729
Views
8
CrossRef citations to date
0
Altmetric
Review

A patent review of adaptor associated kinase 1 (AAK1) inhibitors (2013-present)

, ORCID Icon &
Pages 911-936 | Received 05 Mar 2021, Accepted 07 May 2021, Published online: 21 May 2021

References

  • Sorrell FJ, Szklarz M, Abdul Azeez KR, et al., Family-wide structural analysis of human Numb-associated protein kinases. Structure. 24(3): 401–411. 2016.
  • Sorensen EB, Conner SD. AAK1 regulates Numb function at an early step in clathrin-mediated endocytosis. Traffic. 2008;9(10):1791–1800.
  • Conner SD, Schmid S. Identification of an adaptor-associated kinase, AAK1, as a regulator of clathrin-mediated endocytosis. J Cell Biol. 2002;156(5):921–929.
  • Ricotta D, Conner SD, Schmid SL, et al. Phosphorylation of the AP2 mu subunit by AAK1 mediates high affinity binding to membrane protein sorting signals. J Cell Biol. 2002;156(5):791–795.
  • Conner SD, Schröter T, Schmid SL. AAK1-mediated micro2 phosphorylation is stimulated by assembled clathrin. Traffic. 2003;4(12):885–890.
  • Kadlecova Z, Spielman SJ, Loerke D, et al. Regulation of clathrin-mediated endocytosis by hierarchical allosteric activation of AP2. J Cell Biol. 2017;216(1):167–179.
  • Owen DJ, Collins BM, Evans PR. Adaptors for clathrin coats: structure and function. Annu Rev Cell Dev Biol. 2004;20(1):153–191.
  • Henderson DM, Conner SD. A novel AAK1 splice variant functions at multiple steps of the endocytic pathway. Mol Biol Cell. 2007;18(7):2698–2706.
  • Gupta-Rossi N, Ortica S, Meas-Yedid, et al. The adaptor-associated kinase 1, AAK1, is a positive regulator of the Notch pathway. J Biol Chem. 2011;286(21):18720–18730.
  • Fu X, Ke M, Yu W, et al. Periodic Variation of AAK1 in an Aβ1–42-Induced Mouse Model of Alzheimer’s Disease. J Mol Neurosci. 2018;65(2):179–189.
  • Kostich W, Hamman BD, Li YW, et al., Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 358(3): 371–386. 2016.
  • Kuai L, Ong S, Madison JM, et al. AAK1 Identified as an Inhibitor of Neuregulin-1/ErbB4-Dependent Neurotrophic Factor Signaling Using Integrative Chemical Genomics and Proteomics. Chem Biol. 2011;18(7):891–906.
  • Shi B, Conner SD, Liu J. Dysfunction of Endocytic Kinase AAK1 in ALS. Int J Mol Sci. 2014;15(12):22918–22932.
  • Latourelle JC, Pankratz N, Dumitriu A, et al. Genomewide association study for onset age in Parkinson disease. BMC Med Genet. 2009;10(1):98.
  • Lconada A, Bauer U, Hoflack B. A tyrosine-based motif and a casein kinase II phosphorylation site regulate the intracellular trafficking of the varicella-zoster virus glycoprotein I, a protein localized in the trans-Golgi network. EMBO J. 1996;15:96–6110.
  • Bhattacharyya S, Hope TJ, Young JA. Differential requirements for clathrin endocytic pathway components in cellular entry by Ebola and Marburg glycoprotein pseudovirions. Virology. 2011;419(1):1–9.
  • Huang HC, Chen CC, Chang WC, et al. Entry of hepatitis B virus into immortalized human primary hepatocytes by clathrin-dependent endocytosis. J Virol. 2012;86(17):9443–9453.
  • Humphries AC, Dodding MP, Barry DJ, et al. Clathrin potentiates vaccinia-induced actin polymerization to facilitate viral spread. Cell Host Microbe. 2012;12(3):346–359.
  • Neveu G, Barouch-Bentov R, Ziv-Av A, et al. Identification and targeting of an interaction between a tyrosine motif within hepatitis C virus core protein and AP2M1 essential for viral assembly. PLoS Pathog. 2012;8(8):e1002845.
  • Neveu G, Ziv-Av A, Barouch-Bentov R, et al. AP-2-Associated Protein Kinase 1 and Cyclin G-Associated Kinase Regulate Hepatitis C Virus Entry and Are Potential Drug Targets. J Virol. 2015;89(8):4387–4404.
  • Xiao F, Wang S, Barouch-Bentov R, et al. Interactions between the Hepatitis C Virus Nonstructural 2 Protein and Host Adaptor Proteins 1 and 4 Orchestrate Virus Release. mBio. 2018;9(2):e02233.
  • Bekerman E, Neveu G, Shulla A, et al., Anticancer Kinase Inhibitors Impair Intracellular Viral Trafficking and Exert Broad-Spectrum Antiviral Effects. J Clin Invest. 127(4): 1338–1352. 2017.
