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Items: 1 to 50 of 99

1.

Parallel signaling through IRE1α and PERK regulates pancreatic neuroendocrine tumor growth and survival.

Moore PC, Qi JY, Thamsen M, Ghosh R, Peng J, Gliedt MJ, Meza-Acevedo R, Warren RE, Hiniker A, Kim GE, Maly DJ, Backes BJ, Papa FR, Oakes SA.

Cancer Res. 2019 Oct 31. pii: canres.1116.2019. doi: 10.1158/0008-5472.CAN-19-1116. [Epub ahead of print]

PMID:
31672843
2.

Development of a Chemical Toolset for Studying the Paralog-Specific Function of IRE1.

Feldman HC, Vidadala VN, Potter ZE, Papa FR, Backes BJ, Maly DJ.

ACS Chem Biol. 2019 Oct 14. doi: 10.1021/acschembio.9b00482. [Epub ahead of print]

PMID:
31609569
3.

Multi-input chemical control of protein dimerization for programming graded cellular responses.

Foight GW, Wang Z, Wei CT, Jr Greisen P, Warner KM, Cunningham-Bryant D, Park K, Brunette TJ, Sheffler W, Baker D, Maly DJ.

Nat Biotechnol. 2019 Oct;37(10):1209-1216. doi: 10.1038/s41587-019-0242-8. Epub 2019 Sep 9.

PMID:
31501561
4.

Chemoproteomic Method for Profiling Inhibitor-Bound Kinase Complexes.

Fang L, Chakraborty S, Dieter EM, Potter ZE, Lombard CK, Maly DJ.

J Am Chem Soc. 2019 Jul 31;141(30):11912-11922. doi: 10.1021/jacs.9b02963. Epub 2019 Jul 5.

PMID:
31274292
5.

P-Glycoprotein-Mediated Efflux Reduces the In Vivo Efficacy of a Therapeutic Targeting the Gastrointestinal Parasite Cryptosporidium.

Arnold SLM, Choi R, Hulverson MA, Whitman GR, Mccloskey MC, Dorr CS, Vidadala RSR, Khatod M, Morada M, Barrett LK, Maly DJ, Yarlett N, Van Voorhis WC.

J Infect Dis. 2019 Aug 30;220(7):1188-1198. doi: 10.1093/infdis/jiz269.

6.

Targeting Dynamic ATP-Binding Site Features Allows Discrimination between Highly Homologous Protein Kinases.

Chakraborty S, Inukai T, Fang L, Golkowski M, Maly DJ.

ACS Chem Biol. 2019 Jun 21;14(6):1249-1259. doi: 10.1021/acschembio.9b00214. Epub 2019 May 13.

PMID:
31038916
7.

Bumped kinase inhibitor 1369 is effective against Cystoisospora suis in vivo and in vitro.

Shrestha A, Ojo KK, Koston F, Ruttkowski B, Vidadala RSR, Dorr CS, Navaluna ED, Whitman GR, Barrett KF, Barrett LK, Hulverson MA, Choi R, Michaels SA, Maly DJ, Hemphill A, Van Voorhis WC, Joachim A.

Int J Parasitol Drugs Drug Resist. 2019 Aug;10:9-19. doi: 10.1016/j.ijpddr.2019.03.004. Epub 2019 Apr 2.

8.

A Combined Approach Reveals a Regulatory Mechanism Coupling Src's Kinase Activity, Localization, and Phosphotransferase-Independent Functions.

Ahler E, Register AC, Chakraborty S, Fang L, Dieter EM, Sitko KA, Vidadala RSR, Trevillian BM, Golkowski M, Gelman H, Stephany JJ, Rubin AF, Merritt EA, Fowler DM, Maly DJ.

Mol Cell. 2019 Apr 18;74(2):393-408.e20. doi: 10.1016/j.molcel.2019.02.003. Epub 2019 Apr 4.

PMID:
30956043
9.

A Chemically Disrupted Proximity System for Controlling Dynamic Cellular Processes.

Cunningham-Bryant D, Dieter EM, Foight GW, Rose JC, Loutey DE, Maly DJ.

J Am Chem Soc. 2019 Feb 27;141(8):3352-3355. doi: 10.1021/jacs.8b12382. Epub 2019 Feb 14.

PMID:
30735038
10.

Small molecule inhibition of IRE1α kinase/RNase has anti-fibrotic effects in the lung.

