Pharmacodynamics and proteomic analysis of acalabrutinib therapy: similarity of on-target effects to ibrutinib and rationale for combination therapy

scientific article published on 3 November 2017

Pharmacodynamics and proteomic analysis of acalabrutinib therapy: similarity of on-target effects to ibrutinib and rationale for combination therapy is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1038/LEU.2017.321
P932PMC publication ID5871548
P698PubMed publication ID29099493

P50authorCristina IvanQ56435654
P2093author name stringM Nelson
J Gay
M J Keating
V Gandhi
V K Patel
J R Marszalek
K Balakrishnan
J Morse
M L Ayres
W G Wierda
B Lamothe
J P Cheung
P2860cites workGlycogen synthase kinase-3 regulates mitochondrial outer membrane permeabilization and apoptosis by destabilization of MCL-1Q24308005
High-level expression of the T-cell chemokines CCL3 and CCL4 by chronic lymphocytic leukemia B cells in nurselike cell cocultures and after BCR stimulationQ42184742
Ibrutinib antagonizes rituximab-dependent NK cell-mediated cytotoxicityQ42401591
Comparison of Acalabrutinib, A Selective Bruton Tyrosine Kinase Inhibitor, with Ibrutinib in Chronic Lymphocytic Leukemia CellsQ46055970
Combined BTK and PI3Kδ Inhibition with Acalabrutinib and ACP-319 Improves Survival and Tumor Control in CLL Mouse Model.Q46074725
Expression of apoptosis-regulating proteins in chronic lymphocytic leukemia: correlations with In vitro and In vivo chemoresponses.Q50893928
miR-15 and miR-16 induce apoptosis by targeting BCL2Q24536069
Frequent deletions and down-regulation of micro- RNA genes miR15 and miR16 at 13q14 in chronic lymphocytic leukemiaQ24539231
The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancyQ24633214
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing plateletsQ27683708
An inhibitor of Bcl-2 family proteins induces regression of solid tumoursQ29547595
FOXO transcription factors at the interface between longevity and tumor suppressionQ29620472
Regulation of protein stability by GSK3 mediated phosphorylationQ30437017
Ibrutinib as initial therapy for elderly patients with chronic lymphocytic leukaemia or small lymphocytic lymphoma: an open-label, multicentre, phase 1b/2 trialQ33412064
Direct in vivo evidence for increased proliferation of CLL cells in lymph nodes compared to bone marrow and peripheral bloodQ33774491
Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765.Q34026194
The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivoQ34029869
Ibrutinib versus ofatumumab in previously treated chronic lymphoid leukemiaQ34052075
Selective antitumor activity of ibrutinib in EGFR-mutant non-small cell lung cancer cellsQ34354339
Regulation of Mcl-1 expression in context to bone marrow stromal microenvironment in chronic lymphocytic leukemiaQ35022490
Chronic lymphocytic leukemia: revelations from the B-cell receptor.Q35667038
Pathological glycogenesis through glycogen synthase 1 and suppression of excessive AMP kinase activity in myeloid leukemia cellsQ35836470
Pharmacological and Protein Profiling Suggests Venetoclax (ABT-199) as Optimal Partner with Ibrutinib in Chronic Lymphocytic LeukemiaQ35958056
The phosphoinositide-3-kinase (PI3K)-delta and gamma inhibitor, IPI-145 (Duvelisib), overcomes signals from the PI3K/AKT/S6 pathway and promotes apoptosis in CLL.Q36021849
Treatment with Ibrutinib Inhibits BTK- and VLA-4-Dependent Adhesion of Chronic Lymphocytic Leukemia Cells In VivoQ36172601
Emerging role of kinase-targeted strategies in chronic lymphocytic leukemiaQ36462375
Ibrutinib as Initial Therapy for Patients with Chronic Lymphocytic LeukemiaQ36490049
GSK-3 beta targets Cdc25A for ubiquitin-mediated proteolysis, and GSK-3 beta inactivation correlates with Cdc25A overproduction in human cancers.Q36512934
Analysis of the Effects of the Bruton's tyrosine kinase (Btk) Inhibitor Ibrutinib on Monocyte Fcγ Receptor (FcγR) FunctionQ36548443
Disruption of in vivo Chronic Lymphocytic Leukemia Tumor-Microenvironment Interactions by Ibrutinib--Findings from an Investigator-Initiated Phase II StudyQ36759124
Autoantigen can promote progression to a more aggressive TCL1 leukemia by selecting variants with enhanced B-cell receptor signalingQ36782109
Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic LeukemiaQ36888218
Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1-selective pressure in T lymphocytesQ37226729
Targeting Bruton's tyrosine kinase in B cell malignanciesQ38198490
Ibrutinib for patients with relapsed or refractory chronic lymphocytic leukaemia with 17p deletion (RESONATE-17): a phase 2, open-label, multicentre studyQ38956893
Bruton's tyrosine kinase inhibition increases BCL-2 dependence and enhances sensitivity to venetoclax in chronic lymphocytic leukemiaQ39006397
Duvelisib treatment is associated with altered expression of apoptotic regulators that helps in sensitization of chronic lymphocytic leukemia cells to venetoclax (ABT-199).Q39065374
Ibrutinib modifies the function of monocyte/macrophage population in chronic lymphocytic leukemia.Q39414732
Chronic lymphocytic leukemia B cells express functional CXCR4 chemokine receptors that mediate spontaneous migration beneath bone marrow stromal cells.Q40916348
Bruton's tyrosine kinase: from X-linked agammaglobulinemia toward targeted therapy for B-cell malignanciesQ41524241
P433issue4
P921main subjectpharmacodynamicsQ725307
ibrutinibQ5984881
P304page(s)920-930
P577publication date2017-11-03
P1433published inLeukemiaQ6534498
P1476titlePharmacodynamics and proteomic analysis of acalabrutinib therapy: similarity of on-target effects to ibrutinib and rationale for combination therapy
P478volume32

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cites work (P2860)
Q91735722A pilot study of lower doses of ibrutinib in patients with chronic lymphocytic leukemia
Q91633231Acalabrutinib and Its Therapeutic Potential in the Treatment of Chronic Lymphocytic Leukemia: A Short Review on Emerging Data
Q97524840Resistance-Associated Mutations in Chronic Lymphocytic Leukemia Patients Treated With Novel Agents
Q57029282Splicing modulation sensitizes chronic lymphocytic leukemia cells to venetoclax by remodeling mitochondrial apoptotic dependencies
Q94671635Survey of ex vivo drug combination effects in chronic lymphocytic leukemia reveals synergistic drug effects and genetic dependencies

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