  • Pu SY, Xiao F, Schor S, et al. Feasibility and biological rationale of repurposing sunitinib and erlotinib for dengue treatment. Antiviral Res. 2018;155:67–75.
  • Luo J, Zhang Y, Wang Y, et al. Rhabdovirus Infection Is Dependent on Serine/Threonine Kinase AP2-Associated Kinase 1. Life. 2020;10(9):170.
  • Wang C, Wang J, Shuai L, et al. The Serine/Threonine Kinase AP2-Associated Kinase 1 Plays an Important Role in Rabies Virus Entry. Viruses. 2020;12(1):45.
  • Stebbing J, Krishnan V, De Bono S, et al. Mechanism of baricitinib supports artificial intelligence-predicted testing in COVID-19 patients. EMBO Mol Med. 2020;12(8):e12697.
  • Hoang TN, Pino M, Boddapati AK, et al. Baricitinib treatment resolves lower-airway macrophage inflammation and neutrophil recruitment in SARS-CoV-2-infected rhesus macaques. Cell. 2021;184(2):460–475.
  • Elkins JM, Fedele V, Szklarz M, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016;34(1):95–103.
  • Wells C, Couñago RM, Limas JC, et al., SGC-AAK1-1: a Chemical Probe Targeting AAK1 and BMP2K. ACS Med Chem Lett. 11(3): 340–345. 2020.
  • Agajanian MJ, Walker MP, Axtman AD, et al. WNT Activates the AAK1 Kinase to Promote Clathrin Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop. Cell Rep. 2019;26(1):79–93.
  • Verdonck S, Pu S, Sorrell FJ, et al. Synthesis and Structure–Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3-b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. J Med Chem. 2019;62(12):5810–5831.
  • Lexicon Pharmaceuticals Inc.Imidazo[l,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof. WO2013134219 (2013).
  • Lexicon Pharmaceuticals Inc. Imidazo[l,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use. WO2015035167 (2015).
  • Bristol-Myers Squibb company. Imidazopyridazine kinase inhibitors useful to treating a disease or disorder mediated by AAK1, such as Alzheimer’s disease, bipolar disorder, pain, schizophrenia. WO2015026574 (2015).
  • Lexicon Pharmaceuticals Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain. WO2013134336 (2013).
  • Lexicon Pharmaceuticals Inc. Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use. WO2013134228 (2013).
  • Lexicon Pharmaceuticals Inc. Inhibitors of adaptor associated kinase 1, compositions comprising them, and methods of their use. WO2015142714 (2015).
  • Lexicon Pharmaceuticals Inc. Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use. WO2015035117 (2015).
  • Bristol-Myers Squibb company. Biaryl kinase inhibitors. WO2015153720 (2015).
  • Bristol-Myers Squibb company. Biaryl kinase inhibitors. WO2017059085 (2017).
  • Bristol-Myers Squibb company. Aryl amide kinase inhibitors. WO2015006100 (2015).
  • Bristol-Myers Squibb company. Aryl ether-base kinase inhibitors. WO2013134036 (2013).
  • Bristol-Myers Squibb company. Aryl ether-base kinase inhibitors. WO2015/038112 (2015).
  • Bristol-Myers Squibb company. 5H-Chromeno[3,4-c]pyridines as inhibitors of adaptor associated kinase (AAK1). WO2014130258 (2014).
  • Bristol-Myers Squibb company. Fused pyridines as adaptor associated kinase 1 (AAK1) inhibitors. WO2016164295 (2016).
  • Bristol-Myers Squibb company. Aryl lactam kinase inhibitors. WO2014022167 (2014).
  • Bristol-Myers Squibb company. Aryl lactam kinase inhibitors. WO2015116060 (2015).
  • Louis JV, Lu Y, Pieschl R, et al. [3H]BMT-046091 a potent and selective radioligand to determine AAK1 distribution and target engagement. Neuropharmacology. 2017;118:167–174.
  • Bristol-Myers Squibb company. Pyrrolotriazine kinase inhibitors. WO2015054358 (2015).
  • Bristol-Myers Squibb company. Quinoline-based kinase inhibitors. WO2015116492 (2015).
  • Bristol-Myers Squibb company. Heterocyclic kinase inhibitors.WO2016022312 (2016).
  • A list of FDA-approved targeted small molecule protein kinase inhibitors. [cited 2021 Apr 21]. Available from: http://www.brimr.org/PKI/PKIs.htm

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.