Thamsen M, Ghosh R, Auyeung VC, Brumwell A, Chapman HA, Backes BJ, Perara G, Maly DJ, Sheppard D, Papa FR.

PLoS One. 2019 Jan 9;14(1):e0209824. doi: 10.1371/journal.pone.0209824. eCollection 2019.

11.

Pharmacokinetics and In Vivo Efficacy of Pyrazolopyrimidine, Pyrrolopyrimidine, and 5-Aminopyrazole-4-Carboxamide Bumped Kinase Inhibitors against Toxoplasmosis.

Hulverson MA, Bruzual I, McConnell EV, Huang W, Vidadala RSR, Choi R, Arnold SLM, Whitman GR, McCloskey MC, Barrett LK, Rivas KL, Scheele S, DeRocher AE, Parsons M, Ojo KK, Maly DJ, Fan E, Van Voorhis WC, Doggett JS.

J Infect Dis. 2019 Apr 16;219(9):1464-1473. doi: 10.1093/infdis/jiy664.

PMID:
30423128
12.

Allosteric Modulation of JNK Docking Site Interactions with ATP-Competitive Inhibitors.

Lombard CK, Davis AL, Inukai T, Maly DJ.

Biochemistry. 2018 Oct 9;57(40):5897-5909. doi: 10.1021/acs.biochem.8b00776. Epub 2018 Sep 25.

13.

Kinome chemoproteomics characterization of pyrrolo[3,4-c]pyrazoles as potent and selective inhibitors of glycogen synthase kinase 3.

Golkowski M, Perera GK, Vidadala VN, Ojo KK, Van Voorhis WC, Maly DJ, Ong SE.

Mol Omics. 2018 Feb 12;14(1):26-36. doi: 10.1039/c7mo00006e.

14.

"Examining RAS pathway rewiring with a chemically inducible activator of RAS".

Rose JC, Dieter EM, Cunningham-Bryant D, Maly DJ.

Small GTPases. 2018 Apr 10:1-8. doi: 10.1080/21541248.2018.1446697. [Epub ahead of print]

PMID:
29634387
15.

Toxoplasma Calcium-Dependent Protein Kinase 1 Inhibitors: Probing Activity and Resistance Using Cellular Thermal Shift Assays.

Scheele S, Geiger JA, DeRocher AE, Choi R, Smith TR, Hulverson MA, Vidadala RSR, Barrett LK, Maly DJ, Merritt EA, Ojo KK, Van Voorhis WC, Parsons M.

Antimicrob Agents Chemother. 2018 May 25;62(6). pii: e00051-18. doi: 10.1128/AAC.00051-18. Print 2018 Jun.

16.

7 H-Pyrrolo[2,3- d]pyrimidin-4-amine-Based Inhibitors of Calcium-Dependent Protein Kinase 1 Have Distinct Inhibitory and Oral Pharmacokinetic Characteristics Compared with 1 H-Pyrazolo[3,4- d]pyrimidin-4-amine-Based Inhibitors.

Vidadala RSR, Golkowski M, Hulverson MA, Choi R, McCloskey MC, Whitman GR, Huang W, Arnold SLM, Barrett LK, Fan E, Merritt EA, Van Voorhis WC, Ojo KK, Maly DJ.

ACS Infect Dis. 2018 Apr 13;4(4):516-522. doi: 10.1021/acsinfecdis.7b00224. Epub 2018 Mar 16.

17.

In vitro growth inhibition of Theileria equi by bumped kinase inhibitors.

Gimenez F, Hines SA, Evanoff R, Ojo KK, Van Voorhis WC, Maly DJ, Vidadala RSR, Mealey RH.

Vet Parasitol. 2018 Feb 15;251:90-94. doi: 10.1016/j.vetpar.2017.12.024. Epub 2018 Jan 1.

18.

In vitro efficacy of bumped kinase inhibitors against Besnoitia besnoiti tachyzoites.

Jiménez-Meléndez A, Ojo KK, Wallace AM, Smith TR, Hemphill A, Balmer V, Regidor-Cerrillo J, Ortega-Mora LM, Hehl AB, Fan E, Maly DJ, Van Voorhis WC, Álvarez-García G.

Int J Parasitol. 2017 Oct;47(12):811-821. doi: 10.1016/j.ijpara.2017.08.005. Epub 2017 Sep 9.

PMID:
28899692
19.

Advances in bumped kinase inhibitors for human and animal therapy for cryptosporidiosis.

