Direct inhibition of the NOTCH transcription factor complex

[1]  Xudong Dai,et al.  Inhibition of NOTCH signaling by gamma secretase inhibitor engages the RB pathway and elicits cell cycle exit in T-cell acute lymphoblastic leukemia cells. , 2009, Cancer research.

[2]  Iannis Aifantis,et al.  γ-secretase inhibitors reverse glucocorticoid resistance in T cell acute lymphoblastic leukemia , 2009, Nature Medicine.

[3]  J. Aster,et al.  Leukemia-associated NOTCH1 alleles are weak tumor initiators but accelerate K-ras-initiated leukemia. , 2008, The Journal of clinical investigation.

[4]  Hans Clevers,et al.  Loss of intestinal crypt progenitor cells owing to inactivation of both Notch1 and Notch2 is accompanied by derepression of CDK inhibitors p27Kip1 and p57Kip2 , 2008, EMBO reports.

[5]  J. Aster,et al.  Mutational and energetic studies of Notch 1 transcription complexes. , 2008, Journal of molecular biology.

[6]  M D Alberto Lleo,et al.  Activity of γ -Secretase on Substrates Other than APP , 2008 .

[7]  J. Aster,et al.  Leukemia-associated NOTCH 1 alleles are weak tumor initiators but accelerate Kras – initiated leukemia , 2008 .

[8]  R D Wright,et al.  MLL-AF9 and FLT3 cooperation in acute myelogenous leukemia: development of a model for rapid therapeutic assessment , 2008, Leukemia.

[9]  Govind Bhagat,et al.  Mutational loss of PTEN induces resistance to NOTCH1 inhibition in T-cell leukemia , 2007, Nature Medicine.

[10]  T. Dang,et al.  Gamma-secretase inhibitor prevents Notch3 activation and reduces proliferation in human lung cancers. , 2007, Cancer research.

[11]  Rob Pieters,et al.  FBW7 mutations in leukemic cells mediate NOTCH pathway activation and resistance to γ-secretase inhibitors , 2007, The Journal of experimental medicine.

[12]  Jasmin R Gibson,et al.  An Improved β-Lactamase Reporter Assay: Multiplexing with a Cytotoxicity Readout for Enhanced Accuracy of Hit Identification , 2007, Journal of biomolecular screening.

[13]  Timothy Harrison,et al.  Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling. , 2007, Chemistry & biology.

[14]  Adam A. Margolin,et al.  NOTCH1 directly regulates c-MYC and activates a feed-forward-loop transcriptional network promoting leukemic cell growth , 2006, Proceedings of the National Academy of Sciences.

[15]  Paul A Clemons,et al.  The Connectivity Map: Using Gene-Expression Signatures to Connect Small Molecules, Genes, and Disease , 2006, Science.

[16]  S. Bray.  Notch signalling: a simple pathway becomes complex , 2006, Nature Reviews Molecular Cell Biology.

[17]  J. Aster,et al.  c-Myc is an important direct target of Notch1 in T-cell acute lymphoblastic leukemia/lymphoma. , 2006, Genes & development.

[18]  Tian-Li Wang,et al.  Notch3 gene amplification in ovarian cancer. , 2006, Cancer research.

[19]  Tae Funakoshi,et al.  A novel noninvasive model of endometriosis for monitoring the efficacy of antiangiogenic therapy. , 2006, The American journal of pathology.

[20]  Jon C. Aster,et al.  Structural Basis for Cooperativity in Recruitment of MAML Coactivators to Notch Transcription Complexes , 2006, Cell.

[21]  Rhett A. Kovall,et al.  Crystal Structure of the CSL-Notch-Mastermind Ternary Complex Bound to DNA , 2006, Cell.

[22]  Pablo Tamayo,et al.  Gene set enrichment analysis: A knowledge-based approach for interpreting genome-wide expression profiles , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[23]  D. Srivastava,et al.  Mutations in NOTCH1 cause aortic valve disease , 2005, Nature.

[24]  S. Artavanis-Tsakonas,et al.  Notch signals control the fate of immature progenitor cells in the intestine , 2005, Nature.

[25]  Patrick Maisonneuve,et al.  Loss of negative regulation by Numb over Notch is relevant to human breast carcinogenesis , 2004, The Journal of cell biology.

[26]  Andrew P. Weng,et al.  Activating Mutations of NOTCH1 in Human T Cell Acute Lymphoblastic Leukemia , 2004, Science.

[27]  David Allman,et al.  Mastermind critically regulates Notch-mediated lymphoid cell fate decisions. , 2004, Blood.

[28]  S. Korsmeyer,et al.  Activation of Apoptosis in Vivo by a Hydrocarbon-Stapled BH3 Helix , 2004, Science.

[29]  Yulia Nefedova,et al.  Involvement of Notch-1 signaling in bone marrow stroma-mediated de novo drug resistance of myeloma and other malignant lymphoid cell lines. , 2004, Blood.

[30]  Andrew P. Weng,et al.  Structural Requirements for Assembly of the CSL·Intracellular Notch1·Mastermind-like 1 Transcriptional Activation Complex* , 2003, Journal of Biological Chemistry.

[31]  R. Hruban,et al.  Notch mediates TGF alpha-induced changes in epithelial differentiation during pancreatic tumorigenesis. , 2003, Cancer cell.

[32]  Hans Clevers,et al.  Notch1 functions as a tumor suppressor in mouse skin , 2003, Nature Genetics.

[33]  James D. Griffin,et al.  Growth Suppression of Pre-T Acute Lymphoblastic Leukemia Cells by Inhibition of Notch Signaling , 2003, Molecular and Cellular Biology.

[34]  J. Darnell.  Transcription factors as targets for cancer therapy , 2002, Nature Reviews Cancer.

[35]  F. D. Miller,et al.  Functional gamma‐secretase inhibitors reduce beta‐amyloid peptide levels in brain , 2000, Journal of neurochemistry.

[36]  James D. Griffin,et al.  MAML1, a human homologue of Drosophila Mastermind, is a transcriptional co-activator for NOTCH receptors , 2000, Nature Genetics.

[37]  Robert A. Copeland,et al.  Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors* , 2000, The Journal of Biological Chemistry.

[38]  Jon C. Aster,et al.  Essential Roles for Ankyrin Repeat and Transactivation Domains in Induction of T-Cell Leukemia by Notch1 , 2000, Molecular and Cellular Biology.

[39]  G. Verdine,et al.  An All-Hydrocarbon Cross-Linking System for Enhancing the Helicity and Metabolic Stability of Peptides , 2000 .

[40]  J. Kimble,et al.  Mastermind is a putative activator for Notch , 2000, Current Biology.

[41]  S. Artavanis-Tsakonas,et al.  Notch signaling: cell fate control and signal integration in development. , 1999, Science.

[42]  Iva Greenwald,et al.  Presenilin is required for activity and nuclear access of Notch in Drosophila , 1999, Nature.

[43]  M. Fortini,et al.  Neurogenic phenotypes and altered Notch processing in Drosophila Presenilin mutants , 1999, Nature.

[44]  William J. Ray,et al.  A presenilin-1-dependent γ-secretase-like protease mediates release of Notch intracellular domain , 1999, Nature.

[45]  Colin C. Collins,et al.  Alagille syndrome is caused by mutations in human Jagged1, which encodes a ligand for Notch1 , 1997, Nature Genetics.

[46]  J. Weissenbach,et al.  Notch3 mutations in CADASIL, a hereditary adult-onset condition causing stroke and dementia , 1996, Nature.

[47]  D. Sassoon,et al.  Notch4/int-3, a mammary proto-oncogene, is an endothelial cell-specific mammalian Notch gene. , 1996, Development.

[48]  M. Fortini,et al.  The suppressor of hairless protein participates in notch receptor signaling , 1994, Cell.

[49]  R. Williams,et al.  Asymmetric Synthesis of Monosubstituted and α,α‐ Disubstituted α‐Amino Acids via Diastereoselective Glycine Enolate Alkylations. , 1992 .

[50]  Robert M. Williams,et al.  Asymmetric synthesis of monosubstituted and .alpha.,.alpha.-disubstituted .alpha.-amino acids via diastereoselective glycine enolate alkylations , 1991 .

[51]  J. Sklar,et al.  TAN-1, the human homolog of the Drosophila Notch gene, is broken by chromosomal translocations in T lymphoblastic neoplasms , 1991, Cell.

[52]  Y H Chen,et al.  Determination of the helix and beta form of proteins in aqueous solution by circular dichroism. , 1974, Biochemistry.