Literature DB >> 32184967

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.

Carrow Wells1,2, Rafael M Couñago3,4, Juanita C Limas5, Tuanny L Almeida3,4, Jeanette Gowen Cook6, David H Drewry1,2, Jonathan M Elkins3,7, Opher Gileadi3,7, Nirav R Kapadia1,2, Alvaro Lorente-Macias8, Julie E Pickett1,2, Alexander Riemen9, Roberta R Ruela-de-Sousa3,4, Timothy M Willson1,2, Cunyu Zhang10, William J Zuercher1,2,11, Reena Zutshi9, Alison D Axtman1,2.   

Abstract

Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC-AAK1-1, 25) that is potent and selective for AAK1/BMP2K over other NAK family members, demonstrates narrow activity in a kinome-wide screen, and is functionally active in cells. This inhibitor represents one of the best available small molecule tools to study the functions of AAK1 and BMP2K.
Copyright © 2019 American Chemical Society.

Entities:  

Year:  2019        PMID： 32184967      PMCID： PMC7073879          DOI： 10.1021/acsmedchemlett.9b00399

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.632


  21 in total

Review 1.  The Ark1/Prk1 family of protein kinases. Regulators of endocytosis and the actin skeleton.

Authors:  Elizabeth Smythe; Kathryn R Ayscough
Journal:  EMBO Rep       Date:  2003-03       Impact factor: 8.807

2.  Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity.

Authors:  Sven Verdonck; Szu-Yuan Pu; Fiona J Sorrell; Jon M Elkins; Mathy Froeyen; Ling-Jie Gao; Laura I Prugar; Danielle E Dorosky; Jennifer M Brannan; Rina Barouch-Bentov; Stefan Knapp; John M Dye; Piet Herdewijn; Shirit Einav; Steven De Jonghe
Journal:  J Med Chem       Date:  2019-06-12       Impact factor: 7.446

3.  The adaptor-associated kinase 1, AAK1, is a positive regulator of the Notch pathway.

Authors:  Neetu Gupta-Rossi; Sara Ortica; Vannary Meas-Yedid; Sara Heuss; Julien Moretti; Jean-Christophe Olivo-Marin; Alain Israël
Journal:  J Biol Chem       Date:  2011-04-04       Impact factor: 5.157

4.  Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Authors:  Christopher R M Asquith; Tuomo Laitinen; James M Bennett; Paulo H Godoi; Michael P East; Graham J Tizzard; Lee M Graves; Gary L Johnson; Ronna E Dornsife; Carrow I Wells; Jonathan M Elkins; Timothy M Willson; William J Zuercher
Journal:  ChemMedChem       Date:  2017-11-27       Impact factor: 3.466

5.  AAK1 regulates Numb function at an early step in clathrin-mediated endocytosis.

Authors:  Erika B Sorensen; Sean D Conner
Journal:  Traffic       Date:  2008-07-24       Impact factor: 6.215

6.  Dysfunction of endocytic kinase AAK1 in ALS.

Authors:  Bingxing Shi; Sean D Conner; Jian Liu
Journal:  Int J Mol Sci       Date:  2014-12-10       Impact factor: 5.923

7.  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

8.  The Atypical Kinase RIOK1 Promotes Tumor Growth and Invasive Behavior.

Authors:  Florian Weinberg; Nadine Reischmann; Lisa Fauth; Sanaz Taromi; Justin Mastroianni; Martin Köhler; Sebastian Halbach; Andrea C Becker; Niantao Deng; Tatjana Schmitz; Franziska Maria Uhl; Nicola Herbener; Bianca Riedel; Fabian Beier; Alexander Swarbrick; Silke Lassmann; Jörn Dengjel; Robert Zeiser; Tilman Brummer
Journal:  EBioMedicine       Date:  2017-04-12       Impact factor: 8.143

9.  Structure of the human protein kinase MPSK1 reveals an atypical activation loop architecture.

Authors:  Jeyanthy Eswaran; Antonio Bernad; Jose M Ligos; Barbara Guinea; Judit E Debreczeni; Frank Sobott; Sirlester A Parker; Rafael Najmanovich; Benjamin E Turk; Stefan Knapp
Journal:  Structure       Date:  2008-01       Impact factor: 5.006

