AKT as a therapeutic target in multiple myeloma

Pim2 is required for maintaining multiple myeloma cell growth through modulating TSC2 phosphorylation

(2013) J. Lu et al.   BLOOD

Diverse Mechanisms of AKT Pathway Activation in Human Malignancy

(2013) Mitchell Cheung et al.   CURRENT CANCER DRUG TARGETS

Critical Role of AKT Protein in Myeloma-induced Osteoclast Formation and Osteolysis

(2013) Huiling Cao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Knockdown of DEPTOR inhibits cell proliferation and increases chemosensitivity to melphalan in human multiple myeloma RPMI-8226 cells via inhibiting PI3K/AKT activity

(2013) Hao-Ran Zhang et al.   JOURNAL OF INTERNATIONAL MEDICAL RESEARCH

Continued improvement in survival in multiple myeloma: changes in early mortality and outcomes in older patients

(2013) S K Kumar et al.   LEUKEMIA

Autocrine insulin-like growth factor 1 and stem cell factor but not interleukin 6 support self-renewal of human myeloma cells

(2013) D Chiron et al.   Blood Cancer Journal

Combined targeting of MEK/MAPK and PI3K/Akt signalling in multiple myeloma

(2012) Torsten Steinbrunn et al.   BRITISH JOURNAL OF HAEMATOLOGY

The novel, orally bioavailable HSP90 inhibitor NVP-HSP990 induces cell cycle arrest and apoptosis in multiple myeloma cells and acts synergistically with melphalan by increased cleavage of caspases

(2012) Britta Lamottke et al.   EUROPEAN JOURNAL OF HAEMATOLOGY

Optimal induction of myeloma cell death requires dual blockade of phosphoinositide 3-kinase and mTOR signalling and is determined by translocation subtype

(2012) C Stengel et al.   LEUKEMIA

Improvement in long-term outcomes with successive Total Therapy trials for multiple myeloma: are patients now being cured?

(2012) S Z Usmani et al.   LEUKEMIA

Anti-Myeloma Activity of Akt Inhibition Is Linked to the Activation Status of PI3K/Akt and MEK/ERK Pathway

(2012) Vijay Ramakrishnan et al.   PLoS One

Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma

(2011) Philipp Baumann et al.   ANTI-CANCER DRUGS

Inhibition of heat shock protein 90 (HSP90) as a therapeutic strategy for the treatment of myeloma and other cancers

(2011) Paul G. Richardson et al.   BRITISH JOURNAL OF HAEMATOLOGY

Combination of Farnesyltransferase and Akt Inhibitors Is Synergistic in Breast Cancer Cells and Causes Significant Breast Tumor Regression in ErbB2 Transgenic Mice

(2011) M. E. Balasis et al.   CLINICAL CANCER RESEARCH

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

(2011) A. G. Gilmartin et al.   CLINICAL CANCER RESEARCH

The Pim Kinases: New Targets for Drug Development

(2011) Ronan Swords et al.   CURRENT DRUG TARGETS

Perifosine Plus Bortezomib and Dexamethasone in Patients With Relapsed/Refractory Multiple Myeloma Previously Treated With Bortezomib: Results of a Multicenter Phase I/II Trial

(2011) Paul G. Richardson et al.   JOURNAL OF CLINICAL ONCOLOGY

The serine/threonine kinase Pim-2 is a novel anti-apoptotic mediator in myeloma cells

(2011) J Asano et al.   LEUKEMIA

Risk of progression and survival in multiple myeloma relapsing after therapy with IMiDs and bortezomib: A multicenter international myeloma working group study

(2011) S K Kumar et al.   LEUKEMIA

Targeting HSP 90 Induces Apoptosis and Inhibits Critical Survival and Proliferation Pathways in Multiple Myeloma

(2011) T. Khong et al.   MOLECULAR CANCER THERAPEUTICS

A Mosaic Activating Mutation inAKT1Associated with the Proteus Syndrome

(2011) Marjorie J. Lindhurst et al.   NEW ENGLAND JOURNAL OF MEDICINE

Multiple Myeloma

(2011) Antonio Palumbo et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Survival and Size Are Differentially Regulated by Placental and Fetal PKBalpha/AKT1 in Mice1

(2010) Vicki Plaks et al.   BIOLOGY OF REPRODUCTION

Mutated RAS and constitutively activated Akt delineate distinct oncogenic pathways, which independently contribute to multiple myeloma cell survival

