Literature DB >> 21855335

Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.

Hongbo Zeng1, David B Belanger, Patrick J Curran, Gerald W Shipps, Hua Miao, Jack B Bracken, M Arshad Siddiqui, Michael Malkowski, Yan Wang.   

Abstract

A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selectivity towards other kinases and desirable DMPK properties were achieved to enable the exploration of Brk as an oncology target.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21855335     DOI： 10.1016/j.bmcl.2011.07.101

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


  11 in total

Review 1.  Evolution of breast cancer therapeutics: Breast tumour kinase's role in breast cancer and hope for breast tumour kinase targeted therapy.

Authors:  Haroon A Hussain; Amanda J Harvey
Journal:  World J Clin Oncol       Date:  2014-08-10

2.  Enantioselective Synthesis of Pyrrolopyrimidine Scaffolds through Cation-Directed Nucleophilic Aromatic Substitution.

Authors:  Mariel M Cardenas; Sean T Toenjes; Christopher J Nalbandian; Jeffrey L Gustafson
Journal:  Org Lett       Date:  2018-03-21       Impact factor: 6.005

3.  The associated pyrazolopyrimidines PP1 and PP2 inhibit protein tyrosine kinase 6 activity and suppress breast cancer cell proliferation.

Authors:  Hyun Jae Shim; Han Ie Kim; Seung-Taek Lee
Journal:  Oncol Lett       Date:  2017-01-02       Impact factor: 2.967

Review 4.  Targeting protein tyrosine kinase 6 in cancer.

Authors:  Milica B Gilic; Angela L Tyner
Journal:  Biochim Biophys Acta Rev Cancer       Date:  2020-09-18       Impact factor: 10.680

Review 5.  Context-specific protein tyrosine kinase 6 (PTK6) signalling in prostate cancer.

Authors:  Yu Zheng; Angela L Tyner
Journal:  Eur J Clin Invest       Date:  2013-02-10       Impact factor: 4.686

6.  Additive impact of HER2-/PTK6-RNAi on interactions with HER3 or IGF-1R leads to reduced breast cancer progression in vivo.

Authors:  Natalie Falkenberg; Nataša Anastasov; Ines Höfig; Ksenia Bashkueva; Katrin Lindner; Heinz Höfler; Michael Rosemann; Michaela Aubele
Journal:  Mol Oncol       Date:  2014-09-06       Impact factor: 6.603

7.  Loss-of-function RNAi screens in breast cancer cells identify AURKB, PLK1, PIK3R1, MAPK12, PRKD2, and PTK6 as sensitizing targets of rapamycin activity.

Authors:  Oliver Ou; Konrad Huppi; Sirisha Chakka; Kristen Gehlhaus; Wendy Dubois; Jyoti Patel; Jinqiu Chen; Mark Mackiewicz; Tamara L Jones; Jason J Pitt; Scott E Martin; Paul Goldsmith; John K Simmons; Beverly A Mock; Natasha J Caplen
Journal:  Cancer Lett       Date:  2014-09-01       Impact factor: 8.679

8.  PTK6 inhibition promotes apoptosis of Lapatinib-resistant Her2(+) breast cancer cells by inducing Bim.

Authors:  Sun Hee Park; Koichi Ito; William Olcott; Igor Katsyv; Gwyneth Halstead-Nussloch; Hanna Y Irie
Journal:  Breast Cancer Res       Date:  2015-06-19       Impact factor: 6.466

9.  Small molecule inhibitors reveal PTK6 kinase is not an oncogenic driver in breast cancers.

Authors:  Luping Qiu; Kymberly Levine; Ketan S Gajiwala; Ciarán N Cronin; Asako Nagata; Eric Johnson; Michelle Kraus; John Tatlock; Robert Kania; Timothy Foley; Shaoxian Sun
Journal:  PLoS One       Date:  2018-06-07       Impact factor: 3.240

10.  Expression of protein tyrosine kinase 6 (PTK6) in nonsmall cell lung cancer and their clinical and prognostic significance.

Authors:  Chao Zhao; Yan Chen; Weiwei Zhang; Jianrong Zhang; Yulian Xu; Wenjie Li; Sunxiao Chen; Anmei Deng
Journal:  Onco Targets Ther       Date:  2013-03-08       Impact factor: 4.147
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