Hulverson MA, Choi R, Arnold SLM, Schaefer DA, Hemphill A, McCloskey MC, Betzer DP, Müller J, Vidadala RSR, Whitman GR, Rivas KL, Barrett LK, Hackman RC, Love MS, McNamara CW, Shaughnessy TK, Kondratiuk A, Kurnick M, Banfor PN, Lynch JJ, Freiberg GM, Kempf DJ, Maly DJ, Riggs MW, Ojo KK, Van Voorhis WC.

Int J Parasitol. 2017 Oct;47(12):753-763. doi: 10.1016/j.ijpara.2017.08.006. Epub 2017 Sep 9.

20.

Rheostatic Control of Cas9-Mediated DNA Double Strand Break (DSB) Generation and Genome Editing.

Rose JC, Stephany JJ, Wei CT, Fowler DM, Maly DJ.

ACS Chem Biol. 2018 Feb 16;13(2):438-442. doi: 10.1021/acschembio.7b00652. Epub 2017 Sep 15.

21.

Rapidly inducible Cas9 and DSB-ddPCR to probe editing kinetics.

Rose JC, Stephany JJ, Valente WJ, Trevillian BM, Dang HV, Bielas JH, Maly DJ, Fowler DM.

Nat Methods. 2017 Sep;14(9):891-896. doi: 10.1038/nmeth.4368. Epub 2017 Jul 24.

22.

Proteomic Profiling of Protein Kinase Inhibitor Targets by Mass Spectrometry.

Golkowski M, Maly DJ, Ong SE.

Methods Mol Biol. 2017;1636:105-117. doi: 10.1007/978-1-4939-7154-1_8.

PMID:
28730476
23.

Allosteric Modulation of Src Family Kinases with ATP-Competitive Inhibitors.

Register AC, Chakraborty S, Maly DJ.

Methods Mol Biol. 2017;1636:79-89. doi: 10.1007/978-1-4939-7154-1_6.

PMID:
28730474
24.

Necessity of Bumped Kinase Inhibitor Gastrointestinal Exposure in Treating Cryptosporidium Infection.

Arnold SLM, Choi R, Hulverson MA, Schaefer DA, Vinayak S, Vidadala RSR, McCloskey MC, Whitman GR, Huang W, Barrett LK, Ojo KK, Fan E, Maly DJ, Riggs MW, Striepen B, Van Voorhis WC.

J Infect Dis. 2017 Jul 1;216(1):55-63. doi: 10.1093/infdis/jix247.

25.

5-Aminopyrazole-4-Carboxamide-Based Compounds Prevent the Growth of Cryptosporidium parvum.

Huang W, Choi R, Hulverson MA, Zhang Z, McCloskey MC, Schaefer DA, Whitman GR, Barrett LK, Vidadala RSR, Riggs MW, Maly DJ, Van Voorhis WC, Ojo KK, Fan E.

Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00020-17. doi: 10.1128/AAC.00020-17. Print 2017 Aug.

26.

Development of a murine vertical transmission model for Toxoplasma gondii oocyst infection and studies on the efficacy of bumped kinase inhibitor (BKI)-1294 and the naphthoquinone buparvaquone against congenital toxoplasmosis.

Müller J, Aguado-Martínez A, Ortega-Mora LM, Moreno-Gonzalo J, Ferre I, Hulverson MA, Choi R, McCloskey MC, Barrett LK, Maly DJ, Ojo KK, Van Voorhis W, Hemphill A.

J Antimicrob Chemother. 2017 Aug 1;72(8):2334-2341. doi: 10.1093/jac/dkx134.

27.

Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes.

Morita S, Villalta SA, Feldman HC, Register AC, Rosenthal W, Hoffmann-Petersen IT, Mehdizadeh M, Ghosh R, Wang L, Colon-Negron K, Meza-Acevedo R, Backes BJ, Maly DJ, Bluestone JA, Papa FR.

Cell Metab. 2017 May 2;25(5):1207. doi: 10.1016/j.cmet.2017.04.026. No abstract available.

28.

Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes.

Morita S, Villalta SA, Feldman HC, Register AC, Rosenthal W, Hoffmann-Petersen IT, Mehdizadeh M, Ghosh R, Wang L, Colon-Negron K, Meza-Acevedo R, Backes BJ, Maly DJ, Bluestone JA, Papa FR.

Cell Metab. 2017 Apr 4;25(4):883-897.e8. doi: 10.1016/j.cmet.2017.03.018. Erratum in: Cell Metab. 2017 May 2;25(5):1207.

