Literature DB >> 18474425

IRAK-4 inhibitors. Part 1: a series of amides.

George M Buckley1, Lewis Gowers, Alicia Perez Higueruelo, Kerry Jenkins, Stephen R Mack, Trevor Morgan, David M Parry, William R Pitt, Oliver Rausch, Marianna D Richard, Verity Sabin, Joanne L Fraser.   

Abstract

The synthesis and profile of a series of amides are described. Some of these compounds were potent IRAK-4 inhibitors and two examples were evaluated in vivo.

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Year:  2008        PMID： 18474425     DOI： 10.1016/j.bmcl.2008.04.058

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


  10 in total

1.  Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4).

Authors:  Li Wang; Ryan Ferrao; Qiubai Li; John M Hatcher; Hwan Geun Choi; Sara J Buhrlage; Nathanael S Gray; Hao Wu
Journal:  J Biol Chem       Date:  2019-01-24       Impact factor: 5.157

2.  Crystal structure of human IRAK1.

Authors:  Li Wang; Qi Qiao; Ryan Ferrao; Chen Shen; John M Hatcher; Sara J Buhrlage; Nathanael S Gray; Hao Wu
Journal:  Proc Natl Acad Sci U S A       Date:  2017-12-05       Impact factor: 11.205

3.  Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.

Authors:  Jongwon Lim; Michael D Altman; James Baker; Jason D Brubaker; Hongmin Chen; Yiping Chen; Thierry Fischmann; Craig Gibeau; Melanie A Kleinschek; Erica Leccese; Charles Lesburg; John K F Maclean; Lily Y Moy; Erin F Mulrooney; Jeremy Presland; Larissa Rakhilina; Graham F Smith; Dietrich Steinhuebel; Ruojing Yang
Journal:  ACS Med Chem Lett       Date:  2015-04-20       Impact factor: 4.345

4.  A highly selective inhibitor of interleukin-1 receptor-associated kinases 1/4 (IRAK-1/4) delineates the distinct signaling roles of IRAK-1/4 and the TAK1 kinase.

Authors:  Scott A Scarneo; Philip F Hughes; Kelly W Yang; David A Carlson; Deepak Gurbani; Kenneth D Westover; Timothy A J Haystead
Journal:  J Biol Chem       Date:  2019-12-30       Impact factor: 5.157

Review 5.  Inflammasome-associated nucleotide-binding domain, leucine-rich repeat proteins and inflammatory diseases.

Authors:  Sushmita Jha; Jenny P-Y Ting
Journal:  J Immunol       Date:  2009-12-15       Impact factor: 5.422

Review 6.  Endogenous ligands of TLR4 promote unresolving tissue fibrosis: Implications for systemic sclerosis and its targeted therapy.

Authors:  Swati Bhattacharyya; John Varga
Journal:  Immunol Lett       Date:  2017-09-28       Impact factor: 3.685

Review 7.  IRAK-4 inhibitors for inflammation.

Authors:  Zhulun Wang; Holger Wesche; Tracey Stevens; Nigel Walker; Wen-Chen Yeh
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

Review 8.  IRAK signalling in cancer.

Authors:  G W Rhyasen; D T Starczynowski
Journal:  Br J Cancer       Date:  2014-10-07       Impact factor: 7.640

9.  Design of Novel IRAK4 Inhibitors Using Molecular Docking, Dynamics Simulation and 3D-QSAR Studies.

Authors:  Swapnil P Bhujbal; Weijie He; Jung-Mi Hah
Journal:  Molecules       Date:  2022-09-24       Impact factor: 4.927

Review 10.  Inhibition of interleukin-1 receptor-associated kinase 1 (IRAK1) as a therapeutic strategy.

Authors:  Jack W Singer; Angela Fleischman; Suliman Al-Fayoumi; John O Mascarenhas; Qiang Yu; Anupriya Agarwal
Journal:  Oncotarget       Date:  2018-09-07
  10 in total

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