Literature DB >> 26897593

Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase.

James E Tarver1, Praveen K Pabba2, Joseph Barbosa2, Qiang Han2, Michael W Gardyan2, Robert Brommage3, Andrea Y Thompson3, James M Schmidt3, Alan G E Wilson3, Wei He2, Victoria K Lombardo2, Kenneth G Carson2.   

Abstract

A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Femur cortical bone thickness; Notum Pectinacetylesterase; Osteoporosis; SAR; Thienopyrimidine

Mesh：

Substances：

Year:  2016        PMID： 26897593     DOI： 10.1016/j.bmcl.2016.02.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  16 in total

1.  Notum attenuates Wnt/β-catenin signaling to promote tracheal cartilage patterning.

Authors:  Bradley Gerhardt; Lauren Leesman; Kaulini Burra; John Snowball; Rachel Rosenzweig; Natalie Guzman; Manoj Ambalavanan; Debora Sinner
Journal:  Dev Biol       Date:  2018-02-09       Impact factor: 3.582

2.  Structural Analysis and Development of Notum Fragment Screening Hits.

Authors:  Yuguang Zhao; William Mahy; Nicky J Willis; Hannah L Woodward; David Steadman; Elliott D Bayle; Benjamin N Atkinson; James Sipthorp; Luca Vecchia; Reinis R Ruza; Karl Harlos; Fiona Jeganathan; Stefan Constantinou; Artur Costa; Svend Kjær; Magda Bictash; Patricia C Salinas; Paul Whiting; Jean-Paul Vincent; Paul V Fish; E Yvonne Jones
Journal:  ACS Chem Neurosci       Date:  2022-06-22       Impact factor: 5.780

3.  Notum Deletion From Late-Stage Skeletal Cells Increases Cortical Bone Formation and Potentiates Skeletal Effects of Sclerostin Inhibition.

Authors:  Roy B Choi; Whitney A Bullock; April M Hoggatt; Daniel J Horan; Emily Z Pemberton; Jung Min Hong; Xinjun Zhang; Xi He; Alexander G Robling
Journal:  J Bone Miner Res       Date:  2021-07-23       Impact factor: 6.741

4.  Small-molecule inhibitors of carboxylesterase Notum.

Authors:  Yuguang Zhao; Sarah Jolly; Stefano Benvegnu; E Yvonne Jones; Paul V Fish
Journal:  Future Med Chem       Date:  2021-04-22       Impact factor: 3.808

5.  NOTUM inhibition increases endocortical bone formation and bone strength.

Authors:  Robert Brommage; Jeff Liu; Peter Vogel; Faika Mseeh; Andrea Y Thompson; David G Potter; Melanie K Shadoan; Gwenn M Hansen; Sabrina Jeter-Jones; Jie Cui; Dawn Bright; Jennifer P Bardenhagen; Deon D Doree; Sofia Movérare-Skrtic; Karin H Nilsson; Petra Henning; Ulf H Lerner; Claes Ohlsson; Arthur T Sands; James E Tarver; David R Powell; Brian Zambrowicz; Qingyun Liu
Journal:  Bone Res       Date:  2019-01-08       Impact factor: 13.567

6.  Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen.

Authors:  Benjamin N Atkinson; David Steadman; Yuguang Zhao; James Sipthorp; Luca Vecchia; Reinis R Ruza; Fiona Jeganathan; Georgie Lines; Sarah Frew; Amy Monaghan; Svend Kjær; Magda Bictash; E Yvonne Jones; Paul V Fish
Journal:  Medchemcomm       Date:  2019-04-29       Impact factor: 3.597

7.  Structural characterization of melatonin as an inhibitor of the Wnt deacylase Notum.

Authors:  Yuguang Zhao; Jingshan Ren; James Hillier; Margaret Jones; Weixian Lu; Edith Yvonne Jones
Journal:  J Pineal Res       Date:  2020-01-24       Impact factor: 13.007

8.  Osteoblast-derived NOTUM reduces cortical bone mass in mice and the NOTUM locus is associated with bone mineral density in humans.

Authors:  Sofia Movérare-Skrtic; Karin H Nilsson; Petra Henning; Thomas Funck-Brentano; Maria Nethander; Fernando Rivadeneira; Glaucia Coletto Nunes; Antti Koskela; Juha Tuukkanen; Jan Tuckermann; Christine Perret; Pedro Paulo Chaves Souza; Ulf H Lerner; Claes Ohlsson
Journal:  FASEB J       Date:  2019-07-15       Impact factor: 5.191

9.  An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent.

Authors:  Nicky J Willis; Elliott D Bayle; George Papageorgiou; David Steadman; Benjamin N Atkinson; William Mahy; Paul V Fish
Journal:  Beilstein J Org Chem       Date:  2019-11-19       Impact factor: 2.883

10.  Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling.

Authors:  Radu M Suciu; Armand B Cognetta; Zachary E Potter; Benjamin F Cravatt
Journal:  ACS Med Chem Lett       Date:  2018-05-26       Impact factor: 4.345
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