Histone deacetylases are required for androgen receptor function in hormone-sensitive and castrate-resistant prostate cancer.

PubWeight™: 1.68‹?› | Rank: Top 3%

🔗 View Article (PMC 3219545)

Published in Cancer Res on January 27, 2009

Authors

Derek S Welsbie1, Jin Xu, Yu Chen, Laetitia Borsu, Howard I Scher, Neal Rosen, Charles L Sawyers

Author Affiliations

1: David Geffen School of Medicine, University of California at Los Angeles, Los Angeles, California, USA.

Articles citing this

Castration resistance in human prostate cancer is conferred by a frequently occurring androgen receptor splice variant. J Clin Invest (2010) 5.77

Histone deacetylase inhibitors: Potential in cancer therapy. J Cell Biochem (2009) 3.88

Starving the addiction: new opportunities for durable suppression of AR signaling in prostate cancer. Clin Cancer Res (2009) 3.61

Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents. J Hematol Oncol (2010) 2.94

New strategies in metastatic prostate cancer: targeting the androgen receptor signaling pathway. Clin Cancer Res (2011) 2.01

Mechanisms of the androgen receptor splicing in prostate cancer cells. Oncogene (2013) 1.67

Cooperation between Polycomb and androgen receptor during oncogenic transformation. Genome Res (2011) 1.47

HDAC inhibition impedes epithelial-mesenchymal plasticity and suppresses metastatic, castration-resistant prostate cancer. Oncogene (2015) 1.45

Nuclear receptor co-repressors are required for the histone-deacetylase activity of HDAC3 in vivo. Nat Struct Mol Biol (2013) 1.43

Rational therapeutic combinations with histone deacetylase inhibitors for the treatment of cancer. Future Oncol (2011) 1.34

The epigenome as a therapeutic target in prostate cancer. Nat Rev Urol (2010) 1.28

HDAC6 regulates androgen receptor hypersensitivity and nuclear localization via modulating Hsp90 acetylation in castration-resistant prostate cancer. Mol Endocrinol (2009) 1.15

Chromatin accessibility reveals insights into androgen receptor activation and transcriptional specificity. Genome Biol (2012) 1.15

CCN3/NOV gene expression in human prostate cancer is directly suppressed by the androgen receptor. Oncogene (2013) 1.12

Combinatorial antitumor effect of HDAC and the PI3K-Akt-mTOR pathway inhibition in a Pten defecient model of prostate cancer. Oncotarget (2013) 1.05

Novel targeted therapeutics for metastatic castration-resistant prostate cancer. Cancer Lett (2009) 1.04

Prostate cancer genes associated with TMPRSS2-ERG gene fusion and prognostic of biochemical recurrence in multiple cohorts. Br J Cancer (2010) 1.03

Impact of combined HDAC and mTOR inhibition on adhesion, migration and invasion of prostate cancer cells. Clin Exp Metastasis (2011) 1.00

The lysine demethylase, KDM4B, is a key molecule in androgen receptor signalling and turnover. Nucleic Acids Res (2013) 1.00

Pleiotropic functions of EAPII/TTRAP/TDP2: cancer development, chemoresistance and beyond. Cell Cycle (2011) 0.99

Regulators of gene expression as biomarkers for prostate cancer. Am J Cancer Res (2012) 0.98

Chemopreventive mechanisms of α-keto acid metabolites of naturally occurring organoselenium compounds. Amino Acids (2010) 0.96

Control of progesterone receptor transcriptional synergy by SUMOylation and deSUMOylation. BMC Mol Biol (2012) 0.94

The effect of food on the bioavailability of panobinostat, an orally active pan-histone deacetylase inhibitor, in patients with advanced cancer. Cancer Chemother Pharmacol (2011) 0.94

Concurrent HDAC and mTORC1 inhibition attenuate androgen receptor and hypoxia signaling associated with alterations in microRNA expression. PLoS One (2011) 0.93

Emerging therapeutic approaches in the management of metastatic castration-resistant prostate cancer. Prostate Cancer Prostatic Dis (2011) 0.93

Epigenetic regulation of androgen receptor signaling in prostate cancer. Epigenetics (2010) 0.92

Cooperative activation of cyclin D1 and progesterone receptor gene expression by the SRC-3 coactivator and SMRT corepressor. Mol Endocrinol (2010) 0.92

Redefining hormone resistance in prostate cancer. Ther Adv Med Oncol (2010) 0.91

New hormonal therapies for castration-resistant prostate cancer. Endocrinol Metab Clin North Am (2011) 0.90

A phase 2 study of intravenous panobinostat in patients with castration-resistant prostate cancer. Cancer Chemother Pharmacol (2013) 0.88

Interrogating genomic and epigenomic data to understand prostate cancer. Biochim Biophys Acta (2012) 0.85

Persistent androgen receptor addiction in castration-resistant prostate cancer. J Hematol Oncol (2015) 0.84

The association between histone 3 lysine 27 trimethylation (H3K27me3) and prostate cancer: relationship with clinicopathological parameters. BMC Cancer (2014) 0.83

Cells adapt to the epigenomic disruption caused by histone deacetylase inhibitors through a coordinated, chromatin-mediated transcriptional response. Epigenetics Chromatin (2015) 0.82

Novel therapies for the treatment of advanced prostate cancer. Curr Treat Options Oncol (2013) 0.82

Castration-resistant prostate cancer: new science and therapeutic prospects. Ther Adv Med Oncol (2010) 0.80

Future directions in castrate-resistant prostate cancer therapy. Clin Genitourin Cancer (2010) 0.79

Loss of the NKX3.1 tumorsuppressor promotes the TMPRSS2-ERG fusion gene expression in prostate cancer. BMC Cancer (2014) 0.79

Class I lysine deacetylases facilitate glucocorticoid-induced transcription. J Biol Chem (2013) 0.79

An integrative proteomics and interaction network-based classifier for prostate cancer diagnosis. PLoS One (2013) 0.79

New insights into the androgen-targeted therapies and epigenetic therapies in prostate cancer. Prostate Cancer (2011) 0.79

CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy. Horm Cancer (2016) 0.78

BAP18 coactivates androgen receptor action and promotes prostate cancer progression. Nucleic Acids Res (2016) 0.78

A genomic approach to predict synergistic combinations for breast cancer treatment. Pharmacogenomics J (2011) 0.77

A phase II study of the HDAC inhibitor SB939 in patients with castration resistant prostate cancer: NCIC clinical trials group study IND195. Invest New Drugs (2015) 0.77

Moving Beyond the Androgen Receptor (AR): Targeting AR-Interacting Proteins to Treat Prostate Cancer. Horm Cancer (2016) 0.77

Divergent Binding and Transactivation by Two Related Steroid Receptors at the Same Response Element. J Biol Chem (2016) 0.76

Epigenomic Regulation of Androgen Receptor Signaling: Potential Role in Prostate Cancer Therapy. Cancers (Basel) (2017) 0.75

Hybrid Enzalutamide Derivatives with Histone Deacetylase Inhibitor Activity Decrease Heat Shock Protein 90 and Androgen Receptor Levels and Inhibit Viability in Enzalutamide-Resistant C4-2 Prostate Cancer Cells. Mol Pharmacol (2016) 0.75

Androgens downregulate miR-21 expression in breast cancer cells underlining the protective role of androgen receptor. Oncotarget (2016) 0.75

Subchronic Toxicities of HZ1006, a Hydroxamate-Based Histone Deacetylase Inhibitor, in Beagle Dogs and Sprague-Dawley Rats. Int J Environ Res Public Health (2016) 0.75

Articles cited by this

Primer3 on the WWW for general users and for biologist programmers. Methods Mol Biol (2000) 128.08

Recurrent fusion of TMPRSS2 and ETS transcription factor genes in prostate cancer. Science (2005) 39.06

Molecular determinants of resistance to antiandrogen therapy. Nat Med (2003) 18.90

Cofactor dynamics and sufficiency in estrogen receptor-regulated transcription. Cell (2000) 11.10

Distinct classes of chromosomal rearrangements create oncogenic ETS gene fusions in prostate cancer. Nature (2007) 10.94

Estrogen receptor-alpha directs ordered, cyclical, and combinatorial recruitment of cofactors on a natural target promoter. Cell (2003) 10.42

A complex containing N-CoR, mSin3 and histone deacetylase mediates transcriptional repression. Nature (1997) 9.71

Nuclear receptor repression mediated by a complex containing SMRT, mSin3A, and histone deacetylase. Cell (1997) 8.99

Sensors and signals: a coactivator/corepressor/epigenetic code for integrating signal-dependent programs of transcriptional response. Genes Dev (2006) 6.32

Spatial and temporal recruitment of androgen receptor and its coactivators involves chromosomal looping and polymerase tracking. Mol Cell (2005) 5.38

