaceutical Company Limited, Fujisawa,
Kanagawa 251-8555, Japan
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Shinichi Imamura − Pharmaceutical Research Division, Takeda
Pharmaceutical Company Limited, Fujisawa, Kanagawa 251-
8555, Japan
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Complete contact information is available at:
Author Contributions
All authors contributed equally and have given approval to the
final version of the manuscript.
Notes
The authors declare no competing financial interest.
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ACKNOWLEDGMENTS
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We thank all members of the DHPS Program Team at Takeda
for their contribution. We thank Katsuaki Oda for assistance
with chiral separation and Mitsuyoshi Nishitani for assistance
with single-crystal X-ray study along with deposition of data to
the Cambridge Crystallographic Data Centre. We also thank
Weston Lane and Gyorgy Snell for diffraction data collection
and Jaya Bhatnagar for assistance with crystallization. The
GM/CA@APS has been funded in whole or in part with
federal funds from the National Cancer Institute (ACB-12002)
and the National Institute of General Medical Sciences (AGM-
12006). This research used resources of the Advanced Photon
Source, a U.S. Department of Energy (DOE) Office of Science
User Facility operated for the DOE Office of Science by
Argonne National Laboratory under Contract No. DE-AC02-
06CH11357.
ABBREVIATIONS
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DHPS, deoxyhypusine synthase; eIF5A, eukaryotic translation
initiation factor 5A; DOHH, deoxyhypusine hydroxylase;
G
ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX