Chemical Phosphoproteomics Sheds New Light on the Targets and Modes of Action of AKT Inhibitors

A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity

(2020) Eleftherios Kostaras et al.   BRITISH JOURNAL OF CANCER

Chemoproteomic Selectivity Profiling of PIKK and PI3K Kinase Inhibitors

(2019) Maria Reinecke et al.   ACS Chemical Biology

The ER Contact Proteins VAPA/B Interact with Multiple Autophagy Proteins to Modulate Autophagosome Biogenesis

(2018) Yan G. Zhao et al.   CURRENT BIOLOGY

Mechanism and medical implications of mammalian autophagy

(2018) Ivan Dikic et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Increased autophagy blocks HER2-mediated breast tumorigenesis

(2018) Silvia Vega-Rubín-de-Celis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The target landscape of clinical kinase drugs

(2017) Susan Klaeger et al.   SCIENCE

Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo

(2017) Lan Zhang et al.   Chemical Science

Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors

(2016) Susan Klaeger et al.   ACS Chemical Biology

AKT1 E17K mutation profiling in breast cancer: prevalence, concurrent oncogenic alterations, and blood-based detection

(2016) Marion Rudolph et al.   BMC CANCER

Elevated levels of autophagy-related marker ULK1 and mitochondrion-associated autophagy inhibitor LRPPRC are associated with biochemical progression and overall survival after androgen deprivation therapy in patients with metastatic prostate cancer

(2016) Hong-Yi Zhang et al.   JOURNAL OF CLINICAL PATHOLOGY

Glutathione biosynthesis is a metabolic vulnerability in PI(3)K/Akt-driven breast cancer

(2016) Evan C. Lien et al.   NATURE CELL BIOLOGY

The STRING database in 2017: quality-controlled protein–protein association networks, made broadly accessible

(2016) Damian Szklarczyk et al.   NUCLEIC ACIDS RESEARCH

Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors

(2015) Toshihiko Doi et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Optimized Chemical Proteomics Assay for Kinase Inhibitor Profiling

(2015) Guillaume Médard et al.   JOURNAL OF PROTEOME RESEARCH

Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092

(2015) Yi Yu et al.   PLoS One

The Metastasis Suppressor, N-myc Downstream-regulated Gene 1 (NDRG1), Inhibits Stress-induced Autophagy in Cancer Cells

(2014) Sumit Sahni et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phosphoproteomics Screen Reveals Akt Isoform-Specific Signals Linking RNA Processing to Lung Cancer

(2014) Ioannis Sanidas et al.   MOLECULAR CELL

Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor

(2014) Melissa Dumble et al.   PLoS One

Tracking cancer drugs in living cells by thermal profiling of the proteome

(2014) M. M. Savitski et al.   SCIENCE

A novel mechanism of keratin cytoskeleton organization through casein kinase I  and FAM83H in colorectal cancer

(2013) T. Kuga et al.   JOURNAL OF CELL SCIENCE

Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases

(2013) Matt Addie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors

(2012) James F. Blake et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preclinical Pharmacology of AZD5363, an Inhibitor of AKT: Pharmacodynamics, Antitumor Activity, and Correlation of Monotherapy Activity with Genetic Background

(2012) B. R. Davies et al.   MOLECULAR CANCER THERAPEUTICS

Small molecule-induced cytosolic activation of protein kinase Akt rescues ischemia-elicited neuronal death

(2012) H. Jo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Akt-Mediated Regulation of Autophagy and Tumorigenesis Through Beclin 1 Phosphorylation

(2012) R. C. Wang et al.   SCIENCE

AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity

(2011) Sarat Chandarlapaty et al.   CANCER CELL

A Mosaic Activating Mutation inAKT1Associated with the Proteus Syndrome

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

MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo

(2010) H. Hirai et al.   MOLECULAR CANCER THERAPEUTICS

In vitro and In vivo Activity of Novel Small-Molecule Inhibitors Targeting the Pleckstrin Homology Domain of Protein Kinase B/AKT

(2009) S. A. Moses et al.   CANCER RESEARCH

Akt-dependent and -independent mechanisms of mTOR regulation in cancer

(2009) Regan M. Memmott et al.   CELLULAR SIGNALLING

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

(2009) Véronique Calleja et al.   PLOS BIOLOGY

Mechanism and Management of AKT Inhibitor-Induced Hyperglycemia

(2008) M.-C. Crouthamel et al.   CLINICAL CANCER RESEARCH

Akt regulates centrosome migration and spindle orientation in the earlyDrosophila melanogasterembryo

(2008) Graham J. Buttrick et al.   JOURNAL OF CELL BIOLOGY

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase

(2008) Dirk A. Heerding et al.   JOURNAL OF MEDICINAL CHEMISTRY