Literature DB >> 27590157

Delivery of the Porcupine Inhibitor WNT974 in Mice.

Li-Shu Zhang1, Lawrence Lum1.   

Abstract

We describe here a technique for delivering the porcupine inhibitor WNT974 (formerly LGK974) in mice. The protocol entails once-a-day oral delivery of WNT974 for up to 3 months at a concentration sufficient to achieve systemic Wnt pathway inhibition with limited toxicity as measured by weight change. This route of delivery enables extended durations of Wnt signaling inhibition in a mammalian model organism.

Entities:  

Keywords:  Drug delivery; Mice; Porcupine; Wnt974/LGK974

Mesh：

Substances：

Year:  2016        PMID： 27590157      PMCID： PMC5024565          DOI： 10.1007/978-1-4939-6393-5_12

Source DB:  PubMed          Journal:  Methods Mol Biol        ISSN： 1064-3745


  11 in total

Review 1.  Wnt/β-catenin signaling and disease.

Authors:  Hans Clevers; Roel Nusse
Journal:  Cell       Date:  2012-06-08       Impact factor: 41.582

Review 2.  Chemical Disruption of Wnt-dependent Cell Fate Decision-making Mechanisms in Cancer and Regenerative Medicine.

Authors:  L Lum; C Chen
Journal:  Curr Med Chem       Date:  2015       Impact factor: 4.530

3.  Diverse chemical scaffolds support direct inhibition of the membrane-bound O-acyltransferase porcupine.

Authors:  Michael E Dodge; Jesung Moon; Rubina Tuladhar; Jianming Lu; Leni S Jacob; Li-shu Zhang; Heping Shi; Xiaolei Wang; Enrico Moro; Alessandro Mongera; Francesco Argenton; Courtney M Karner; Thomas J Carroll; Chuo Chen; James F Amatruda; Lawrence Lum
Journal:  J Biol Chem       Date:  2012-05-15       Impact factor: 5.157

4.  Tankyrase Inhibition Causes Reversible Intestinal Toxicity in Mice with a Therapeutic Index < 1.

Authors:  Yu Zhong; Paula Katavolos; Trung Nguyen; Ted Lau; Jason Boggs; Amy Sambrone; David Kan; Mark Merchant; Eric Harstad; Dolores Diaz; Mike Costa; Melissa Schutten
Journal:  Toxicol Pathol       Date:  2015-12-20       Impact factor: 1.902

5.  Porcupine inhibitor suppresses paracrine Wnt-driven growth of Rnf43;Znrf3-mutant neoplasia.

Authors:  Bon-Kyoung Koo; Johan H van Es; Maaike van den Born; Hans Clevers
Journal:  Proc Natl Acad Sci U S A       Date:  2015-05-28       Impact factor: 11.205

6.  Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma.

Authors:  Xiaomo Jiang; Huai-Xiang Hao; Joseph D Growney; Steve Woolfenden; Cindy Bottiglio; Nicholas Ng; Bo Lu; Mindy H Hsieh; Linda Bagdasarian; Ronald Meyer; Timothy R Smith; Monika Avello; Olga Charlat; Yang Xie; Jeffery A Porter; Shifeng Pan; Jun Liu; Margaret E McLaughlin; Feng Cong
Journal:  Proc Natl Acad Sci U S A       Date:  2013-07-11       Impact factor: 11.205

7.  Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer.

Authors:  Kyle David Proffitt; Babita Madan; Zhiyuan Ke; Vishal Pendharkar; Lijun Ding; May Ann Lee; Rami N Hannoush; David M Virshup
Journal:  Cancer Res       Date:  2012-11-27       Impact factor: 12.701

8.  Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974.

Authors:  Jun Liu; Shifeng Pan; Mindy H Hsieh; Nicholas Ng; Fangxian Sun; Tao Wang; Shailaja Kasibhatla; Alwin G Schuller; Allen G Li; Dai Cheng; Jie Li; Celin Tompkins; AnneMarie Pferdekamper; Auzon Steffy; Jane Cheng; Colleen Kowal; Van Phung; Guirong Guo; Yan Wang; Martin P Graham; Shannon Flynn; J Chad Brenner; Chun Li; M Cristina Villarroel; Peter G Schultz; Xu Wu; Peter McNamara; William R Sellers; Lilli Petruzzelli; Anthony L Boral; H Martin Seidel; Margaret E McLaughlin; Jianwei Che; Thomas E Carey; Gary Vanasse; Jennifer L Harris
Journal:  Proc Natl Acad Sci U S A       Date:  2013-11-25       Impact factor: 11.205

9.  WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited.

Authors:  Luke Boulter; Rachel V Guest; Timothy J Kendall; David H Wilson; Davina Wojtacha; Andrew J Robson; Rachel A Ridgway; Kay Samuel; Nico Van Rooijen; Simon T Barry; Stephen J Wigmore; Owen J Sansom; Stuart J Forbes
Journal:  J Clin Invest       Date:  2015-02-17       Impact factor: 14.808

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

Authors:  Baozhi Chen; Michael E Dodge; Wei Tang; Jianming Lu; Zhiqiang Ma; Chih-Wei Fan; Shuguang Wei; Wayne Hao; Jessica Kilgore; Noelle S Williams; Michael G Roth; James F Amatruda; Chuo Chen; Lawrence Lum
Journal:  Nat Chem Biol       Date:  2009-01-04       Impact factor: 15.040
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  5 in total

1.  Potent in vivo lung cancer Wnt signaling inhibition via cyclodextrin-LGK974 inclusion complexes.

Authors:  Pedro P G Guimaraes; Mingchee Tan; Tuomas Tammela; Katherine Wu; Amanda Chung; Matthias Oberli; Karin Wang; Roman Spektor; Rachel S Riley; Celso T R Viana; Tyler Jacks; Robert Langer; Michael J Mitchell
Journal:  J Control Release       Date:  2018-10-02       Impact factor: 9.776

2.  Blockade to pathological remodeling of infarcted heart tissue using a porcupine antagonist.

Authors:  Jesung Moon; Huanyu Zhou; Li-Shu Zhang; Wei Tan; Ying Liu; Shanrong Zhang; Lorraine K Morlock; Xiaoping Bao; Sean P Palecek; Jian Q Feng; Noelle S Williams; James F Amatruda; Eric N Olson; Rhonda Bassel-Duby; Lawrence Lum
Journal:  Proc Natl Acad Sci U S A       Date:  2017-01-31       Impact factor: 11.205

Review 3.  Recent advances on the progressive mechanism and therapy in castration-resistant prostate cancer.

Authors:  Keshan Wang; Hailong Ruan; Tianbo Xu; Lei Liu; Di Liu; Hongmei Yang; Xiaoping Zhang; Ke Chen
Journal:  Onco Targets Ther       Date:  2018-05-28       Impact factor: 4.147

4.  Loss of endothelial glucocorticoid receptor accelerates diabetic nephropathy.

Authors:  Swayam Prakash Srivastava; Han Zhou; Ocean Setia; Bing Liu; Keizo Kanasaki; Daisuke Koya; Alan Dardik; Carlos Fernandez-Hernando; Julie Goodwin
Journal:  Nat Commun       Date:  2021-04-22       Impact factor: 14.919

5.  A Dominant Heterozygous Mutation in COG4 Causes Saul-Wilson Syndrome, a Primordial Dwarfism, and Disrupts Zebrafish Development via Wnt Signaling.

Authors:  Zhi-Jie Xia; Xin-Xin I Zeng; Mitali Tambe; Bobby G Ng; P Duc S Dong; Hudson H Freeze
Journal:  Front Cell Dev Biol       Date:  2021-09-14
  5 in total

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