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Flax RG, Rosston P, Rocha C, Anderson B, Capener JL, Durcan TM, Drewry DH, Prinos P, Axtman AD. Illumination of understudied ciliary kinases. Front Mol Biosci. 2024;11:1352781. doi: 10.3389/fmolb.2024.1352781. eCollection 2024. Review. PubMed PMID: 38523660; PubMed Central PMCID: PMC10958382.
Gomez SM, Axtman AD, Willson TM, Major MB, Townsend RR, Sorger PK, Johnson GL. Illuminating function of the understudied druggable kinome. Drug Discov Today. 2024 Mar;29(3):103881. doi: 10.1016/j.drudis.2024.103881. Epub 2024 Jan 11. Review. PubMed PMID: 38218213.
Bashore FM, Katis VL, Du Y, Sikdar A, Wang D, Bradshaw WJ, Rygiel KA, Leisner TM, Chalk R, Mishra S, Williams CA, Gileadi O, Brennan PE, Wiley JC, Gockley J, Cary GA, Carter GW, Young JE, Pearce KH, Fu H, Axtman AD. Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM. PLoS One. 2024;19(2):e0293548. doi: 10.1371/journal.pone.0293548. eCollection 2024. PubMed PMID: 38359047; PubMed Central PMCID: PMC10868801.
Asressu KH, Smith JL, Dickmander RJ, Moorman NJ, Wellnitz J, Popov K, Axtman AD, Willson TM. Synthesis of 5-Benzylamino and 5-Alkylamino-substituted Pyrimido[4,5-c]quinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity. BioRxiv. 2024. doi: 10.1101/2024.01.30.578037.
Asressu KH, Smith JL, Dickmander RJ, Moorman NJ, Wellnitz J, Popov KI, Axtman AD, Willson TM. Synthesis of 5-Benzylamino and 5-Alkylamino-substituted Pyrimido[4,5-c]quinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity. Pharmaceuticals. 2024; 17:306. doi: 10.3390/ph17030306.
Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL. Discovery and Optimization of Narrow Spectrum Inhibitors of Tousled Like Kinase 2 (TLK2) Using Quantitative Structure Activity Relationships. bioRxiv. 2023 Dec 28;. doi: 10.1101/2023.12.28.573261. PubMed PMID: 38234837; PubMed Central PMCID: PMC10793458.
Du Y, Bradshaw WJ, Leisner TM, Annor-Gyamfi JK, Qian K, Bashore FM, Sikdar A, Nwogbo FO, Ivanov AA, Frye SV, Gileadi O, Brennan PE, Levey AI, Axtman AD, Pearce KH, Fu H, Katis VL. Discovery of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer's disease. J Biol Chem. 2023 Dec;299(12):105382. doi: 10.1016/j.jbc.2023.105382. Epub 2023 Oct 21. PubMed PMID: 37866628; PubMed Central PMCID: PMC10692723.
Bashore FM, Annor-Gyamfi J, Du Y, Katis V, Nwogbo F, Flax RG, Frye SV, Pearce KH, Fu H, Willson TM, Drewry DH, Axtman AD. Fused Tetrahydroquinolines Are Interfering with Your Assay. J Med Chem. 2023 Nov 9;66(21):14434-14446. doi: 10.1021/acs.jmedchem.3c01277. Epub 2023 Oct 24. Review. PubMed PMID: 37874947; PubMed Central PMCID: PMC10641811.
Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM. Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines toward the Development of an In Vivo Chemical Probe for CSNK2A. ACS Omega. 2023 Oct 24;8(42):39546-39561. doi: 10.1021/acsomega.3c05377. eCollection 2023 Oct 24. PubMed PMID: 37901516; PubMed Central PMCID: PMC10600890.
Bashore FM, Katis VL, Du Y, Sikdar A, Wang D, Bradshaw WJ, Rygiel KA, Leisner TM, Chalk R, Mishra S, Williams AC, Gileadi O, Brennan PE, Wiley JC, Gockley J, Cary GA, Carter GW, Young JE, Pearce KH, Fu H, Axtman AD. Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM. bioRxiv. 2023 Jul 29;. doi: 10.1101/2023.07.28.551026. PubMed PMID: 37547005; PubMed Central PMCID: PMC10402180.
Castano A, Silvestre M, Wells CI, Sanderson JL, Ferrer CA, Ong HW, Lang Y, Richardson W, Silvaroli JA, Bashore FM, Smith JL, Genereux IM, Dempster K, Drewry DH, Pabla NS, Bullock AN, Benke TA, Ultanir SK, Axtman AD. Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology. Elife. 2023 Jul 25;12. doi: 10.7554/eLife.88206. PubMed PMID: 37490324; PubMed Central PMCID: PMC10406435.
Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM. Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines Toward the Development of an In Vivo Chemical Probe for CSNK2A. bioRxiv. 2023 Jul 23;. doi: 10.1101/2023.05.15.540828. PubMed PMID: 37292607; PubMed Central PMCID: PMC10245575.
Castano A, Silvestre M, Wells CI, Sanderson JL, Ferrer CA, Ong HW, Lang Y, Richardson W, Silvaroli JA, Bashore FM, Smith JL, Genereux IM, Dempster K, Drewry DH, Pabla NS, Bullock AN, Benke TA, Ultanir S, Axtman AD. Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology. bioRxiv. 2023 Jun 16;. doi: 10.1101/2023.04.24.538049. PubMed PMID: 37162893; PubMed Central PMCID: PMC10168277.
Du Y, Bradshaw WJ, Leisner TM, Annor-Gyamfi JK, Qian K, Bashore FM, Sikdar A, Nwogbo FO, Ivanov AA, Frye SV, Gileadi O, Brennan PE, Levey AI, Axtman AD, Pearce KH, Fu H, Katis VL. Development of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic strategy for Alzheimer's disease. bioRxiv. 2023 May 22;. doi: 10.1101/2023.05.22.541727. PubMed PMID: 37292860; PubMed Central PMCID: PMC10245921.
Axtman AD, Brennan PE, Frappier-Brinton T, Betarbet R, Carter GW, Fu H, Gileadi O, Greenwood AK, Leal K, Longo FM, Mangravite LM, Edwards AM, Levey AI. Open drug discovery in Alzheimer's disease. Alzheimers Dement (N Y). 2023 Apr-Jun;9(2):e12394. doi: 10.1002/trc2.12394. eCollection 2023 Apr-Jun. PubMed PMID: 37215505; PubMed Central PMCID: PMC10192886.
Ong HW, Liang Y, Richardson W, Lowry ER, Wells CI, Chen X, Silvestre M, Dempster K, Silvaroli JA, Smith JL, Wichterle H, Pabla NS, Ultanir SK, Bullock AN, Drewry DH, Axtman AD. Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective. ACS Chem Neurosci. 2023 May 3;14(9):1672-1685. doi: 10.1021/acschemneuro.3c00135. Epub 2023 Apr 21. PubMed PMID: 37084253; PubMed Central PMCID: PMC10161233.
Durcan TM, Axtman AD. Editorial: The next generation of tools and technologies for studying human neurons in a dish. Front Cell Neurosci. 2023;17:1196543. doi: 10.3389/fncel.2023.1196543. eCollection 2023. PubMed PMID: 37124399; PubMed Central PMCID: PMC10140577.
Bashore FM, Marquez AB, Chaikuad A, Howell S, Dunn AS, Beltran AA, Smith JL, Drewry DH, Beltran AS, Axtman AD. Modulation of tau tubulin kinases (TTBK1 and TTBK2) impacts ciliogenesis. Sci Rep. 2023 Apr 14;13(1):6118. doi: 10.1038/s41598-023-32854-4. PubMed PMID: 37059819; PubMed Central PMCID: PMC10104807.
Davis-Gilbert ZW, Krämer A, Dunford JE, Howell S, Senbabaoglu F, Wells CI, Bashore FM, Havener TM, Smith JL, Hossain MA, Oppermann U, Drewry DH, Axtman AD. Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2. ACS Med Chem Lett. 2023 Apr 13;14(4):432-441. doi: 10.1021/acsmedchemlett.2c00530. eCollection 2023 Apr 13. PubMed PMID: 37077385; PubMed Central PMCID: PMC10108397.
Ong HW, Liang Y, Richardson W, Lowry ER, Wells CI, Chen X, Silvestre M, Dempster K, Silvaroli JA, Smith JL, Wichterle H, Pabla NS, Ultanir SK, Bullock AN, Drewry DH, Axtman AD. A Potent and Selective CDKL5/GSK3 Chemical Probe is Neuroprotective. bioRxiv. 2023 Feb 10;. doi: 10.1101/2023.02.09.527935. PubMed PMID: 36798313; PubMed Central PMCID: PMC9934649.
Menyhart D, Gyenis L, Jurcic K, Roffey SE, Puri A, Jovanovic P, Szkop KJ, Pittock P, Lajoie G, Axtman AD, Larsson O, Topisirovic I, Litchfield DW. Comparison of CX-4945 and SGC-CK2-1 as inhibitors of CSNK2 using quantitative phosphoproteomics: Triple SILAC in combination with inhibitor-resistant CSNK2. Current research in chemical biology. 2023; 3:100041. doi: 10.1016/j.crchbi.2023.100041.
Potjewyd FM, Katis V, Du Y, Bradshaw W, Sikdar A, Nwogbo F, Leisner T, Wang D, Hardy BP, Kireev DB, Pearce KH, Fu H, Frye SV, Axtman AD. Towards the development of a chemical probe targeting the disruption of SYK tandem SH2 domain and FCεR1γ interactions for Alzheimer’s disease. Alzheimers Dement. 2023; 19:e067392. doi: 10.1002/alz.067392.
Ong H, Drewry DH, Axtman AD. CK2 chemical probes: Past, present, and future. Kinases and phosphatases. 2023; 1:288. doi: 10.3390/kinasesphosphatases1040017.
Drewry DH, Potjewyd FM, Smith JL, Howell S, Axtman AD. Identification of a chemical probe for lipid kinase phosphatidylinositol-5-phosphate 4-kinase gamma (PI5P4Kγ). Curr Res Chem Biol. 2022 December. doi: 10.1016/j.crchbi.2022.100036.
Drewry DH, Potjewyd FM, Bayati A, Smith JL, Dickmander RJ, Howell S, Taft-Benz S, Min SM, Hossain MA, Heise M, McPherson PS, Moorman NJ, Axtman AD. Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses. J Med Chem. 2022 Oct 13;65(19):12860-12882. doi: 10.1021/acs.jmedchem.2c00697. Epub 2022 Sep 16. PubMed PMID: 36111834; PubMed Central PMCID: PMC9574855.
Yang X, Dickmander RJ, Bayati A, Taft-Benz SA, Smith JL, Wells CI, Madden EA, Brown JW, Lenarcic EM, Yount BL Jr, Chang E, Axtman AD, Baric RS, Heise MT, McPherson PS, Moorman NJ, Willson TM. Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses. ACS Chem Biol. 2022 Jul 15;17(7):1937-1950. doi: 10.1021/acschembio.2c00378. Epub 2022 Jun 19. PubMed PMID: 35723434; PubMed Central PMCID: PMC9236220.
Mishra S, Kinoshita C, Axtman AD, Young JE. Evaluation of a Selective Chemical Probe Validates That CK2 Mediates Neuroinflammation in a Human Induced Pluripotent Stem Cell-Derived Microglial Model. Front Mol Neurosci. 2022;15:824956. doi: 10.3389/fnmol.2022.824956. eCollection 2022. PubMed PMID: 35774866; PubMed Central PMCID: PMC9239073.
Agajanian MJ, Potjewyd FM, Bowman BM, Solomon S, LaPak KM, Bhatt DP, Smith JL, Goldfarb D, Axtman AD, Major MB. Protein proximity networks and functional evaluation of the casein kinase 1 gamma family reveal unique roles for CK1γ3 in WNT signaling. J Biol Chem. 2022 Jun;298(6):101986. doi: 10.1016/j.jbc.2022.101986. Epub 2022 Apr 27. PubMed PMID: 35487243; PubMed Central PMCID: PMC9157009.
