Literature DB >> 35403825

Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype.

Christopher R M Asquith1,2, Louisa Temme1, Michael P East2, Tuomo Laitinen3, Julie Pickett1, Frank E Kwarcinski4, Parvathi Sinha4, Carrow I Wells1, Gary L Johnson2,5, Reena Zutshi4, David H Drewry1,5.   

Abstract

Deep annotation of a library of 4-anilinoquin(az)olines led to the identification of 7-iodo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine 16 as a potent inhibitor (IC50 =14 nM) of Protein Kinase Novel 3 (PKN3) with micromolar activity in cells. Compound 16 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T-cell acute lymphoblastic leukemia. These 4-anilinoquin(az)olines may also be useful tools to uncover the therapeutic potential of PKN3 inhibition in a broad range of diseases.
© 2022 Wiley-VCH GmbH.

Entities:  

Keywords:  4-anilinoquinazoline; 4-anilinoquinoline; Protein Kinase Novel 3 (PKN3); homology model

Mesh：

Substances：

Year:  2022        PMID： 35403825      PMCID： PMC9233141          DOI： 10.1002/cmdc.202200161

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.540


  55 in total

1.  Targeting the Water Network in Cyclin G-Associated Kinase (GAK) with 4-Anilino-quin(az)oline Inhibitors.

Authors:  Christopher R M Asquith; Graham J Tizzard; James M Bennett; Carrow I Wells; Jonathan M Elkins; Timothy M Willson; Antti Poso; Tuomo Laitinen
Journal:  ChemMedChem       Date:  2020-05-26       Impact factor: 3.466

Review 2.  RNAi therapeutics: principles, prospects and challenges.

Authors:  Lars Aagaard; John J Rossi
Journal:  Adv Drug Deliv Rev       Date:  2007-03-16       Impact factor: 15.470

Review 3.  Phosphoinositide 3-kinase/Akt signaling pathway and its therapeutical implications for human acute myeloid leukemia.

Authors:  A M Martelli; M Nyåkern; G Tabellini; R Bortul; P L Tazzari; C Evangelisti; L Cocco
Journal:  Leukemia       Date:  2006-06       Impact factor: 11.528

4.  Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.

Authors:  Christopher R M Asquith; Neil Fleck; Chad D Torrice; Daniel J Crona; Christoph Grundner; William J Zuercher
Journal:  Bioorg Med Chem Lett       Date:  2019-07-10       Impact factor: 2.823

5.  Atu027, a liposomal small interfering RNA formulation targeting protein kinase N3, inhibits cancer progression.

Authors:  Manuela Aleku; Petra Schulz; Oliver Keil; Ansgar Santel; Ute Schaeper; Britta Dieckhoff; Oliver Janke; Jens Endruschat; Birgit Durieux; Nadine Röder; Kathrin Löffler; Christian Lange; Melanie Fechtner; Kristin Möpert; Gerald Fisch; Sibylle Dames; Wolfgang Arnold; Karin Jochims; Klaus Giese; Bertram Wiedenmann; Arne Scholz; Jörg Kaufmann
Journal:  Cancer Res       Date:  2008-12-01       Impact factor: 12.701

6.  Development of an intracellularly acting inhibitory peptide selective for PKN.

Authors:  Kazuhiro Shiga; Kentaro Takayama; Shiroh Futaki; Jessica E Hutti; Lewis C Cantley; Katsuko Ueki; Yoshitaka Ono; Hideyuki Mukai
Journal:  Biochem J       Date:  2009-12-23       Impact factor: 3.857

7.  Crystal structures of PRK1 in complex with the clinical compounds lestaurtinib and tofacitinib reveal ligand induced conformational changes.

Authors:  Philip Chamberlain; Silvia Delker; Barbra Pagarigan; Afshin Mahmoudi; Pilgrim Jackson; Mahan Abbasian; Jeff Muir; Neil Raheja; Brian Cathers
Journal:  PLoS One       Date:  2014-08-11       Impact factor: 3.240

8.  Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.

Authors:  James D Vasta; Cesear R Corona; Jennifer Wilkinson; Chad A Zimprich; James R Hartnett; Morgan R Ingold; Kristopher Zimmerman; Thomas Machleidt; Thomas A Kirkland; Kristin G Huwiler; Rachel Friedman Ohana; Michael Slater; Paul Otto; Mei Cong; Carrow I Wells; Benedict-Tilman Berger; Thomas Hanke; Carina Glas; Ke Ding; David H Drewry; Kilian V M Huber; Timothy M Willson; Stefan Knapp; Susanne Müller; Poncho L Meisenheimer; Frank Fan; Keith V Wood; Matthew B Robers
Journal:  Cell Chem Biol       Date:  2017-11-22       Impact factor: 8.116

9.  Structural Basis for the Inhibition of Cyclin G-Associated Kinase by Gefitinib.

Authors:  Naomi Ohbayashi; Kazutaka Murayama; Miyuki Kato-Murayama; Mutsuko Kukimoto-Niino; Tamami Uejima; Takayoshi Matsuda; Noboru Ohsawa; Shigeyuki Yokoyoma; Hiroshi Nojima; Mikako Shirouzu
Journal:  ChemistryOpen       Date:  2018-09-10       Impact factor: 2.911

10.  Optimization of 4-Anilinoquinolines as Dengue Virus Inhibitors.

Authors:  Pei-Tzu Huang; Sirle Saul; Shirit Einav; Christopher R M Asquith
Journal:  Molecules       Date:  2021-12-03       Impact factor: 4.411
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