Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression

Discovery of (R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4-b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies

(2019) Hui-Ling Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

26S Proteasomes are rapidly activated by diverse hormones and physiological states that raise cAMP and cause Rpn6 phosphorylation

(2019) Jordan J. S. VerPlank et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

New Drugs in Multiple Myeloma

(2019) Chutima Kunacheewa et al.   Annual Review of Medicine

Forced expression of DYRK2 exerts anti-tumor effects via apoptotic induction in liver cancer

(2019) Shiho Yokoyama-Mashima et al.   CANCER LETTERS

Harmine, a dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor induces caspase-mediated apoptosis in neuroblastoma

(2018) Katie L. Uhl et al.   Cancer Cell International

Downregulation of dual-specificity tyrosine-regulated kinase 2 promotes tumor cell proliferation and invasion by enhancing cyclin-dependent kinase 14 expression in breast cancer

(2018) Yoshimi Imawari et al.   CANCER SCIENCE

Spectrum and functional validation of PSMB5 mutations in multiple myeloma

(2018) Santiago Barrio et al.   LEUKEMIA

Ancient drug curcumin impedes 26S proteasome activity by direct inhibition of dual-specificity tyrosine-regulated kinase 2

(2018) Sourav Banerjee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting Bcl-2 for the treatment of multiple myeloma

(2018) Cyrille Touzeau et al.   LEUKEMIA

Cryo-EM structures and dynamics of substrate-engaged human 26S proteasome

(2018) Yuanchen Dong et al.   NATURE

The Essential Medicinal Chemistry of Curcumin

(2017) Kathryn M. Nelson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Carfilzomib or bortezomib in relapsed or refractory multiple myeloma (ENDEAVOR): an interim overall survival analysis of an open-label, randomised, phase 3 trial

(2017) Meletios A Dimopoulos et al.   LANCET ONCOLOGY

Natural history of relapsed myeloma, refractory to immunomodulatory drugs and proteasome inhibitors: a multicenter IMWG study

(2017) S K Kumar et al.   LEUKEMIA

Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11

(2017) Jing Li et al.   Nature Chemical Biology

Anticancer activities of harmine by inducing a pro-death autophagy and apoptosis in human gastric cancer cells

(2017) Chuan Li et al.   PHYTOMEDICINE

Progress and Paradigms in Multiple Myeloma

(2016) Kenneth C. Anderson   CLINICAL CANCER RESEARCH

New Developments in Diagnosis, Prognosis, and Assessment of Response in Multiple Myeloma

(2016) Ola Landgren et al.   CLINICAL CANCER RESEARCH

Triple-negative breast cancer: challenges and opportunities of a heterogeneous disease

(2016) Giampaolo Bianchini et al.   Nature Reviews Clinical Oncology

Impairment of DYRK2 augments stem-like traits by promoting KLF4 expression in breast cancer

(2016) R Mimoto et al.   ONCOGENE

DUBbing Cancer: Deubiquitylating Enzymes Involved in Epigenetics, DNA Damage and the Cell Cycle As Therapeutic Targets

(2016) Adan Pinto-Fernandez et al.   Frontiers in Genetics

Phase 1 study of ixazomib, an investigational proteasome inhibitor, in advanced non-hematologic malignancies

(2015) David C. Smith et al.   INVESTIGATIONAL NEW DRUGS

Site-specific proteasome phosphorylation controls cell proliferation and tumorigenesis

(2015) Xing Guo et al.   NATURE CELL BIOLOGY

Copper–zinc superoxide dismutase-mediated redox regulation of bortezomib resistance in multiple myeloma

(2015) Kelley Salem et al.   Redox Biology

Pim-2 kinase is an important target of treatment for tumor progression and bone loss in myeloma

(2014) M Hiasa et al.   LEUKEMIA

A Genome-wide siRNA Screen Identifies Proteasome Addiction as a Vulnerability of Basal-like Triple-Negative Breast Cancer Cells

(2013) Fabio Petrocca et al.   CANCER CELL

Xbp1s-Negative Tumor B Cells and Pre-Plasmablasts Mediate Therapeutic Proteasome Inhibitor Resistance in Multiple Myeloma

(2013) Chungyee Leung-Hagesteijn et al.   CANCER CELL

DYRK2 controls the epithelial–mesenchymal transition in breast cancer by degrading Snail

(2013) Rei Mimoto et al.   CANCER LETTERS

Dual Specificity Kinase DYRK3 Couples Stress Granule Condensation/Dissolution to mTORC1 Signaling

(2013) Frank Wippich et al.   CELL

Conformational switching of the 26S proteasome enables substrate degradation

(2013) Mary E Matyskiela et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure–activity relationship study of beta-carboline derivatives as haspin kinase inhibitors

(2012) Gregory D. Cuny et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of proteasome inhibitors as research tools and cancer drugs

(2012) Alfred L. Goldberg   JOURNAL OF CELL BIOLOGY

Bortezomib resistance in a myeloma cell line is associated to PSMβ5 overexpression and polyploidy

(2011) Patricia Balsas et al.   LEUKEMIA RESEARCH

UBLCP1 is a 26S proteasome phosphatase that regulates nuclear proteasome activity

(2011) X. Guo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure–activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors

(2010) Gregory D. Cuny et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Kinome-wide RNAi studies in human multiple myeloma identify vulnerable kinase targets, including a lymphoid-restricted kinase, GRK6

(2009) R. E. Tiedemann et al.   BLOOD

Getting to First Base in Proteasome Assembly

(2009) Henrike C. Besche et al.   CELL

Molecular basis of bortezomib resistance: proteasome subunit  5 (PSMB5) gene mutation and overexpression of PSMB5 protein

(2008) R. Oerlemans et al.   BLOOD

Proteasome Inhibitors in Cancer Therapy: Lessons from the First Decade

(2008) R. Z. Orlowski et al.   CLINICAL CANCER RESEARCH