Small-molecule triggers of tadpole metamorphosis.
Small molecules that function as highly selective agonists and antagonists of cellular receptors comprise some of the most valuable therapeutic agents and molecular probes. A recent paper describes the design, synthesis, and evaluation of CO23, the first potent and specific agonist of thyroid hormone receptor-alpha (TRalpha), a member of the nuclear receptor (NR) superfamily of transcription factors. Together with previously reported TRbeta-selective agonists such as GC-1, these compounds represent powerful new tools for studying gene expression, signaling, differentiation, and development controlled by this important NR.
Peterson
Blake R
BR
Department of Chemistry, The Pennsylvania State University, University Park, Pennsylvania 16802, USA. brpeters@chem.psu.edu
D000818:Animals; D002454:Cell Differentiation; D002467:Cell Nucleus / Q000378:metabolism; D015195:Drug Design; D005786:Gene Expression Regulation; D007814:Larva; D008954:Models, Biological; D008956:Models, Chemical; D008958:Models, Molecular; D015398:Signal Transduction; D037021:Thyroid Hormone Receptors alpha / Q000819:agonists*; D014157:Transcription Factors / Q000378:metabolism; D014982:Xenopus laevis
D037021:Thyroid Hormone Receptors alpha; D014157:Transcription Factors