Development of a Fragment-Based Screening Assay for the Focal Adhesion Targeting Domain Using SPR and NMR

Phase I Study of BI 853520, an Inhibitor of Focal Adhesion Kinase, in Patients with Advanced or Metastatic Nonhematologic Malignancies

(2019) Maja J. A. de Jonge et al.   Targeted Oncology

Development of a High-Throughput Fluorescence Polarization Assay to Detect Inhibitors of the FAK–Paxillin Interaction

(2019) Timothy Marlowe et al.   SLAS Discovery

When fragments link: a bibliometric perspective on the development of fragment-based drug discovery

(2018) Angelo K.S. Romasanta et al.   DRUG DISCOVERY TODAY

Current perspectives in fragment-based lead discovery (FBLD)

(2017) Bas Lamoree et al.   Essays in Biochemistry

Oncogenic Receptor Tyrosine Kinases Directly Phosphorylate Focal Adhesion Kinase (FAK) as a Resistance Mechanism to FAK-Kinase Inhibitors

(2016) Timothy A. Marlowe et al.   MOLECULAR CANCER THERAPEUTICS

Twenty years on: the impact of fragments on drug discovery

(2016) Daniel A. Erlanson et al.   NATURE REVIEWS DRUG DISCOVERY

FAK and paxillin, two potential targets in pancreatic cancer

(2016) Rajani Kanteti et al.   Oncotarget

A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors

(2015) Suzanne F. Jones et al.   INVESTIGATIONAL NEW DRUGS

Altering FAK-Paxillin Interactions Reduces Adhesion, Migration and Invasion Processes

(2014) Thérèse B. Deramaudt et al.   PLoS One

The 'rule of three' for fragment-based drug discovery: where are we now?

(2013) Harren Jhoti et al.   NATURE REVIEWS DRUG DISCOVERY

Disrupting the Scaffold to Improve Focal Adhesion Kinase-Targeted Cancer Therapeutics

(2013) W. G. Cance et al.   Science Signaling

Function of Focal Adhesion Kinase Scaffolding to Mediate Endophilin A2 Phosphorylation Promotes Epithelial-Mesenchymal Transition and Mammary Cancer Stem Cell Activitiesin Vivo

(2012) Huaping Fan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Fragment Screening by Surface Plasmon Resonance

(2010) Iva Navratilova et al.   ACS Medicinal Chemistry Letters

Ras- and PI3K-dependent breast tumorigenesis in mice and humans requires focal adhesion kinase signaling

(2009) Yuliya Pylayeva et al.   JOURNAL OF CLINICAL INVESTIGATION

The rise of fragment-based drug discovery

(2009) Christopher W. Murray et al.   Nature Chemistry

Mammary Epithelial-Specific Disruption of Focal Adhesion Kinase Retards Tumor Formation and Metastasis in a Transgenic Mouse Model of Human Breast Cancer

(2008) Paolo P. Provenzano et al.   AMERICAN JOURNAL OF PATHOLOGY

Mutation of Y925F in focal adhesion kinase (FAK) suppresses melanoma cell proliferation and metastasis

(2008) Tomonori Kaneda et al.   CANCER LETTERS

Ligand efficiency and fragment-based drug discovery

(2008) Scott D. Bembenek et al.   DRUG DISCOVERY TODAY