10.  WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.

Authors:  Megan J Agajanian; Matthew P Walker; Alison D Axtman; Roberta R Ruela-de-Sousa; D Stephen Serafin; Alex D Rabinowitz; David M Graham; Meagan B Ryan; Tigist Tamir; Yuko Nakamichi; Melissa V Gammons; James M Bennett; Rafael M Couñago; David H Drewry; Jonathan M Elkins; Carina Gileadi; Opher Gileadi; Paulo H Godoi; Nirav Kapadia; Susanne Müller; André S Santiago; Fiona J Sorrell; Carrow I Wells; Oleg Fedorov; Timothy M Willson; William J Zuercher; Michael B Major
Journal:  Cell Rep       Date:  2019-01-02       Impact factor: 9.423
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  8 in total

1.  Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses.

Authors:  David H Drewry; Frances M Potjewyd; Armin Bayati; Jeffery L Smith; Rebekah J Dickmander; Stefanie Howell; Sharon Taft-Benz; Sophia M Min; Mohammad Anwar Hossain; Mark Heise; Peter S McPherson; Nathaniel J Moorman; Alison D Axtman
Journal:  J Med Chem       Date:  2022-09-16       Impact factor: 8.039

2.  Development of a potent and selective chemical probe for the pleiotropic kinase CK2.

Authors:  Carrow I Wells; David H Drewry; Julie E Pickett; Amelie Tjaden; Andreas Krämer; Susanne Müller; Laszlo Gyenis; Daniel Menyhart; David W Litchfield; Stefan Knapp; Alison D Axtman
Journal:  Cell Chem Biol       Date:  2021-01-22       Impact factor: 8.116

3.  Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2.

Authors:  Xuan Yang; Rebekah J Dickmander; Armin Bayati; Sharon A Taft-Benz; Jeffery L Smith; Carrow I Wells; Emily A Madden; Jason W Brown; Erik M Lenarcic; Boyd L Yount; Edcon Chang; Alison D Axtman; Ralph S Baric; Mark T Heise; Peter S McPherson; Nathaniel J Moorman; Timothy M Willson
Journal:  bioRxiv       Date:  2022-01-26

4.  AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.

Authors:  Frances M Potjewyd; Joel K Annor-Gyamfi; Jeffrey Aubé; Shaoyou Chu; Ivie L Conlon; Kevin J Frankowski; Shiva K R Guduru; Brian P Hardy; Megan D Hopkins; Chizuru Kinoshita; Dmitri B Kireev; Emily R Mason; Charles T Moerk; Felix Nwogbo; Kenneth H Pearce; Timothy I Richardson; David A Rogers; Disha M Soni; Michael Stashko; Xiaodong Wang; Carrow Wells; Timothy M Willson; Stephen V Frye; Jessica E Young; Alison D Axtman
Journal:  Alzheimers Dement (N Y)       Date:  2022-04-20

5.  Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses.

Authors:  Xuan Yang; Rebekah J Dickmander; Armin Bayati; Sharon A Taft-Benz; Jeffery L Smith; Carrow I Wells; Emily A Madden; Jason W Brown; Erik M Lenarcic; Boyd L Yount; Edcon Chang; Alison D Axtman; Ralph S Baric; Mark T Heise; Peter S McPherson; Nathaniel J Moorman; Timothy M Willson
Journal:  ACS Chem Biol       Date:  2022-06-19       Impact factor: 4.634

6.  PKIS deep dive yields a chemical starting point for dark kinases and a cell active BRSK2 inhibitor.

Authors:  Tigist Y Tamir; David H Drewry; Carrow Wells; M Ben Major; Alison D Axtman
Journal:  Sci Rep       Date:  2020-09-28       Impact factor: 4.379

Review 7.  Kinase Inhibitors as Underexplored Antiviral Agents.

Authors:  Javier García-Cárceles; Elena Caballero; Carmen Gil; Ana Martínez
Journal:  J Med Chem       Date:  2021-05-10       Impact factor: 7.446

8.  Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.

Authors:  David H Drewry; Joel K Annor-Gyamfi; Carrow I Wells; Julie E Pickett; Verena Dederer; Franziska Preuss; Sebastian Mathea; Alison D Axtman
Journal:  J Med Chem       Date:  2021-08-01       Impact factor: 7.446
  8 in total

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