PMID

Data

Article Title

Organization

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.

University of Bath

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

Health & Science University

Recent Advances in Scaffold Hopping.

Rheinische Friedrich-Wilhelms-Universit£T

Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.

University of Bath

Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.

Therachem Research Medilab (India)

Development and structural analysis of adenosine site binding tankyrase inhibitors.

University of Oulu

Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.

University of Oulu

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

University of Bath

Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.

Philochem

Structure-activity relationship and properties optimization of a series of quinazoline-2,4-diones as inhibitors of the canonical Wnt pathway.

Siena Biotech

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.

The Institute of Cancer Research

Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors.

Universit£

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

University of Bath

Screening and structural analysis of flavones inhibiting tankyrases.

University of Oulu

Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor.

Oslo University Hospital

Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.

Amgen

Structural basis of selective inhibition of human tankyrases.

Abo Akademi University

[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.

Novartis Institutes For Biomedical Research

Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.

Karolinska Institutet

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-

Astrazeneca

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.

West China Hospital

Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.

Hubei Polytechnic University

Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules.

University of Perugia

Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.

Nanjing University

Potent 2,3-dihydrophthalazine-1,4-dione derivatives as dual inhibitors for mono-ADP-ribosyltransferases PARP10 and PARP15.

University of Perugia

Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.

University of South Australia

Analogs of TIQ-A as inhibitors of human mono-ADP-ribosylating PARPs.

University of Oulu

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II.

Symeres

Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors.

Glaxosmithkline

Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.

TBA

Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.

Lupin

Novel 4-Heteroarylcarbonyl-N-(phenyl or heteroaryl) Piperidine-1-carboxamides as Tankyrase Inhibitors.

Lauren Mccallister

Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.

University of Oslo

From PARP1 to TNKS2 Inhibition: A Structure-Based Approach.

University of Naples

Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.

Nirma University

Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors.

Riken

Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.

Japanese Foundation For Cancer Research

Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.

Merck Healthcare

Rational Design of Cell-Active Inhibitors of PARP10.

Oregon Health and Science University

Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.

Astrazeneca

Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.

Hoffmann-La Roche

Scaffold hopping approach on the route to selective tankyrase inhibitors.

University of Perugia

Tankyrase inhibitors: potential treatment of hyperproliferative diseases.

Therachem Research Medilab (India)

Design and Synthesis of Poly(ADP-ribose) Polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-Oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity.

St. John'S University

4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.

University of Oulu

Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.

Universitaire Vaudois

Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors.

University of Perugia

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

University of Salerno

Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.

University of Pennsylvania

Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.

Mcdaniel College

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

Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)

Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.

Stony Brook University

4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.

Kudos Pharmaceuticals

Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.

Boehringer Ingelheim Pharmaceuticals

Design and synthesis of novel 5,6-disubstituted uracil derivatives as potent inhibitors of thymidine phosphorylase.

Academy of Sciences of The Czech Republic