Targeting PDK1 for Chemosensitization of Cancer Cells

AGC kinases, mechanisms of regulation ‎and innovative drug development

(2018) Alejandro E. Leroux et al.   SEMINARS IN CANCER BIOLOGY

PDK1: At the crossroad of cancer signaling pathways

(2018) Paolo Armando Gagliardi et al.   SEMINARS IN CANCER BIOLOGY

Akt activation by Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) in ovarian cancer cells

(2017) Angela M. Gocher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242

(2017) Chunmei Yang et al.   Oncotarget

TCRP1 promotes NIH/3T3 cell transformation by over-activating PDK1 and AKT1

(2017) C Wang et al.   Oncogenesis

Timp1 Promotes Cell Survival by Activating the PDK1 Signaling Pathway in Melanoma

(2017) Mariana Toricelli et al.   Cancers

Serine/Threonine Kinase 3-Phosphoinositide-Dependent Protein Kinase-1 (PDK1) as a Key Regulator of Cell Migration and Cancer Dissemination

(2017) Laura Di Blasio et al.   Cancers

Dual Inhibition of PDK1 and Aurora Kinase A: An Effective Strategy to Induce Differentiation and Apoptosis of Human Glioblastoma Multiforme Stem Cells

(2016) Simona Daniele et al.   ACS Chemical Neuroscience

PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition

(2016) Pau Castel et al.   CANCER CELL

The hVps34‐SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth

(2016) Ruzica Bago et al.   EMBO JOURNAL

Correlation of PDK1 expression with clinicopathologic features and prognosis of hepatocellular carcinoma

(2016) Xiuying Wu et al.   OncoTargets and Therapy

A Small Molecule Inhibitor of PDK1/PLCγ1 Interaction Blocks Breast and Melanoma Cancer Cell Invasion

(2016) Claudio Raimondi et al.   Scientific Reports

Phosphoinositide-dependent kinase 1 regulates leukemia stem cell maintenance in MLL-AF9-induced murine acute myeloid leukemia

(2015) Tianyuan Hu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

PDK1: A signaling hub for cell migration and tumor invasion

(2015) Paolo Armando Gagliardi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

PDK1 and SGK3 Contribute to the Growth of BRAF-Mutant Melanomas and Are Potential Therapeutic Targets

(2015) M. Scortegagna et al.   CANCER RESEARCH

Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme

(2015) Simona Sestito et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Abstract C198: PDK1 inhibitors SNS-229 and SNS-510 cause pathway modulation, apoptosis and tumor regression in hematologic cancer models in addition to solid tumors

(2015) Stig Hansen et al.   MOLECULAR CANCER THERAPEUTICS

Regulation of mTORC1 by PI3K signaling

(2015) Christian C. Dibble et al.   TRENDS IN CELL BIOLOGY

PDK1 induces JunB, EMT, cell migration and invasion in human gallbladder cancer

(2015) Shixian Lian et al.   Oncotarget

COL11A1 confers chemoresistance on ovarian cancer cells through the activation of Akt/c/EBPβ pathway and PDK1 stabilization

(2015) Yi-Hui Wu et al.   Oncotarget

3-Phosphoinositide-Dependent Kinase 1 Controls Breast Tumor Growth in a Kinase-Dependent but Akt-Independent Manner

(2015) Paolo Armando Gagliardi et al.   NEOPLASIA

Curcumin restores sensitivity to retinoic acid in triple negative breast cancer cells

(2014) Padmamalini Thulasiraman et al.   BMC CANCER

TCRP1 contributes to cisplatin resistance by preventing Pol β degradation in lung cancer cells

(2014) Xiaorong Liu et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

BRAF V600E Cooperates with PI3K Signaling, Independent of AKT, to Regulate Melanoma Cell Proliferation