(2010) T. Steinbrunn et al.   BLOOD

An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo

(2010) Craig Cherrin et al.   CANCER BIOLOGY & THERAPY

The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane

(2010) N Berndt et al.   CELL DEATH AND DIFFERENTIATION

Dual Inhibition of Akt/Mammalian Target of Rapamycin Pathway byNanoparticle Albumin-Bound–Rapamycin and Perifosine Induces Antitumor Activity in Multiple Myeloma

(2010) Diana Cirstea et al.   MOLECULAR CANCER THERAPEUTICS

Molecular Pharmacology and Antitumor Activity of PHT-427, a Novel Akt/Phosphatidylinositide-Dependent Protein Kinase 1 Pleckstrin Homology Domain Inhibitor

(2010) E. J. Meuillet et al.   MOLECULAR CANCER THERAPEUTICS

Crystal Structure of Human AKT1 with an Allosteric Inhibitor Reveals a New Mode of Kinase Inhibition

(2010) Wen-I Wu et al.   PLoS One

AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer

(2009) Krishna M. Vasudevan et al.   CANCER CELL

In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models

(2009) K. P. Hoeflich et al.   CLINICAL CANCER RESEARCH

Probing Akt-inhibitor interaction by chemical cross-linking and mass spectrometry

(2009) Bill X. Huang et al.   JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY

Hotspot mutations of PIK3CA and AKT1 genes are absent in multiple myeloma

(2009) Said I. Ismail et al.   LEUKEMIA RESEARCH

Inhibitor hijacking of Akt activation

(2009) Tatsuya Okuzumi et al.   Nature Chemical Biology

Perifosine: Update on a novel Akt inhibitor

(2009) Joell J. Gills et al.   Current Oncology Reports

Role of a Novel PH-Kinase Domain Interface in PKB/Akt Regulation: Structural Mechanism for Allosteric Inhibition

(2009) Véronique Calleja et al.   PLOS BIOLOGY

AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines

(2008) D. S. Levy et al.   BLOOD

Combined functional and molecular analysis of tumor cell signaling defines 2 distinct myeloma subgroups: Akt-dependent and Akt-independent multiple myeloma

(2008) A. Zollinger et al.   BLOOD

Validation of PDGFR  and c-Src tyrosine kinases as tumor/vessel targets in patients with multiple myeloma: preclinical efficacy of the novel, orally available inhibitor dasatinib

(2008) A. M. L. Coluccia et al.   BLOOD

Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

(2008) N. Rhodes et al.   CANCER RESEARCH

Targeting Akt and Heat Shock Protein 90 Produces Synergistic Multiple Myeloma Cell Cytotoxicity in the Bone Marrow Microenvironment

(2008) A. Huston et al.   CLINICAL CANCER RESEARCH

Anticancer Alkylphospholipids: Mechanisms of Action, Cellular Sensitivity and Resistance, and Clinical Prospects

(2008) Wim van Blitterswijk et al.   CURRENT PHARMACEUTICAL DESIGN

Use of Akt Inhibitor and a Drug-resistant Mutant Validates a Critical Role for Protein Kinase B/Akt in the Insulin-dependent Regulation of Glucose and System A Amino Acid Uptake

(2008) Charlotte J. Green et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Clinical and biological significance of RAS mutations in multiple myeloma

(2008) W J Chng et al.   LEUKEMIA

Bone marrow microenvironment and the identification of new targets for myeloma therapy

(2008) K Podar et al.   LEUKEMIA

The oral protein-kinase Cβinhibitor enzastaurin (LY317615) suppresses signalling through the AKT pathway, inhibits proliferation and induces apoptosis in multiple myeloma cell lines

(2008) Antonino Neri et al.   LEUKEMIA & LYMPHOMA

Breast Tumor Cells with PI3K Mutation or HER2 Amplification Are Selectively Addicted to Akt Signaling

(2008) Qing-Bai She et al.   PLoS One

Interactions of myeloma cells with osteoclasts promote tumour expansion and bone degradation through activation of a complex signalling network and upregulation of cathepsin K, matrix metalloproteinases (MMPs) and urokinase plasminogen activator (uPA)

(2007) Monica Hecht et al.   EXPERIMENTAL CELL RESEARCH