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Disrupted in Schizophrenia 1 Regulates Neuronal Progenitor Proliferation via Modulation of GSK3β/β-Catenin Signaling
The Disrupted in Schizophrenia 1 (DISC1) gene is disrupted by a balanced chromosomal translocation (1; 11) (q42; q14.3) in a Scottish family with a high incidence of major depression, schizophrenia,Expand
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Identifying the proteins to which small-molecule probes and drugs bind in cells
Most small-molecule probes and drugs alter cell circuitry by interacting with 1 or more proteins. A complete understanding of the interacting proteins and their associated protein complexes, whetherExpand
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A small molecule that binds Hedgehog and blocks its signaling in human cells
Small-molecule inhibition of extracellular proteins that activate membrane receptors has proved to be extremely challenging. Diversity-oriented synthesis and small-molecule microarrays enabled theExpand
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Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis.
Small molecule microarrays were screened to identify a small molecule ligand for Hap3p, a subunit of the yeast Hap2/3/4/5p transcription factor complex. The compound, named haptamide A, wasExpand
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Identification of cancer cytotoxic modulators of PDE3A by predictive chemogenomics
High cancer death rates indicate the need for new anti-cancer therapeutic agents. Approaches to discover new cancer drugs include target-based drug discovery and phenotypic screening. Here, weExpand
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The role of lysine 55 in determining the specificity of the purine repressor for its operators through minor groove interactions.
The interaction of the dimeric Escherichia coli purine repressor (PurR) with its cognate sequences leads to a 45 degrees to 50 degrees kink at a central CpG base step towards the major groove, asExpand
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Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles
Using a diverse collection of small molecules generated from a variety of sources, we measured protein-binding activities of each individual compound against each of 100 diverse (sequence-unrelated)Expand
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A complex task? Direct modulation of transcription factors with small molecules.
  • A. Koehler
  • Biology, Medicine
  • Current opinion in chemical biology
  • 1 June 2010
Transcription factors with aberrant activity in disease are promising yet untested targets for therapeutic development, particularly in oncology. Directly inhibiting or activating the function of aExpand
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A robust small-molecule microarray platform for screening cell lysates.
Herein we report the expanded functional group compatibility of small-molecule microarrays to include immobilization of primary alcohols, secondary alcohols, phenols, carboxylic acids, hydroxamicExpand
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Identification of Orai1 channel inhibitors by using minimal functional domains to screen small molecule microarrays.
Store-operated calcium (SOC) channels are vital for activation of the immune cells, and mutations in the channel result in severe combined immunodeficiency in human patients. In lymphocytes, SOCExpand
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