Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

INCB16562, a JAK1/2 Selective Inhibitor, Is Efficacious against Multiple Myeloma Cells and Reverses the Protective Effects of Cytokine and Stromal Cell Support

(2015) Jun Li et al.   NEOPLASIA

Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

(2013) Mathew P. Martin et al.   ACS Chemical Biology

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

(2013) Michael Siu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD

(2013) C. C. Smith et al.   BLOOD

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

PI3K Pathway Dependencies in Endometrioid Endometrial Cancer Cell Lines

(2013) B. Weigelt et al.   CLINICAL CANCER RESEARCH

Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma

(2013) Z. Cheng et al.   CLINICAL CANCER RESEARCH

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

(2013) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transient Exposure to Quizartinib Mediates Sustained Inhibition of FLT3 Signaling while Specifically Inducing Apoptosis in FLT3-Activated Leukemia Cells

(2013) R. N. Gunawardane et al.   MOLECULAR CANCER THERAPEUTICS

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

(2013) S. Picaud et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Roles of p38 MAPKs in invasion and metastasis

(2012) Ivan del Barco Barrantes et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

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

(2012) C. J. Ott et al.   BLOOD

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

(2012) Panagis Filippakopoulos et al.   CELL

Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

(2012) Catherine C. Smith et al.   NATURE

A selective inhibitor reveals PI3Kγ dependence of TH17 cell differentiation

(2012) Giovanna Bergamini et al.   Nature Chemical Biology

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins

(2012) W. W. Lockwood et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF -Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib

(2012) Ryan B. Corcoran et al.   Cancer Discovery

Compensatory Pathways in Oncogenic Kinase Signaling and Resistance to Targeted Therapies: Six Degrees of Separation: Figure 1.

(2012) Livio Trusolino et al.   Cancer Discovery

Kinase inhibitors: a new class of antirheumatic drugs

(2012) Vasileios Kyttaris   Drug Design Development and Therapy

The Evolving War on Cancer

(2011) Daniel A. Haber et al.   CELL

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

(2011) Jake E. Delmore et al.   CELL

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

(2011) Oleg Fedorov et al.   CHEMISTRY & BIOLOGY

Bromodomains as therapeutic targets

(2011) Susanne Muller et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in Myelofibrosis

(2011) Animesh Pardanani et al.   JOURNAL OF CLINICAL ONCOLOGY

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

(2011) Martin Philpott et al.   Molecular BioSystems

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

(2011) Johannes Zuber et al.   NATURE

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

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

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells

(2010) Vijay Ramakrishnan et al.   AMERICAN JOURNAL OF HEMATOLOGY

Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1–C-Mad2 core complex

(2010) Laura Hewitt et al.   JOURNAL OF CELL BIOLOGY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity

(2009) D. Rudolph et al.   CLINICAL CANCER RESEARCH

Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design

(2009) Seungil Han et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Development of a Fluorescent-Tagged Kinase Assay System for the Detection and Characterization of Allosteric Kinase Inhibitors

(2009) Jeffrey R. Simard et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Chemical target and pathway toxicity mechanisms defined in primary human cell systems

(2009) Ellen L. Berg et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: Chemistry, biological activities, and molecular modeling

(2008) Yunsong Tong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Brivanib Alaninate ((S)-((R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinase Inhibitor (BMS-540215)

(2008) Zhen-wei Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY