Literature DB >> 25479567

Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.

Divya Chaudhary1, Shaughnessy Robinson, Donna L Romero.   

Abstract

IRAK4, a serine/threonine kinase, plays a key role in both inflammation and oncology diseases. Herein, we summarize the compelling biology surrounding the IRAK4 signaling node in disease, review key structural features of IRAK4 including selectivity challenges, and describe efforts to discover clinically viable IRAK4 inhibitors. Finally, a view of knowledge gained and remaining challenges is provided.

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Year:  2014        PMID： 25479567     DOI： 10.1021/jm5016044

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  26 in total

Review 1.  Translating nucleic acid-sensing pathways into therapies.

Authors:  Tobias Junt; Winfried Barchet
Journal:  Nat Rev Immunol       Date:  2015-08-21       Impact factor: 53.106

Review 2.  TLR-4 Signaling vs. Immune Checkpoints, miRNAs Molecules, Cancer Stem Cells, and Wingless-Signaling Interplay in Glioblastoma Multiforme-Future Perspectives.

Authors:  Jakub Litak; Cezary Grochowski; Joanna Litak; Ida Osuchowska; Krzysztof Gosik; Elżbieta Radzikowska; Piotr Kamieniak; Jacek Rolinski
Journal:  Int J Mol Sci       Date:  2020-04-28       Impact factor: 5.923

Review 3.  Lipopolysaccharide induced vascular smooth muscle cells proliferation: A new potential therapeutic target for proliferative vascular diseases.

Authors:  Dehua Jiang; Yu Yang; Dongye Li
Journal:  Cell Prolif       Date:  2017-02-02       Impact factor: 6.831

4.  Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.

Authors:  Naomi S Rajapaksa; Alberto Gobbi; Joy Drobnick; Steven Do; Aleksandr Kolesnikov; Jun Liang; Yongsheng Chen; Swathi Sujatha-Bhaskar; Zhiyu Huang; Hans Brightbill; Ross Francis; Christine Yu; Edna F Choo; Kevin DeMent; Yingqing Ran; Le An; Claire Emson; Jonathan Maher; John Wai; Brent S McKenzie; Patrick J Lupardus; Ali A Zarrin; James R Kiefer; Marian C Bryan
Journal:  ACS Med Chem Lett       Date:  2019-11-11       Impact factor: 4.345

5.  Overcoming adaptive therapy resistance in AML by targeting immune response pathways.

Authors:  Katelyn Melgar; Morgan M Walker; LaQuita M Jones; Lyndsey C Bolanos; Kathleen Hueneman; Mark Wunderlich; Jian-Kang Jiang; Kelli M Wilson; Xiaohu Zhang; Patrick Sutter; Amy Wang; Xin Xu; Kwangmin Choi; Gregory Tawa; Donald Lorimer; Jan Abendroth; Eric O'Brien; Scott B Hoyt; Ellin Berman; Christopher A Famulare; James C Mulloy; Ross L Levine; John P Perentesis; Craig J Thomas; Daniel T Starczynowski
Journal:  Sci Transl Med       Date:  2019-09-04       Impact factor: 17.956

Review 6.  Deconstructing innate immune signaling in myelodysplastic syndromes.

Authors:  Madeline Niederkorn; Molly Smith; Laura Barreyro; Melinda E Varney; Katelyn Melgar; Daniel T Starczynowski
Journal:  Exp Hematol       Date:  2015-07-02       Impact factor: 3.084

7.  PROTAC Degradation of IRAK4 for the Treatment of Cancer.

Authors:  Robert B Kargbo
Journal:  ACS Med Chem Lett       Date:  2019-09-30       Impact factor: 4.345

8.  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

9.  Small Molecule Mimetics of α-Helical Domain of IRAK2 Attenuate the Proinflammatory Effects of IL-33 in Asthma-like Mouse Models.

Authors:  Jinghong Li; Kunio Saruta; Justin P Dumouchel; Jenna M Magat; Joanna L Thomas; Dariush Ajami; Mitra Rebek; Julius Rebek; Timothy D Bigby
Journal:  J Immunol       Date:  2018-05-04       Impact factor: 5.422

10.  Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.

Authors:  W Michael Seganish; Thierry O Fischmann; Brad Sherborne; Julius Matasi; Brian Lavey; William T McElroy; Deen Tulshian; James Tata; Christopher Sondey; Charles G Garlisi; Kristine Devito; James Fossetta; Daniel Lundell; Xiaoda Niu
Journal:  ACS Med Chem Lett       Date:  2015-07-12       Impact factor: 4.345
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