Controlling destiny through chemistry: small-molecule regulators of cell fate.

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Published in ACS Chem Biol on January 15, 2010

Authors

Ari J Firestone1, James K Chen

Author Affiliations

1: Department of Chemical and Systems Biology, Stanford University School of Medicine, Stanford, CA 94305, USA.

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Human homolog of patched, a candidate gene for the basal cell nevus syndrome. Science (1996) 8.06

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Prostaglandin E2 regulates vertebrate haematopoietic stem cell homeostasis. Nature (2007) 7.55

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Heterozygous germline mutations in BMPR2, encoding a TGF-beta receptor, cause familial primary pulmonary hypertension. Nat Genet (2000) 7.20

Alagille syndrome is caused by mutations in human Jagged1, which encodes a ligand for Notch1. Nat Genet (1997) 6.66

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