(2014) Jillian M. Silva et al.   MOLECULAR CANCER RESEARCH

PI3K and cancer: lessons, challenges and opportunities

(2014) David A. Fruman et al.   NATURE REVIEWS DRUG DISCOVERY

The 16p13.3 (PDPK1) Genomic Gain in Prostate Cancer: A Potential Role in Disease Progression

(2014) Khalil A. Choucair et al.   Translational Oncology

FOXO transcription factors: key regulators of cellular quality control

(2014) Ashley E. Webb et al.   TRENDS IN BIOCHEMICAL SCIENCES

Emerging role of the KRAS-PDK1 axis in pancreatic cancer

(2014) Riccardo Ferro   WORLD JOURNAL OF GASTROENTEROLOGY

Combined PDK1 and CHK1 inhibition is required to kill glioblastoma stem-like cells in vitro and in vivo

(2014) M Signore et al.   Cell Death & Disease

Elevated SGK1 predicts resistance of breast cancer cells to Akt inhibitors

(2013) Eeva M. Sommer et al.   BIOCHEMICAL JOURNAL

AGC protein kinases: From structural mechanism of regulation to allosteric drug development for the treatment of human diseases

(2013) José M. Arencibia et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Selective Requirement of PI3K/PDK1 Signaling for Kras Oncogene-Driven Pancreatic Cell Plasticity and Cancer

(2013) Stefan Eser et al.   CANCER CELL

The PDK1 master kinase is over-expressed in acute myeloid leukemia and promotes PKC-mediated survival of leukemic blasts

(2013) J. Zabkiewicz et al.   HAEMATOLOGICA

The Importance of the PI3K/AKT/MTOR Pathway in the Progression of Ovarian Cancer

(2013) Zachary Dobbin et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

PDK1 decreases TACE-mediated α-secretase activity and promotes disease progression in prion and Alzheimer's diseases

(2013) Mathéa Pietri et al.   NATURE MEDICINE

Activation of PDK-1 maintains mouse embryonic stem cell self-renewal in a PKB-dependent manner

(2013) L S Ling et al.   ONCOGENE

Regulation of Hippo pathway by mitogenic growth factors via phosphoinositide 3-kinase and phosphoinositide-dependent kinase-1

(2013) R. Fan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

mTORC1 Inhibition Is Required for Sensitivity to PI3K p110  Inhibitors in PIK3CA-Mutant Breast Cancer

(2013) M. Elkabets et al.   Science Translational Medicine

Synthesis of Novel 3,5-Disubstituted-2-oxindole Derivatives As Antitumor Agents against Human Nonsmall Cell Lung Cancer

(2013) Giulia Nesi et al.   ACS Medicinal Chemistry Letters

PDK1 Signaling Toward PLK1-MYC Activation Confers Oncogenic Transformation, Tumor-Initiating Cell Activation, and Resistance to mTOR-Targeted Therapy

(2013) J. Tan et al.   Cancer Discovery

Akt is efficiently activated by PIF-pocket- and PtdIns(3,4,5)P3-dependent mechanisms leading to resistance to PDK1 inhibitors

(2012) Ayaz Najafov et al.   BIOCHEMICAL JOURNAL

Interaction of PDK1 with Phosphoinositides Is Essential for Neuronal Differentiation but Dispensable for Neuronal Survival

(2012) T. Zurashvili et al.   MOLECULAR AND CELLULAR BIOLOGY

PDK1 Attenuation Fails to Prevent Tumor Formation in PTEN-Deficient Transgenic Mouse Models

(2011) K. Ellwood-Yen et al.   CANCER RESEARCH

Targeting PDK1 in Cancer

(2011) C. Raimondi et al.   CURRENT MEDICINAL CHEMISTRY

TCRP1 promotes radioresistance of oral squamous cell carcinoma cells via Akt signal pathway

(2011) Yixue Gu et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

The Hippo pathway transcriptional co-activator, YAP, is an ovarian cancer oncogene

