Targeting oncogenic and epigenetic survival pathways in lymphoma

Phase I study of CAL-101, an isoform-selective inhibitor of phosphatidylinositol 3‐kinase P110d, in patients with previously treated chronic lymphocytic leukemia.

(2017) S. E. Coutre et al.   JOURNAL OF CLINICAL ONCOLOGY

The management of patients with T1 adenocarcinoma of the low rectum: An updated decision analysis.

(2017) Calvin F. Johnston et al.   JOURNAL OF CLINICAL ONCOLOGY

The pan-deacetylase inhibitor panobinostat induces cell death and synergizes with everolimus in Hodgkin lymphoma cell lines

(2012) M. Lemoine et al.   BLOOD

A687V EZH2 is a gain-of-function mutation found in lymphoma patients

(2012) Christina R. Majer et al.   FEBS LETTERS

Panobinostat in Patients With Relapsed/Refractory Hodgkin's Lymphoma After Autologous Stem-Cell Transplantation: Results of a Phase II Study

(2012) Anas Younes et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Study of a Novel Oral Janus Kinase 2 Inhibitor, SB1518, in Patients With Relapsed Lymphoma: Evidence of Clinical and Biologic Activity in Multiple Lymphoma Subtypes

(2012) Anas Younes et al.   JOURNAL OF CLINICAL ONCOLOGY

Bruton Tyrosine Kinase Inhibitor Ibrutinib (PCI-32765) Has Significant Activity in Patients With Relapsed/Refractory B-Cell Malignancies

(2012) Ranjana H. Advani et al.   JOURNAL OF CLINICAL ONCOLOGY

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

(2012) Michael T. McCabe et al.   NATURE

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

(2012) Sarah K Knutson et al.   Nature Chemical Biology

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

(2012) M. T. McCabe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765

(2011) S. E. M. Herman et al.   BLOOD

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

(2011) Yan-Jie Zhang et al.   DRUG DISCOVERY TODAY

Phase II Study of Vorinostat for Treatment of Relapsed or Refractory Indolent Non-Hodgkin's Lymphoma and Mantle Cell Lymphoma

(2011) Mark Kirschbaum et al.   JOURNAL OF CLINICAL ONCOLOGY

Temsirolimus and rituximab in patients with relapsed or refractory mantle cell lymphoma: a phase 2 study

(2011) Stephen M Ansell et al.   LANCET ONCOLOGY

Mocetinostat for relapsed classical Hodgkin's lymphoma: an open-label, single-arm, phase 2 trial

(2011) Anas Younes et al.   LANCET ONCOLOGY

A phase 2 study of vorinostat for treatment of relapsed or refractory Hodgkin lymphoma: Southwest Oncology Group Study S0517

(2011) Mark H. Kirschbaum et al.   LEUKEMIA & LYMPHOMA

Inactivating mutations of acetyltransferase genes in B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

The Mammalian Class 3 PI3K (PIK3C3) Is Required for Early Embryogenesis and Cell Proliferation

(2011) Xiang Zhou et al.   PLoS One

Determinants of Sensitivity to DZNep Induced Apoptosis in Multiple Myeloma Cells

(2011) Zhigang Xie et al.   PLoS One

EZH2 Codon 641 Mutations are Common in BCL2-Rearranged Germinal Center B Cell Lymphomas

(2011) Russell J. H. Ryan et al.   PLoS One

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma

(2011) E Derenzini et al.   Blood Cancer Journal

EZH2-mediated epigenetic silencing in germinal center B cells contributes to proliferation and lymphomagenesis

(2010) I. Velichutina et al.   BLOOD

Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation

(2010) D. B. Yap et al.   BLOOD

Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2

(2010) K. Yu et al.   CANCER RESEARCH

Temsirolimus Has Activity in Non–Mantle Cell Non-Hodgkin's Lymphoma Subtypes: The University of Chicago Phase II Consortium

(2010) Sonali M. Smith et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase II trial of the oral mTOR inhibitor everolimus in relapsed aggressive lymphoma

(2010) T E Witzig et al.   LEUKEMIA

Oncogenically active MYD88 mutations in human lymphoma

(2010) Vu N. Ngo et al.   NATURE

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

(2010) R. Eric Davis et al.   NATURE

Helical assembly in the MyD88–IRAK4–IRAK2 complex in TLR/IL-1R signalling

(2010) Su-Chang Lin et al.   NATURE

Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2

(2010) Shuai Chen et al.   NATURE CELL BIOLOGY

Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin

(2010) Ryan D Morin et al.   NATURE GENETICS

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

(2010) C. J. Sneeringer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells

(2009) W. Fiskus et al.   BLOOD

Inhibition of Syk with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia

(2009) J. W. Friedberg et al.   BLOOD

AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity

(2009) C. M. Chresta et al.   CANCER RESEARCH

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

(2009) K. Yu et al.   CANCER RESEARCH

Phase III Study to Evaluate Temsirolimus Compared With Investigator's Choice Therapy for the Treatment of Relapsed or Refractory Mantle Cell Lymphoma

(2009) Georg Hess et al.   JOURNAL OF CLINICAL ONCOLOGY

DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation

(2009) T. B. Miranda et al.   MOLECULAR CANCER THERAPEUTICS

Phase II trial of oral vorinostat (suberoylanilide hydroxamic acid) in relapsed diffuse large-B-cell lymphoma

(2008) M. Crump et al.   ANNALS OF ONCOLOGY

Low-dose, single-agent temsirolimus for relapsed mantle cell lymphoma

(2008) Stephen M. Ansell et al.   CANCER

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

(2008) Beth Apsel et al.   Nature Chemical Biology

Cooperative signaling through the signal transducer and activator of transcription 3 and nuclear factor- B pathways in subtypes of diffuse large B-cell lymphoma

(2007) L. T. Lam et al.   BLOOD