Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy

Discovery of antiproliferative and anti-FAK inhibitory activity of 1,2,4-triazole derivatives containing acetamido carboxylic acid skeleton

(2021) Muhamad Mustafa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, Synthesis, Biological Evaluation, and Molecular Docking of 2,4-Diaminopyrimidine Derivatives Targeting Focal Adhesion Kinase as Tumor Radiotracers

(2021) Yueheng Qi et al.   MOLECULAR PHARMACEUTICS

Benzopyrimidodiazepinone inhibitors of TNK2

(2020) Brian J. Groendyke et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bifunctional Pyrimidines as Modulators of Focal Adhesion Kinase

(2020) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Chemically Induced Degradation of FAK-ALK for Application in Cancer Therapeutics

(2020) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Design, synthesis, and biological evaluation of F-18-labelled 2, 4-diaminopyrimidine-type FAK-targeted inhibitors as potential tumour imaging agents

(2020) Yueheng Qi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK)

(2020) Yang Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor

(2020) Brian J. Groendyke et al.   ACS Medicinal Chemistry Letters

Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

(2019) Johannes Popow et al.   JOURNAL OF MEDICINAL CHEMISTRY

A phase Ib dose-finding, pharmacokinetic study of the focal adhesion kinase inhibitor GSK2256098 and trametinib in patients with advanced solid tumours

(2019) Gabriel Mak et al.   BRITISH JOURNAL OF CANCER

Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells

(2019) Luhong Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities

(2019) Yue Su et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK)

(2019) Xiaotian Kong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 1,2,4-triazine-based derivatives as novel neddylation inhibitors and anticancer activity studies against gastric cancer MGC-803 cells

(2019) Jian Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of diphenylpyrimidine derivatives (DPPYs) as potential dual EGFR T790M and FAK inhibitors against a diverse range of cancer cell lines

(2019) Min Ai et al.   BIOORGANIC CHEMISTRY

Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs

(2019) Hongying Gao et al.   ACS Medicinal Chemistry Letters

Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents

(2019) Ruifeng Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors

(2019) Ruifeng Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Phase 2 study of the focal adhesion kinase inhibitor defactinib (VS-6063) in previously treated advanced KRAS mutant non-small cell lung cancer

(2019) David E. Gerber et al.   LUNG CANCER

Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase

(2018) Expédite Yen-Pon et al.   ACS Chemical Biology

PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

(2018) Yonghui Sun et al.   CELL RESEARCH

Design, synthesis, in vitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors

(2018) Mehlika Dilek Altıntop et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Study of the Focal Adhesion Kinase Inhibitor GSK2256098 in Patients with Recurrent Glioblastoma with Evaluation of Tumor Penetration of [11C]GSK2256098

(2018) Nicholas F Brown et al.   NEURO-ONCOLOGY

VS-4718 Antagonizes Multidrug Resistance in ABCB1- and ABCG2-Overexpressing Cancer Cells by Inhibiting the Efflux Function of ABC Transporters

(2018) Ning Ji et al.   Frontiers in Pharmacology

Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers

(2017) Dong-Jun Fu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of formononetin-dithiocarbamate hybrids that inhibit growth and migration of PC-3 cells via MAPK/Wnt signaling pathways

(2017) Dong-Jun Fu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines

(2017) Dan Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia

(2017) He Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Reply to Letter to the Editor “Concern on article “Predicting procedure successful rate and 1-year patency after endovascular recanalization for chronic carotid artery occlusion by CT angiography””

(2017) Hon-Man Liu et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

Chemical Structure Characteristics and Bioactivity of Small Molecule FAK Inhibitors

(2016) Fang-Yuan Cao et al.   Anti-Cancer Agents in Medicinal Chemistry

Phosphonate-based irreversible inhibitors of human γ-glutamyl transpeptidase (GGT). GGsTop is a non-toxic and highly selective inhibitor with critical electrostatic interaction with an active-site residue Lys562 for enhanced inhibitory activity

(2016) Akane Kamiyama et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency

(2016) Julie Farand et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and antiproliferative activity studies of novel dithiocarbamate–chalcone derivates

(2016) Dong-Jun Fu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A first-in-Asian phase 1 study to evaluate safety, pharmacokinetics and clinical activity of VS-6063, a focal adhesion kinase (FAK) inhibitor in Japanese patients with advanced solid tumors

(2016) Toshio Shimizu et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK)

(2016) Gregory R. Ott et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

(2016) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program

(2016) Raushan T. Kurmasheva et al.   PEDIATRIC BLOOD & CANCER

Discovery of Novel Bruton’s Tyrosine Kinase (BTK) Inhibitors Bearing a N,9-Diphenyl-9H-purin-2-amine Scaffold

(2016) Yang Ge et al.   ACS Medicinal Chemistry Letters

Designed to Kill: Novel Menin-MLL Inhibitors Target MLL -Rearranged Leukemia

(2015) Michael W.M. Kühn et al.   CANCER CELL

Evaluating reaction pathways of hydrothermal abiotic organic synthesis at elevated temperatures and pressures using carbon isotopes

(2015) Qi Fu et al.   GEOCHIMICA ET COSMOCHIMICA ACTA

Targeting FAK scaffold functions inhibits human renal cell carcinoma growth

(2015) Claire Béraud et al.   INTERNATIONAL JOURNAL OF CANCER

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

FAK signaling in human cancer as a target for therapeutics

(2015) Brian Y. Lee et al.   PHARMACOLOGY & THERAPEUTICS

Emerging Roles of Focal Adhesion Kinase in Cancer

(2015) Yu-Ling Tai et al.   Biomed Research International

Advances in molecular-based personalized non-small-cell lung cancer therapy: targeting epidermal growth factor receptor and mechanisms of resistance

(2015) Robert M. Jotte et al.   Cancer Medicine

Synthesis, biological evaluation, and molecular docking studies of novel 2-styryl-5-nitroimidazole derivatives containing 1,4-benzodioxan moiety as FAK inhibitors with anticancer activity

(2014) Yong-Tao Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

PND-1186 FAK inhibitor selectively promotes tumore cell apoptosis in three-dimensional environments

(2014) Michael D. Schaller et al.   CANCER BIOLOGY & THERAPY

Focal adhesion kinase

(2014) Rebecca L Stone et al.   CANCER BIOLOGY & THERAPY

A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells

(2014) Jianliang Zhang et al.   CELL CYCLE

Focal adhesion kinase inhibitors in the treatment of metastatic cancer: a patent review

(2014) Ekambaram Shanthi et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Design, Synthesis, and Evaluation of Novel Imidazo[1,2-a][1,3,5]triazines and Their Derivatives as Focal Adhesion Kinase Inhibitors with Antitumor Activity

(2014) Pascal Dao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent Inhibitory Activities against Both Wild-type and Mutant ALK Kinases

(2014) Zilan Song et al.   JOURNAL OF MEDICINAL CHEMISTRY

A New Challenging and Promising Era of Tyrosine Kinase Inhibitors

(2014) J. Jean Cui   ACS Medicinal Chemistry Letters

Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity

(2013) Pascal Dao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-based discovery of cellular-active allosteric inhibitors of FAK

(2013) Naoki Tomita et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

High-Throughput Tyrosine Kinase Activity Profiling Identifies FAK as a Candidate Therapeutic Target in Ewing Sarcoma

(2013) B. D. Crompton et al.   CANCER RESEARCH

Role of Focal Adhesion Kinase in Regulating YB–1–Mediated Paclitaxel Resistance in Ovarian Cancer

(2013) Yu Kang et al.   JNCI-Journal of the National Cancer Institute

Irreversible kinase inhibitors gain traction

(2013) Katharine Sanderson   NATURE REVIEWS DRUG DISCOVERY

Clinical Importance and Potential Use of Small Molecule Inhibitors of Focal Adhesion Kinase

(2012) Alexander Schultze et al.   Anti-Cancer Agents in Medicinal Chemistry

Synthesis, biological evaluation, and molecular docking studies of 1,3,4-thiadiazol-2-amide derivatives as novel anticancer agents

(2012) Xian-Hui Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

2-Anilino-4-(benzimidazol-2-yl)pyrimidines – A multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines

(2012) Renate Determann et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Focal Adhesion Kinase Inhibitors Using a Hybrid Protocol of Virtual Screening Approach Based on Multicomplex-Based Pharmacophore and Molecular Docking