TMPRSS2:ETV4 gene fusions define a third molecular subtype of prostate cancer. Cancer Res (2006) 4.99

Formation of the androgen receptor transcription complex. Mol Cell (2002) 4.93

A new human prostate carcinoma cell line, 22Rv1. In Vitro Cell Dev Biol Anim (1999) 4.93

Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors. J Biol Chem (2005) 4.62

Phase I clinical trial of histone deacetylase inhibitor: suberoylanilide hydroxamic acid administered intravenously. Clin Cancer Res (2003) 4.55

Suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses the growth of prostate cancer cells in vitro and in vivo. Cancer Res (2000) 3.83

17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts. Clin Cancer Res (2002) 3.72

Identification and functional significance of genes regulated by structurally different histone deacetylase inhibitors. Proc Natl Acad Sci U S A (2005) 3.66

Targeting the androgen receptor pathway in prostate cancer. Curr Opin Pharmacol (2008) 3.56

Combinatorial roles of the nuclear receptor corepressor in transcription and development. Cell (2000) 3.47

Gene expression profiling of multiple histone deacetylase (HDAC) inhibitors: defining a common gene set produced by HDAC inhibition in T24 and MDA carcinoma cell lines. Mol Cancer Ther (2003) 3.37

Histone deacetylases 1, 2 and 3 are highly expressed in prostate cancer and HDAC2 expression is associated with shorter PSA relapse time after radical prostatectomy. Br J Cancer (2008) 2.67

HDAC3: taking the SMRT-N-CoRrect road to repression. Oncogene (2007) 2.19

Androgen mediated regulation and functional implications of fkbp51 expression in prostate cancer. J Urol (2005) 2.01

Involvement of proteasome in the dynamic assembly of the androgen receptor transcription complex. J Biol Chem (2002) 1.90

Acetylation of androgen receptor enhances coactivator binding and promotes prostate cancer cell growth. Mol Cell Biol (2003) 1.89

Evolution of the androgen receptor pathway during progression of prostate cancer. Cancer Res (2006) 1.83

Locus-wide chromatin remodeling and enhanced androgen receptor-mediated transcription in recurrent prostate tumor cells. Mol Cell Biol (2006) 1.46

Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer cell proliferation. Mol Cancer Ther (2007) 1.32

Cooperative assembly of androgen receptor into a nucleoprotein complex that regulates the prostate-specific antigen enhancer. J Biol Chem (1999) 1.32

Chemical ablation of androgen receptor in prostate cancer cells by the histone deacetylase inhibitor LAQ824. Mol Cancer Ther (2005) 1.24

Divergent phenotypic patterns and commitment to apoptosis of Caco-2 cells during spontaneous and butyrate-induced differentiation. J Cell Physiol (2000) 1.16

Oestrogen receptor alpha increases p21(WAF1/CIP1) gene expression and the antiproliferative activity of histone deacetylase inhibitors in human breast cancer cells. J Endocrinol (2003) 1.05

Potentiation of androgen receptor transcriptional activity by inhibition of histone deacetylation--rescue of transcriptionally compromised mutants. J Endocrinol (2004) 1.03

Mechanisms of cell death induced by histone deacetylase inhibitors in androgen receptor-positive prostate cancer cells. Mol Cancer Res (2006) 1.02

Inhibition of histone deacetylation augments dihydrotestosterone induction of androgen receptor levels: an explanation for trichostatin A effects on androgen-induced chromatin remodeling and transcription of the mouse mammary tumor virus promoter. Exp Cell Res (1999) 0.86

Articles by these authors

The phosphatidylinositol 3-Kinase AKT pathway in human cancer. Nat Rev Cancer (2002) 28.11

Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med (2011) 27.58

Integrative genomic profiling of human prostate cancer. Cancer Cell (2010) 23.61

Molecular determinants of resistance to antiandrogen therapy. Nat Med (2003) 18.90

mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res (2006) 18.44

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature (2010) 17.31

BRAF mutation predicts sensitivity to MEK inhibition. Nature (2005) 17.14

Crucial role of p53-dependent cellular senescence in suppression of Pten-deficient tumorigenesis. Nature (2005) 15.83

Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med (2012) 15.69

Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors. N Engl J Med (2005) 15.42

Circulating tumor cells predict survival benefit from treatment in metastatic castration-resistant prostate cancer. Clin Cancer Res (2008) 14.37

Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science (2009) 13.87

Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med (2006) 13.54

Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell (2002) 13.03

Overriding imatinib resistance with a novel ABL kinase inhibitor. Science (2004) 11.83

Granulocyte-macrophage progenitors as candidate leukemic stem cells in blast-crisis CML. N Engl J Med (2004) 11.29

Circulating mitochondrial DAMPs cause inflammatory responses to injury. Nature (2010) 11.24

Enzalutamide in metastatic prostate cancer before chemotherapy. N Engl J Med (2014) 11.05

Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet (2010) 10.79

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature (2011) 10.77

Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis. J Clin Oncol (2005) 10.48

Reciprocal feedback regulation of PI3K and androgen receptor signaling in PTEN-deficient prostate cancer. Cancer Cell (2011) 7.32

Association between body-mass index and risk of death in more than 1 million Asians. N Engl J Med (2011) 6.89

(V600E)BRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway. Proc Natl Acad Sci U S A (2009) 6.78

AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity. Cancer Cell (2011) 6.74

Dynamics of chronic myeloid leukaemia. Nature (2005) 6.63

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A (2010) 6.54

Abiraterone acetate for treatment of metastatic castration-resistant prostate cancer: final overall survival analysis of the COU-AA-301 randomised, double-blind, placebo-controlled phase 3 study. Lancet Oncol (2012) 6.49

Symbiotic gut microbes modulate human metabolic phenotypes. Proc Natl Acad Sci U S A (2008) 6.42

Myc-driven murine prostate cancer shares molecular features with human prostate tumors. Cancer Cell (2003) 6.38

Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate. J Clin Oncol (2010) 5.86

Constitutively active androgen receptor splice variants expressed in castration-resistant prostate cancer require full-length androgen receptor. Proc Natl Acad Sci U S A (2010) 5.59

Antitumor activity of rapamycin in a Phase I trial for patients with recurrent PTEN-deficient glioblastoma. PLoS Med (2008) 5.54

Poor prognosis in carcinoma is associated with a gene expression signature of aberrant PTEN tumor suppressor pathway activity. Proc Natl Acad Sci U S A (2007) 5.44

Circulating tumor cell number and prognosis in progressive castration-resistant prostate cancer. Clin Cancer Res (2007) 5.36

Cooperativity of TMPRSS2-ERG with PI3-kinase pathway activation in prostate oncogenesis. Nat Genet (2009) 5.31

Arsenic exposure from drinking water, and all-cause and chronic-disease mortalities in Bangladesh (HEALS): a prospective cohort study. Lancet (2010) 5.12

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A (2005) 4.70

Phase II multicenter study of abiraterone acetate plus prednisone therapy in patients with docetaxel-treated castration-resistant prostate cancer. J Clin Oncol (2010) 4.64

Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain. PLoS Med (2006) 4.63

The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cells. Cancer Cell (2005) 4.48

4E-BP1 is a key effector of the oncogenic activation of the AKT and ERK signaling pathways that integrates their function in tumors. Cancer Cell (2010) 4.48

Hypoxia-inducible factor determines sensitivity to inhibitors of mTOR in kidney cancer. Nat Med (2005) 4.44

Differential exoprotease activities confer tumor-specific serum peptidome patterns. J Clin Invest (2006) 4.37

Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell (2002) 4.34

Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling. PLoS One (2008) 4.12

Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency. J Clin Invest (2007) 4.07

mTOR kinase inhibition causes feedback-dependent biphasic regulation of AKT signaling. Cancer Discov (2011) 4.05

Nomogram for overall survival of patients with progressive metastatic prostate cancer after castration. J Clin Oncol (2002) 3.93

Initial hormonal management of androgen-sensitive metastatic, recurrent, or progressive prostate cancer: 2006 update of an American Society of Clinical Oncology practice guideline. J Clin Oncol (2007) 3.91

Effect of abiraterone acetate and prednisone compared with placebo and prednisone on pain control and skeletal-related events in patients with metastatic castration-resistant prostate cancer: exploratory analysis of data from the COU-AA-301 randomised trial. Lancet Oncol (2012) 3.82

Rapid growth of a hepatocellular carcinoma and the driving mutations revealed by cell-population genetic analysis of whole-genome data. Proc Natl Acad Sci U S A (2011) 3.80

HER2/neu kinase-dependent modulation of androgen receptor function through effects on DNA binding and stability. Cancer Cell (2004) 3.79

