p21-Activated kinase inhibitors: a patent review

Phase I, dose-escalation, safety, pharmacokinetic, and pharmacodynamic study of single-agent PF-03758309, an oral PAK inhibitor, in patients with advanced solid tumors.

(2017) L. R. Mileshkin et al.   JOURNAL OF CLINICAL ONCOLOGY

p21-activated kinase 1: PAK’ed with potential

(2015) Christy Ong et al.   Oncotarget

From Conventional to Unusual Enzyme Inhibitor Scaffolds: The Quest for Target Specificity

(2011) Eric Meggers   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Role of the p21-activated kinases (PAKs) in influenza A virus replication

(2011) Philippe Noriel Q. Pascua et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells

(2011) Jian Zhang et al.   CANCER LETTERS

The Methylation Effect in Medicinal Chemistry

(2011) Eliezer J. Barreiro et al.   CHEMICAL REVIEWS

A key role for Pak4 in proliferation and differentiation of neural progenitor cells

(2011) Yanmei Tian et al.   DEVELOPMENTAL BIOLOGY

Inhibition or Ablation of p21-activated Kinase (PAK1) Disrupts Glucose Homeostatic Mechanismsin Vivo

(2011) Zhanxiang Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selectivity of Kinase Inhibitor Fragments

(2011) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

The influence of the 'organizational factor' on compound quality in drug discovery

(2011) Paul D. Leeson et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells

(2011) C. C. Ong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties

(2010) Travis T. Wager et al.   ACS Chemical Neuroscience

The emerging importance of group II PAKs

(2010) Claire M. Wells et al.   BIOCHEMICAL JOURNAL

Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity

(2010) Simona Bindi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of 5-Chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a Novel Inhibitor of the Jak/Stat Pathway

(2010) Stephanos Ioannidis et al.   JOURNAL OF MEDICINAL CHEMISTRY

p21-Activated Kinases 1 and 3 Control Brain Size through Coordinating Neuronal Complexity and Synaptic Properties

(2010) W. Huang et al.   MOLECULAR AND CELLULAR BIOLOGY

A Functional Requirement for PAK1 Binding to the KH(2) Domain of the Fragile X Protein-Related FXR1

(2010) Evonne Say et al.   MOLECULAR CELL

The protein kinase Pak4 disrupts mammary acinar architecture and promotes mammary tumorigenesis

(2010) Y Liu et al.   ONCOGENE

A Rac–Pak signaling pathway is essential for ErbB2-mediated transformation of human breast epithelial cancer cells

(2010) L E Arias-Romero et al.   ONCOGENE

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth

(2010) B. W. Murray et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Why an A-Loop Phospho-Mimetic Fails to Activate PAK1: Understanding an Inaccessible Kinase State by Molecular Dynamics Simulations

(2010) Yuen-Wai Ng et al.   STRUCTURE

An emerging role for p21-activated kinases (Paks) in viral infections

(2010) Celine Van den Broeke et al.   TRENDS IN CELL BIOLOGY

The discovery of the potent aurora inhibitor MK-0457 (VX-680)

(2009) David Bebbington et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles

(2009) Hong Lin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

p21-activated kinase regulates mast cell degranulation via effects on calcium mobilization and cytoskeletal dynamics

(2009) J. D. Allen et al.   BLOOD

Pak protein kinases and their role in cancer

(2009) Bettina Dummler et al.   CANCER AND METASTASIS REVIEWS

Essential role for the Pak4 protein kinase in extraembryonic tissue development and vessel formation

(2009) Yanmei Tian et al.   MECHANISMS OF DEVELOPMENT

An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently

(2009) J. Viaud et al.   MOLECULAR CANCER THERAPEUTICS

Pharmacophore identification of PAK4 inhibitors

(2009) Jian Wang et al.   MOLECULAR SIMULATION

Human host factors required for influenza virus replication

(2009) Renate König et al.   NATURE

Alphaherpesvirus US3-mediated reorganization of the actin cytoskeleton is mediated by group A p21-activated kinases

(2009) C. Van den Broeke et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A tale of two Paks

(2008) Luis E. Arias-Romero et al.   BIOLOGY OF THE CELL

PAK signalling in neuronal physiology

(2008) Patricia Kreis et al.   CELLULAR SIGNALLING

An Isoform-Selective, Small-Molecule Inhibitor Targets the Autoregulatory Mechanism of p21-Activated Kinase

(2008) Sean W. Deacon et al.   CHEMISTRY & BIOLOGY

Targeted disruption of the Pak5 and Pak6 genes in mice leads to deficits in learning and locomotion

(2008) Tanya Nekrasova et al.   DEVELOPMENTAL BIOLOGY

The closure of Pak1-dependent macropinosomes requires the phosphorylation of CtBP1/BARS

(2008) Prisca Liberali et al.   EMBO JOURNAL

Subversion of CtBP1-controlled macropinocytosis by human adenovirus serotype 3

(2008) Beat Amstutz et al.   EMBO JOURNAL

p21-activated Kinase-aberrant Activation and Translocation in Alzheimer Disease Pathogenesis

(2008) Qiu-Lan Ma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting Large Kinase Active Site with Rigid, Bulky Octahedral Ruthenium Complexes

(2008) Jasna Maksimoska et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Pak4 Protein Kinase Plays a Key Role in Cell Survival and Tumorigenesis in Athymic Mice

(2008) Y. Liu et al.   MOLECULAR CANCER RESEARCH

Regulation of hippocampal long-term potentiation by p21-activated protein kinase 1 (PAK1)

(2008) Suhail Asrar et al.   NEUROPHARMACOLOGY

Genomic alterations link Rho family of GTPases to the highly invasive phenotype of pancreas cancer

(2008) A. C. Kimmelman et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA