Discovery of Novel Inhibitor for WNT/β-Catenin Pathway by Tankyrase 1/2 Structure-Based Virtual Screening

A novel tankyrase inhibitor, MSC2504877, enhances the effects of clinical CDK4/6 inhibitors

(2019) Malini Menon et al.   Scientific Reports

Identification by Inverse Virtual Screening of magnolol-based scaffold as new tankyrase-2 inhibitors

(2018) Simone Di Micco et al.   BIOORGANIC & MEDICINAL CHEMISTRY

IWR-1, a tankyrase inhibitor, attenuates Wnt/β-catenin signaling in cancer stem-like cells and inhibits in vivo the growth of a subcutaneous human osteosarcoma xenograft

(2018) Sara R. Martins-Neves et al.   CANCER LETTERS

Targeting the Wnt/beta-catenin pathway in cancer: Update on effectors and inhibitors

(2018) Nithya Krishnamurthy et al.   CANCER TREATMENT REVIEWS

Multiple grid arrangement improves ligand docking with unknown binding sites: Application to the inverse docking problem

(2018) Tomohiro Ban et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays

(2018) Wenfeng Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors

(2018) Yves Nkizinkiko et al.   Scientific Reports

In silico insights on Tankyrase protein: a potential target for colorectal cancer

(2018) Loganathan Lakshmanan et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques

(2018) Giosuè Costa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of tankyrase by a novel small molecule significantly attenuates prostate cancer cell proliferation

(2018) Honglin Cheng et al.   CANCER LETTERS

Discovery of novel CDK8 inhibitors using multiple crystal structures in docking-based virtual screening

(2017) Taijin Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors

(2017) Martina Ferri et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines

(2017) Douglas W. Thomson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

(2017) Upendra Rao Anumala et al.   JOURNAL OF MEDICINAL CHEMISTRY

APC Mutations as a Potential Biomarker for Sensitivity to Tankyrase Inhibitors in Colorectal Cancer

(2017) Noritaka Tanaka et al.   MOLECULAR CANCER THERAPEUTICS

Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors

(2016) Ann-Gerd Thorsell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Wnt signaling in colorectal cancer. A Review in the Theme: Cell Signaling: Proteins, Pathways and Mechanisms

(2015) Laura Novellasdemunt et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics

(2015) Yves Nkizinkiko et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases

(2015) Katerina Kumpan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tankyrases: Structure, Function and Therapeutic Implications in Cancer

(2014) Teemu Haikarainen et al.   CURRENT PHARMACEUTICAL DESIGN

Sighting of tankyrase inhibitors by structure- and ligand-based screening and in vitro approach

(2014) Palani Kirubakaran et al.   Molecular BioSystems

A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation-Driven Colorectal Tumor Growth

(2013) T. Lau et al.   CANCER RESEARCH

Discovery of Novel, Induced-Pocket Binding Oxazolidinones as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors

(2013) Howard Bregman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Screening and Structural Analysis of Flavones Inhibiting Tankyrases

(2013) Mohit Narwal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases

(2013) Amit Nathubhai et al.   ACS Medicinal Chemistry Letters

A Novel Tankyrase Inhibitor Decreases Canonical Wnt Signaling in Colon Carcinoma Cells and Reduces Tumor Growth in Conditional APC Mutant Mice

(2012) J. Waaler et al.   CANCER RESEARCH

ZINC: A Free Tool to Discover Chemistry for Biology

(2012) John J. Irwin et al.   Journal of Chemical Information and Modeling

Docking performance of the glide program as evaluated on the Astex and DUD datasets: a complete set of glide SP results and selected results for a new scoring function integrating WaterMap and glide

(2012) Matthew P. Repasky et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Structural Basis of Selective Inhibition of Human Tankyrases

(2012) Mohit Narwal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tankyrase-targeted therapeutics: expanding opportunities in the PARP family

(2012) Jenna L. Riffell et al.   NATURE REVIEWS DRUG DISCOVERY

Novel Binding Mode of a Potent and Selective Tankyrase Inhibitor

(2012) Hakan Gunaydin et al.   PLoS One

WIKI4, a Novel Inhibitor of Tankyrase and Wnt/ß-Catenin Signaling

(2012) Richard G. James et al.   PLoS One

Novel Synthetic Antagonists of Canonical Wnt Signaling Inhibit Colorectal Cancer Cell Growth

(2011) J. Waaler et al.   CANCER RESEARCH

A diterpenoid derivative 15-oxospiramilactone inhibits Wnt/β-catenin signaling and colon cancer cell tumorigenesis

(2011) Wei Wang et al.   CELL RESEARCH

FluorinatedN,N-Dialkylaminostilbenes for Wnt Pathway Inhibition and Colon Cancer Repression

(2011) Wen Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

AV-65, a novel Wnt/β-catenin signal inhibitor, successfully suppresses progression of multiple myeloma in a mouse model

(2011) H Yao et al.   Blood Cancer Journal

The Wnt signaling pathway in cellular proliferation and differentiation: A tale of two coactivators

(2010) Jia-Ling Teo et al.   ADVANCED DRUG DELIVERY REVIEWS

Structural Basis for the Interaction between Tankyrase-2 and a Potent Wnt-Signaling Inhibitor

(2010) Tobias Karlberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

(2009) Shih-Min A. Huang et al.   NATURE

Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

(2009) Baozhi Chen et al.   Nature Chemical Biology

Zinc Binding Catalytic Domain of Human Tankyrase 1

(2008) Lari Lehtiö et al.   JOURNAL OF MOLECULAR BIOLOGY