Patient versus clinician symptom reporting using the National Cancer Institute Common Terminology Criteria for Adverse Events: results of a questionnaire-based study. Lancet Oncol (2006) 3.75

Drugging the cancer chaperone HSP90: combinatorial therapeutic exploitation of oncogene addiction and tumor stress. Ann N Y Acad Sci (2007) 3.74

17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts. Clin Cancer Res (2002) 3.72

Progress and promise of FDG-PET imaging for cancer patient management and oncologic drug development. Clin Cancer Res (2005) 3.71

Akt forms an intracellular complex with heat shock protein 90 (Hsp90) and Cdc37 and is destabilized by inhibitors of Hsp90 function. J Biol Chem (2002) 3.70

Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis. Cancer Cell (2008) 3.68

Starving the addiction: new opportunities for durable suppression of AR signaling in prostate cancer. Clin Cancer Res (2009) 3.61

Portable filter-based microdevice for detection and characterization of circulating tumor cells. Clin Cancer Res (2010) 3.61

Long-term toxicity monitoring via electronic patient-reported outcomes in patients receiving chemotherapy. J Clin Oncol (2007) 3.60

Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study. Blood (2002) 3.60

Glucocorticoid receptor confers resistance to antiandrogens by bypassing androgen receptor blockade. Cell (2013) 3.59

Plasma multianalyte profiling in mild cognitive impairment and Alzheimer disease. Neurology (2012) 3.58

Targeting the androgen receptor pathway in prostate cancer. Curr Opin Pharmacol (2008) 3.56

Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244). Cancer Res (2010) 3.54

Health Effects of Arsenic Longitudinal Study (HEALS): description of a multidisciplinary epidemiologic investigation. J Expo Sci Environ Epidemiol (2006) 3.53

Circulating tumor cell analysis in patients with progressive castration-resistant prostate cancer. Clin Cancer Res (2007) 3.53

Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol (2004) 3.51

Overcoming mutation-based resistance to antiandrogens with rational drug design. Elife (2013) 3.49

A novel type of cellular senescence that can be enhanced in mouse models and human tumor xenografts to suppress prostate tumorigenesis. J Clin Invest (2010) 3.47

Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas. Cancer Cell (2012) 3.37

Analysis of the phosphatidylinositol 3'-kinase signaling pathway in glioblastoma patients in vivo. Cancer Res (2003) 3.36

Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors. Oncogene (2003) 3.32

Mammalian target of rapamycin inhibition promotes response to epidermal growth factor receptor kinase inhibitors in PTEN-deficient and PTEN-intact glioblastoma cells. Cancer Res (2006) 3.31

Persistence of malignant hematopoietic progenitors in chronic myelogenous leukemia patients in complete cytogenetic remission following imatinib mesylate treatment. Blood (2003) 3.24

FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR. Nature (2011) 3.18

Pretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutations. Clin Cancer Res (2011) 3.15

Anti-androgens and androgen-depleting therapies in prostate cancer: new agents for an established target. Lancet Oncol (2009) 3.13

Tumor adaptation and resistance to RAF inhibitors. Nat Med (2013) 3.11

LIS1 RNA interference blocks neural stem cell division, morphogenesis, and motility at multiple stages. J Cell Biol (2005) 3.11

Phase 1 trial of high-dose exogenous testosterone in patients with castration-resistant metastatic prostate cancer. Eur Urol (2009) 3.11

Functional stoichiometry of the unitary calcium-release-activated calcium channel. Proc Natl Acad Sci U S A (2008) 3.07

Structure of the protein phosphatase 2A holoenzyme. Cell (2006) 3.07

Arsenic exposure from drinking water and risk of premalignant skin lesions in Bangladesh: baseline results from the Health Effects of Arsenic Longitudinal Study. Am J Epidemiol (2006) 2.93

AKT activity determines sensitivity to mammalian target of rapamycin (mTOR) inhibitors by regulating cyclin D1 and c-myc expression. J Biol Chem (2003) 2.88

Mutant BRAF melanomas--dependence and resistance. Cancer Cell (2011) 2.87

Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance. Proc Natl Acad Sci U S A (2005) 2.85

Combination of trastuzumab and tanespimycin (17-AAG, KOS-953) is safe and active in trastuzumab-refractory HER-2 overexpressing breast cancer: a phase I dose-escalation study. J Clin Oncol (2007) 2.80

Rapid induction of apoptosis by PI3K inhibitors is dependent upon their transient inhibition of RAS-ERK signaling. Cancer Discov (2014) 2.79