(2012) Fengbo Wu et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

FAK promotes recruitment of talin to nascent adhesions to control cell motility

(2012) Christine Lawson et al.   JOURNAL OF CELL BIOLOGY

Safety, Pharmacokinetic, and Pharmacodynamic Phase I Dose-Escalation Trial of PF-00562271, an Inhibitor of Focal Adhesion Kinase, in Advanced Solid Tumors

(2012) Jeffrey R. Infante et al.   JOURNAL OF CLINICAL ONCOLOGY

Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

(2012) Tjeerd Barf et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein tyrosine kinase 6 protects cells from anoikis by directly phosphorylating focal adhesion kinase and activating AKT

(2012) Y Zheng et al.   ONCOGENE

In oral squamous cell carcinoma, high FAK expression is correlated with low P53 expression

(2012) Pablo Rosado et al.   VIRCHOWS ARCHIV

Synthesis, biological evaluation and molecular docking studies of 1,3,4-thiadiazole derivatives containing 1,4-benzodioxan as potential antitumor agents

(2011) Juan Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases

(2011) Craig A. Zificsak et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Prodrugs - An Efficient Way to Breach Delivery and Targeting Barriers

(2011) Kristiina M. Huttunen et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Focal adhesion kinase and tumour angiogenesis

(2011) Tanguy Lechertier et al.   JOURNAL OF PATHOLOGY

Inhibition of Focal Adhesion Kinase by PF-562,271 Inhibits the Growth and Metastasis of Pancreatic Cancer Concomitant with Altering the Tumor Microenvironment

(2011) J. B. Stokes et al.   MOLECULAR CANCER THERAPEUTICS

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Tuning protein autoinhibition by domain destabilization

(2011) Jae-Hyun Cho et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Crystal Structures of Anaplastic Lymphoma Kinase in Complex with ATP Competitive Inhibitors

(2010) Roberto T. Bossi et al.   BIOCHEMISTRY

Sunitinib and PF-562,271 (FAK/Pyk2 inhibitor) effectively block growth and recovery of human hepatocellular carcinoma in a rat xenograft model

(2010) Cedo M Bagi et al.   CANCER BIOLOGY & THERAPY

PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments

(2010) Isabelle Tanjoni et al.   CANCER BIOLOGY & THERAPY

Therapeutic potential and limitations of new FAK inhibitors in the treatment of cancer

(2010) Alexander Schultze et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Chemical Inducers of Targeted Protein Degradation

(2010) Kanak Raina et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cellular functions of FAK kinases: insight into molecular mechanisms and novel functions

(2010) M. D. Schaller   JOURNAL OF CELL SCIENCE

The FERM domain: organizing the structure and function of FAK

(2010) Margaret C. Frame et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Discovery of a Potent Inhibitor of Anaplastic Lymphoma Kinase with in Vivo Antitumor Activity

(2010) Gregory R. Ott et al.   ACS Medicinal Chemistry Letters

Synthesis and SAR of sulfonyl- and phosphoryl amidine compounds as anti-resorptive agents

(2009) Myung Yun Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Signal transduction by focal adhesion kinase in cancer

(2009) Jihe Zhao et al.   CANCER AND METASTASIS REVIEWS

ABC Efflux Pump-Based Resistance to Chemotherapy Drugs

(2009) Paul D. W. Eckford et al.   CHEMICAL REVIEWS

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

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

Progress in researches about focal adhesion kinase ingastrointestinal tract

(2009) Hui Fang Hao et al.   WORLD JOURNAL OF GASTROENTEROLOGY

Transport proteins of the ABC family and multidrug resistance of tumor cells

(2008) A. A. Stavrovskaya et al.   BIOCHEMISTRY-MOSCOW

Antitumor Activity and Pharmacology of a Selective Focal Adhesion Kinase Inhibitor, PF-562,271

(2008) W. G. Roberts et al.   CANCER RESEARCH

Synthesis of some new 1,3,4-thiadiazol-2-ylmethyl-1,2,4-triazole derivatives and investigation of their antimicrobial activities

(2008) Ahmet Demirbas et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Nuclear FAK Promotes Cell Proliferation and Survival through FERM-Enhanced p53 Degradation

(2008) Ssang-Taek Lim et al.   MOLECULAR CELL

Crystal Structures of the FAK Kinase in Complex with TAE226 and Related Bis-Anilino Pyrimidine Inhibitors Reveal a Helical DFG Conformation

(2008) Daniel Lietha et al.   PLoS One