29.

Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.

Hulverson MA, Vinayak S, Choi R, Schaefer DA, Castellanos-Gonzalez A, Vidadala RSR, Brooks CF, Herbert GT, Betzer DP, Whitman GR, Sparks HN, Arnold SLM, Rivas KL, Barrett LK, White AC Jr, Maly DJ, Riggs MW, Striepen B, Van Voorhis WC, Ojo KK.

J Infect Dis. 2017 Apr 15;215(8):1275-1284. doi: 10.1093/infdis/jix120. Erratum in: J Infect Dis. 2018 Jan 4;217(2):340.

30.

Two Novel Calcium-Dependent Protein Kinase 1 Inhibitors Interfere with Vertical Transmission in Mice Infected with Neospora caninum Tachyzoites.

Müller J, Aguado-Martínez A, Balmer V, Maly DJ, Fan E, Ortega-Mora LM, Ojo KK, Van Voorhis WC, Hemphill A.

Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: e02324-16. doi: 10.1128/AAC.02324-16. Print 2017 Apr.

31.

Kinobead and Single-Shot LC-MS Profiling Identifies Selective PKD Inhibitors.

Golkowski M, Vidadala RS, Lombard CK, Suh HW, Maly DJ, Ong SE.

J Proteome Res. 2017 Mar 3;16(3):1216-1227. doi: 10.1021/acs.jproteome.6b00817. Epub 2017 Feb 3.

32.

Extended-spectrum antiprotozoal bumped kinase inhibitors: A review.

Van Voorhis WC, Doggett JS, Parsons M, Hulverson MA, Choi R, Arnold SLM, Riggs MW, Hemphill A, Howe DK, Mealey RH, Lau AOT, Merritt EA, Maly DJ, Fan E, Ojo KK.

Exp Parasitol. 2017 Sep;180:71-83. doi: 10.1016/j.exppara.2017.01.001. Epub 2017 Jan 5. Review.

33.

Novel Bumped Kinase Inhibitors Are Safe and Effective Therapeutics in the Calf Clinical Model for Cryptosporidiosis.

Schaefer DA, Betzer DP, Smith KD, Millman ZG, Michalski HC, Menchaca SE, Zambriski JA, Ojo KK, Hulverson MA, Arnold SL, Rivas KL, Vidadala RS, Huang W, Barrett LK, Maly DJ, Fan E, Van Voorhis WC, Riggs MW.

J Infect Dis. 2016 Dec 15;214(12):1856-1864. Epub 2016 Oct 17.

34.

Reduced Activity of Mutant Calcium-Dependent Protein Kinase 1 Is Compensated in Plasmodium falciparum through the Action of Protein Kinase G.

Bansal A, Ojo KK, Mu J, Maly DJ, Van Voorhis WC, Miller LH.

MBio. 2016 Dec 6;7(6). pii: e02011-16. doi: 10.1128/mBio.02011-16.

35.

A computationally engineered RAS rheostat reveals RAS-ERK signaling dynamics.

Rose JC, Huang PS, Camp ND, Ye J, Leidal AM, Goreshnik I, Trevillian BM, Dickinson MS, Cunningham-Bryant D, Debnath J, Baker D, Wolf-Yadlin A, Maly DJ.

Nat Chem Biol. 2017 Jan;13(1):119-126. doi: 10.1038/nchembio.2244. Epub 2016 Nov 21.

36.

Profiling the Dual Enzymatic Activities of the Serine/Threonine Kinase IRE1α.

Feldman HC, Maly DJ.

Methods Mol Biol. 2017;1513:233-242.

PMID:
27807842
37.

5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.

Huang W, Hulverson MA, Zhang Z, Choi R, Hart KJ, Kennedy M, Vidadala RSR, Maly DJ, Van Voorhis WC, Lindner SE, Fan E, Ojo KK.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5487-5491. doi: 10.1016/j.bmcl.2016.10.014. Epub 2016 Oct 10.

38.

Selective inhibition of Sarcocystis neurona calcium-dependent protein kinase 1 for equine protozoal myeloencephalitis therapy.

Ojo KK, Dangoudoubiyam S, Verma SK, Scheele S, DeRocher AE, Yeargan M, Choi R, Smith TR, Rivas KL, Hulverson MA, Barrett LK, Fan E, Maly DJ, Parsons M, Dubey JP, Howe DK, Van Voorhis WC.

Int J Parasitol. 2016 Dec;46(13-14):871-880. doi: 10.1016/j.ijpara.2016.08.003. Epub 2016 Oct 8.

39.

Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis.

Vidadala RS, Rivas KL, Ojo KK, Hulverson MA, Zambriski JA, Bruzual I, Schultz TL, Huang W, Zhang Z, Scheele S, DeRocher AE, Choi R, Barrett LK, Siddaramaiah LK, Hol WG, Fan E, Merritt EA, Parsons M, Freiberg G, Marsh K, Kempf DJ, Carruthers VB, Isoherranen N, Doggett JS, Van Voorhis WC, Maly DJ.

J Med Chem. 2016 Jul 14;59(13):6531-46. doi: 10.1021/acs.jmedchem.6b00760. Epub 2016 Jul 1.

40.

Structural and Functional Analysis of the Allosteric Inhibition of IRE1α with ATP-Competitive Ligands.

Feldman HC, Tong M, Wang L, Meza-Acevedo R, Gobillot TA, Lebedev I, Gliedt MJ, Hari SB, Mitra AK, Backes BJ, Papa FR, Seeliger MA, Maly DJ.

ACS Chem Biol. 2016 Aug 19;11(8):2195-205. doi: 10.1021/acschembio.5b00940. Epub 2016 Jun 9.

41.

A novel protein kinase is essential in bloodstream Trypanosoma brucei.

Jensen BC, Booster N, Vidadala RS, Maly DJ, Parsons M.

Int J Parasitol. 2016 Jul;46(8):479-83. doi: 10.1016/j.ijpara.2016.03.001. Epub 2016 Mar 23.

42.

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.

Crowther GJ, Hillesland HK, Keyloun KR, Reid MC, Lafuente-Monasterio MJ, Ghidelli-Disse S, Leonard SE, He P, Jones JC, Krahn MM, Mo JS, Dasari KS, Fox AM, Boesche M, El Bakkouri M, Rivas KL, Leroy D, Hui R, Drewes G, Maly DJ, Van Voorhis WC, Ojo KK.

PLoS One. 2016 Mar 2;11(3):e0149996. doi: 10.1371/journal.pone.0149996. eCollection 2016.

43.

Bumped kinase inhibitor prohibits egression in Babesia bovis.

Pedroni MJ, Vidadala RS, Choi R, Keyloun KR, Reid MC, Murphy RC, Barrett LK, Van Voorhis WC, Maly DJ, Ojo KK, Lau AO.

Vet Parasitol. 2016 Jan 15;215:22-8. doi: 10.1016/j.vetpar.2015.10.023. Epub 2015 Nov 5.

44.

SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.

Huang W, Ojo KK, Zhang Z, Rivas K, Vidadala RS, Scheele S, DeRocher AE, Choi R, Hulverson MA, Barrett LK, Bruzual I, Siddaramaiah LK, Kerchner KM, Kurnick MD, Freiberg GM, Kempf D, Hol WG, Merritt EA, Neckermann G, de Hostos EL, Isoherranen N, Maly DJ, Parsons M, Doggett JS, Van Voorhis WC, Fan E.

ACS Med Chem Lett. 2015 Oct 22;6(12):1184-1189. eCollection 2015 Dec 10.

45.

Conversion of a Single Polypharmacological Agent into Selective Bivalent Inhibitors of Intracellular Kinase Activity.

Gower CM, Thomas JR, Harrington E, Murphy J, Chang ME, Cornella-Taracido I, Jain RK, Schirle M, Maly DJ.

ACS Chem Biol. 2016 Jan 15;11(1):121-31. doi: 10.1021/acschembio.5b00847. Epub 2015 Nov 6.

46.

In Vitro and In Vivo Effects of the Bumped Kinase Inhibitor 1294 in the Related Cyst-Forming Apicomplexans Toxoplasma gondii and Neospora caninum.

Winzer P, Müller J, Aguado-Martínez A, Rahman M, Balmer V, Manser V, Ortega-Mora LM, Ojo KK, Fan E, Maly DJ, Van Voorhis WC, Hemphill A.

Antimicrob Agents Chemother. 2015 Oct;59(10):6361-74. doi: 10.1128/AAC.01236-15. Epub 2015 Jul 27.

47.

Radiotherapy followed by aurora kinase inhibition targets tumor-propagating cells in human glioblastoma.

Li N, Maly DJ, Chanthery YH, Sirkis DW, Nakamura JL, