Andrew L. Kung

Structural basis for recruitment of CBP/p300 by hypoxia-inducible factor-1 alpha.

Distinct roles for CREB-binding protein and p300 in hematopoietic stem cell self-renewal.

Inhibition of FLT3 in MLL. Validation of a therapeutic target identified by gene expression based classification.

Polyubiquitination of p53 by a ubiquitin ligase activity of p300.

Structural basis for negative regulation of hypoxia-inducible factor-1alpha by CITED2.

A small-molecule antagonist of CXCR4 inhibits intracranial growth of primary brain tumors.

Mouse reporter strain for noninvasive bioluminescent imaging of cells that have undergone Cre-mediated recombination.

Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors.

p53 targets simian virus 40 large T antigen for acetylation by CBP.

Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway.

Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix.

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

Dicer-deficient mouse embryonic stem cells are defective in differentiation and centromeric silencing.

Cyclin D1 represses p300 transactivation through a cyclin-dependent kinase-independent mechanism.

A HIF1alpha regulatory loop links hypoxia and mitochondrial signals in pheochromocytomas.

In vivo assessment of RAS-dependent maintenance of tumor angiogenesis by real-time magnetic resonance imaging.

Antimyeloma activity of heat shock protein-90 inhibition.

Widespread CXCR4 activation in astrocytomas revealed by phospho-CXCR4-specific antibodies.

Noninvasive bioluminescence imaging of luciferase expressing intracranial U87 xenografts: correlation with magnetic resonance imaging determined tumor volume and longitudinal use in assessing tumor growth and antiangiogenic treatment effect.

Prolonged dormancy of human liposarcoma is associated with impaired tumor angiogenesis.

A novel noninvasive model of endometriosis for monitoring the efficacy of antiangiogenic therapy.

Oncogenic MITF dysregulation in clear cell sarcoma: defining the MiT family of human cancers.

Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias.

Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity.

Mechanisms of regulation of CXCR4/SDF-1 (CXCL12)-dependent migration and homing in multiple myeloma.

CXCR4 inhibition synergizes with cytotoxic chemotherapy in gliomas.

Targeting the AIB1 oncogene through mammalian target of rapamycin inhibition in the mammary gland.

Practices and pitfalls of mouse cancer models in drug discovery.

Signature-based small molecule screening identifies cytosine arabinoside as an EWS/FLI modulator in Ewing sarcoma.

Potentiation of antileukemic therapies by Smac mimetic, LBW242: effects on mutant FLT3-expressing cells.

Therapeutic targeting of apoptosis pathways in cancer.

Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells.

Anti-apoptosis mechanisms in malignant gliomas.

Monoallele deletion of CBP leads to pericentromeric heterochromatin condensation through ESET expression and histone H3 (K9) methylation.

Stromal-mediated protection of tyrosine kinase inhibitor-treated BCR-ABL-expressing leukemia cells.

Expression-based screening identifies the combination of histone deacetylase inhibitors and retinoids for neuroblastoma differentiation.

The requirement for cyclin D function in tumor maintenance.

Pharmacologic suppression of MITF expression via HDAC inhibitors in the melanocyte lineage.

Resistance of human glioblastoma multiforme cells to growth factor inhibitors is overcome by blockade of inhibitor of apoptosis proteins.

Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells.

H3K79 methylation profiles define murine and human MLL-AF4 leukemias.

Desferroxamine infusion increases cerebral blood flow: a potential association with hypoxia-inducible factor-1.

HOXA9 is required for survival in human MLL-rearranged acute leukemias.

Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy.

Glioblastoma inhibition by cell surface immunoglobulin protein EWI-2, in vitro and in vivo.

CXCR4 inhibitor AMD3100 disrupts the interaction of multiple myeloma cells with the bone marrow microenvironment and enhances their sensitivity to therapy.

Lipocalin 2 promotes breast cancer progression.

Integrative analysis of HIF binding and transactivation reveals its role in maintaining histone methylation homeostasis.

The F-box protein beta-TrCp1/Fbw1a interacts with p300 to enhance beta-catenin transcriptional activity.

Fatty acid synthase: a metabolic enzyme and candidate oncogene in prostate cancer.

Identification of AML1-ETO modulators by chemical genomics.

HIF2alpha cooperates with RAS to promote lung tumorigenesis in mice.

In vivo pharmacodynamic imaging of proteasome inhibition.

Proteomic and genetic approaches identify Syk as an AML target.

CBP and p300 are cytoplasmic E4 polyubiquitin ligases for p53.

Systematic in vivo structure-function analysis of p300 in hematopoiesis.

Preferential binding of HIF-1 to transcriptionally active loci determines cell-type specific response to hypoxia.

Direct inhibition of the NOTCH transcription factor complex.

An activated ErbB3/NRG1 autocrine loop supports in vivo proliferation in ovarian cancer cells.

Tumor cell-specific bioluminescence platform to identify stroma-induced changes to anticancer drug activity.

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.

Discovery and characterization of novel mutant FLT3 kinase inhibitors.

Selective inhibition of BET bromodomains.

Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene.

A stapled p53 helix overcomes HDMX-mediated suppression of p53.

Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas.

Optical techniques for tracking multiple myeloma engraftment, growth, and response to therapy.

SCF(FBW7) regulates cellular apoptosis by targeting MCL1 for ubiquitylation and destruction.

Differentiation of NUT midline carcinoma by epigenomic reprogramming.

Crebbp haploinsufficiency in mice alters the bone marrow microenvironment, leading to loss of stem cells and excessive myelopoiesis.

A small-molecule IAP inhibitor overcomes resistance to cytotoxic therapies in malignant gliomas in vitro and in vivo.

Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.

Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation.

A class of human proteins that deliver functional proteins into mammalian cells in vitro and in vivo.

High-level IGF1R expression is required for leukemia-initiating cell activity in T-ALL and is supported by Notch signaling.

Green tea epigallocatechin-3-gallate inhibits angiogenesis and suppresses vascular endothelial growth factor C/vascular endothelial growth factor receptor 2 expression and signaling in experimental endometriosis in vivo.

BET bromodomain inhibition as a therapeutic strategy to target c-Myc.

Inactivation of a single copy of Crebbp selectively alters pre-mRNA processing in mouse hematopoietic stem cells.

Hypoxia-induced transcriptional repression of the melanoma-associated oncogene MITF.

P-selectin glycoprotein ligand regulates the interaction of multiple myeloma cells with the bone marrow microenvironment.

Mice heterozygous for CREB binding protein are hypersensitive to γ-radiation and invariably develop myelodysplastic/myeloproliferative neoplasm.

Molecular and cellular effects of NEDD8-activating enzyme inhibition in myeloma.

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.

Incongruity of imaging using fluorescent 2-DG conjugates compared to 18F-FDG in preclinical cancer models.

The intersection of genetic and chemical genomic screens identifies GSK-3α as a target in human acute myeloid leukemia.

Anti-inflammatory properties of histone deacetylase inhibitors: a mechanistic study.

Hypoxia promotes dissemination of multiple myeloma through acquisition of epithelial to mesenchymal transition-like features.

A murine lung cancer co-clinical trial identifies genetic modifiers of therapeutic response.

Chemical genomics identifies small-molecule MCL1 repressors and BCL-xL as a predictor of MCL1 dependency.

A stapled BIM peptide overcomes apoptotic resistance in hematologic cancers.

Autocrine activation of the MET receptor tyrosine kinase in acute myeloid leukemia.

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.

Targeted disruption of the BCL9/β-catenin complex inhibits oncogenic Wnt signaling.

Integrative analysis reveals an outcome-associated and targetable pattern of p53 and cell cycle deregulation in diffuse large B cell lymphoma.

In vivo imaging of inflammatory phagocytes.

In Vivo Fluorescent Labeling of Tumor Cells with the HaloTag® Technology.

The STAT5 Inhibitor Pimozide Displays Efficacy in Models of Acute Myelogenous Leukemia Driven by FLT3 Mutations.

Vascular endothelial growth factor C is increased in endometrium and promotes endothelial functions, vascular permeability and angiogenesis and growth of endometriosis.

KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.

Shikonin, a natural product from the root of Lithospermum erythrorhizon, is a cytotoxic DNA-binding agent.

Targeting MYCN in neuroblastoma by BET bromodomain inhibition.

Complementary genomic screens identify SERCA as a therapeutic target in NOTCH1 mutated cancer.

Oncogenic BRAF regulates oxidative metabolism via PGC1α and MITF.

High-throughput tyrosine kinase activity profiling identifies FAK as a candidate therapeutic target in Ewing sarcoma.

AML1-ETO mediates hematopoietic self-renewal and leukemogenesis through a COX/β-catenin signaling pathway.

Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation.

Metabolic and Functional Genomic Studies Identify Deoxythymidylate Kinase as a Target in LKB1-Mutant Lung Cancer.

Differential Disruption of EWS-FLI1 Binding by DNA-Binding Agents.