Drewry DH, Potjewyd FM, Smith JL, Dickmander RJ, Bayati A, Howell S, Taft-Benz SA, Hossain MA, Heise MT, McPherson PS, Moorman NJ, Axtman AD. Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses. [preprint]. 2022 April. doi: 10.26434/chemrxiv-2022-bj274.
Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD. AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery. Alzheimers Dement (N Y). 2022;8(1):e12246. doi: 10.1002/trc2.12246. eCollection 2022. PubMed PMID: 35475262; PubMed Central PMCID: PMC9019904.
Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH Jr, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD. Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology. Alzheimers Dement (N Y). 2022;8(1):e12253. doi: 10.1002/trc2.12253. eCollection 2022. PubMed PMID: 35434254; PubMed Central PMCID: PMC9005681.
Johnson ECB, Carter EK, Dammer EB, Duong DM, Gerasimov ES, Liu Y, Liu J, Betarbet R, Ping L, Yin L, Serrano GE, Beach TG, Peng J, De Jager PL, Haroutunian V, Zhang B, Gaiteri C, Bennett DA, Gearing M, Wingo TS, Wingo AP, Lah JJ, Levey AI, Seyfried NT. Large-scale deep multi-layer analysis of Alzheimer's disease brain reveals strong proteomic disease-related changes not observed at the RNA level. Nat Neurosci. 2022 Feb;25(2):213-225. doi: 10.1038/s41593-021-00999-y. Epub 2022 Feb 3. PubMed PMID: 35115731; PubMed Central PMCID: PMC8825285.
Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD. Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. J Med Chem. 2022 Jan 27;65(2):1313-1328. doi: 10.1021/acs.jmedchem.1c00440. Epub 2021 Aug 1. PubMed PMID: 34333981; PubMed Central PMCID: PMC8802302.
Yang X, Dickmander RJ, Bayati A, Taft-Benz SA, Smith JL, Wells CI, Madden EA, Brown JW, Lenarcic EM, Yount BL Jr, Chang E, Axtman AD, Baric RS, Heise MT, McPherson PS, Moorman NJ, Willson TM. Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2. bioRxiv. 2022 Jan 26;. doi: 10.1101/2022.01.03.474779. PubMed PMID: 35018375; PubMed Central PMCID: PMC8750650.
Potjewyd FM, Marquez AB, Chaikuad A, Howell S, Dunn AS, Beltran AA, Smith JL, Drewry DH, Beltran AS, Axtman AD. Modulation of tau tubulin kinases ((TTBK1 and TTBK2) impacts ciliogenesis. Cell Press Sneak Peek. 2022.
Potjewyd FM, Marquez AB, Chaikuad A, Howell S, Dunn AS, Beltran AA, Smith JL, Drewry DH, Beltran AS, Axtman AD. Modulation of tau tubulin kinases (TTBK1 and TTBK2) impacts ciliogenesis. BioRxiv. 2022. doi: 10.1101/2022.05.06.490937.
Drewry DH, Potjewyd FM, Smith JL, Howell S, Axtman AD. Identification of a chemical probe for lipid kinase phosphatidylinositol-5-phosphate 4-kinase gamma (PI5P4Kγ). bioRxiv : the preprint server for biology. 2022. doi: 10.1101/2022.09.08.507203.
Davis-Gilbert ZW, Kramer A, Dunford JE, Howell S, Senbabaoglu F, Wells CI, Havener T, Smith JL, Hossain MA, Oppermann U, Drewry DH, Axtman AD. Discovery of a potent and selective naphthyridine-based chemical probe for casein kinase 2. ChemRxiv : the preprint server for chemistry. 2022. doi: 10.26434/chemrxiv-2022-05jcz.
Leal K, Axtman AD, Betarbet R, Brennan PE, Carter GW, Frye SV, Fu H, Greenwood AK, Longo FM, Pearce KH, Edwards AE, Levey AI, Consortium T. The Emory-Sage-SGC TREAT-AD Center: Tool and probe development for emerging targets in Alzheimer’s Disease. The Emory-Sage-SGC TREAT-AD Center: Tool and probe development for emerging targets in Alzheimer’s Disease. 2022; 18:e064748. doi: 10.1002/alz.064748.
Axtman AD. Characterizing the role of the dark kinome in neurodegenerative disease - A mini review. Biochim Biophys Acta Gen Subj. 2021 Dec;1865(12):130014. doi: 10.1016/j.bbagen.2021.130014. Epub 2021 Sep 20. PubMed PMID: 34547390.
Potjewyd FM, Axtman AD. Exploration of Aberrant E3 Ligases Implicated in Alzheimer's Disease and Development of Chemical Tools to Modulate Their Function. Front Cell Neurosci. 2021;15:768655. doi: 10.3389/fncel.2021.768655. eCollection 2021. Review. PubMed PMID: 34867205; PubMed Central PMCID: PMC8637409.
Wells CI, Drewry DH, Pickett JE, Tjaden A, Krämer A, Müller S, Gyenis L, Menyhart D, Litchfield DW, Knapp S, Axtman AD. Development of a potent and selective chemical probe for the pleiotropic kinase CK2. Cell Chem Biol. 2021 Apr 15;28(4):546-558.e10. doi: 10.1016/j.chembiol.2020.12.013. Epub 2021 Jan 22. PubMed PMID: 33484635; PubMed Central PMCID: PMC8864761.
Drewry D, Annor-Gyamfi JK, Wells C, Pickett JE, Axtman A. Strategy for Lead Identification for Understudied Kinases. ChemRxiv : the preprint server for chemistry. 2021 March. doi: 10.26434/chemrxiv.14195207.v1.
Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, Michaelides M, Mills CE, Müller S, Owen D, Picado A, Saikatendu KS, Schröder M, Stolz A, Tellechea M, Turunen BJ, Vilar S, Wang J, Zuercher WJ, Willson TM, Drewry DH. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. Int J Mol Sci. 2021 Jan 8;22(2). doi: 10.3390/ijms22020566. PubMed PMID: 33429995; PubMed Central PMCID: PMC7826789.
Wang CB, Lorente-Macías Á, Wells C, Pickett JE, Picado A, Zuercher WJ, Axtman AD. Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series. RSC Med Chem. 2021 Jan 1;12(1):129-136. doi: 10.1039/d0md00292e. eCollection 2021 Jan 1. PubMed PMID: 34046605; PubMed Central PMCID: PMC8130602.
Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SK, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH, Richardson T, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD. AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery. BioRxiv. 2021. doi: 10.1101/2021.07.22.453404v1.
Agajanian MJ, Potjewyd FM, Bowman BM, Solomon S, LaPak KM, Bhatt DP, Smith J, Goldfarb D, Axtman AD, Major MB. Protein proximity networks and functional evaluation of the Casein Kinase 1 γ family reveals unique roles for CK1γ3 in WNT signaling. bioRxiv : the preprint server for biology. 2021. doi: 10.1101/2021.11.30.470617.
Tamir TY, Drewry DH, Wells C, Major MB, Axtman AD. PKIS deep dive yields a chemical starting point for dark kinases and a cell active BRSK2 inhibitor. Sci Rep. 2020 Sep 28;10(1):15826. doi: 10.1038/s41598-020-72869-9. PubMed PMID: 32985588; PubMed Central PMCID: PMC7522982.
Lindsley CW, Axtman AD. NeuroChat with Research Assistant Professor Alison Axtman. ACS Chem Neurosci. 2020 Sep 16;11(18):2783-2785. doi: 10.1021/acschemneuro.0c00548. PubMed PMID: 32933260.
Wang CB, Lorente-Macías Á, Wells C, Pickett JE, Picado A, Zuercher WJ, Axtman AD. Towards a RIOK2 chemical probe: Cellular potency improvement of a selective 2-(acylamino)pyridine series. ChemRxiv : the preprint server for chemistry. 2020 August. doi: 10.26434/chemrxiv.12805271.
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