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From Chemistry to the Clinic: Pathways for Drug Discovery and Development, Part 4: Design of Small Molecules Targeting Tumor Metabolism
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Optimization of glutaminase inhibitors for the treatment of cancer
Rene M. Lemieux
Agios Pharmaceuticals, Cambridge, MA, United States
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Discovery of in vivo inhibitors of Lactate Dehydrogenase A (LDHA)
Hans Purkey
Genentech, Inc., South San Francisco, CA, United States
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Discovery of a Potent, Selective, NAMPT inhibitor from the Pyridyloxyacetyl-Dihydro-Isoquinoline-Sulfonamide series that demonstrated robust efficacy and improved tolerability with nicotinic acid co-administration
Timothy P. Burkholder
Eli Lilly and Company, Indianapolis, IN, United States
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MCT1: The journey from phenotypic screen hit to clinical candidate
Jon Winter
AstraZeneca R&D, Cheshire, United Kingdom