(2011) X Zhang et al.   ONCOGENE

Knockdown of MTDH Sensitizes Endometrial Cancer Cells to Cell Death Induction by Death Receptor Ligand TRAIL and HDAC Inhibitor LBH589 Co-Treatment

(2011) Xiangbing Meng et al.   PLoS One

Identification of Direct Target Engagement Biomarkers for Kinase-Targeted Therapeutics

(2011) Cloud P. Paweletz et al.   PLoS One

Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1

(2010) Ayaz Najafov et al.   BIOCHEMICAL JOURNAL

A novel inhibitor of the PI3K/Akt pathway based on the structure of inositol 1,3,4,5,6-pentakisphosphate

(2010) M Falasca et al.   BRITISH JOURNAL OF CANCER

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

The Hippo Signaling Pathway in Development and Cancer

(2010) Duojia Pan   DEVELOPMENTAL CELL

Genetic and Pharmacological Inhibition of PDK1 in Cancer Cells

(2010) Kumiko Nagashima et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Genetic inactivation of AKT1, AKT2, and PDPK1 in human colorectal cancer cells clarifies their roles in tumor growth regulation

(2010) K. Ericson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

3-Phosphoinositide-Dependent Kinase 1 Potentiates Upstream Lesions on the Phosphatidylinositol 3-Kinase Pathway in Breast Carcinoma

(2009) M. Maurer et al.   CANCER RESEARCH

Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells

(2009) Tina X. Lee et al.   EUROPEAN JOURNAL OF CANCER

New anti-cancer role for PDK1 inhibitors: preventing resistance to tamoxifen

(2008) Christian Peifer et al.   BIOCHEMICAL JOURNAL

Parallel RNAi and compound screens identify the PDK1 pathway as a target for tamoxifen sensitization

(2008) Elizabeth Iorns et al.   BIOCHEMICAL JOURNAL

An immunohistochemical perspective of PPARβ and one of its putative targets PDK1 in normal ovaries, benign and malignant ovarian tumours

(2008) N Ahmed et al.   BRITISH JOURNAL OF CANCER

TUSC4/NPRL2, a novel PDK1-interacting protein, inhibits PDK1 tyrosine phosphorylation and its downstream signaling

(2008) Atsuo Kurata et al.   CANCER SCIENCE

Module Map of Stem Cell Genes Guides Creation of Epithelial Cancer Stem Cells

(2008) David J. Wong et al.   Cell Stem Cell

Role of PDK1 in Regulation of Gastric Acid Secretion

(2008) Anand Rotte et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Small-Molecule Inhibitors of PDK1

(2008) Christian Peifer et al.   ChemMedChem

TEAD mediates YAP-dependent gene induction and growth control

(2008) B. Zhao et al.   GENES & DEVELOPMENT

Targeting survival cascades induced by activation of Ras/Raf/MEK/ERK, PI3K/PTEN/Akt/mTOR and Jak/STAT pathways for effective leukemia therapy

(2008) J A McCubrey et al.   LEUKEMIA

Freud-1/Aki1, a Novel PDK1-Interacting Protein, Functions as a Scaffold To Activate the PDK1/Akt Pathway in Epidermal Growth Factor Signaling

(2008) A. Nakamura et al.   MOLECULAR AND CELLULAR BIOLOGY

Mutation of the PDK1 PH Domain Inhibits Protein Kinase B/Akt, Leading to Small Size and Insulin Resistance

(2008) J. R. Bayascas et al.   MOLECULAR AND CELLULAR BIOLOGY

Sensitizing estrogen receptor-negative breast cancer cells to tamoxifen with OSU-03012, a novel celecoxib-derived phosphoinositide-dependent protein kinase-1/Akt signaling inhibitor

(2008) S.-C. Weng et al.   MOLECULAR CANCER THERAPEUTICS

PDK1 regulates cancer cell motility by antagonising inhibition of ROCK1 by RhoE

(2008) Sophie Pinner et al.   NATURE CELL BIOLOGY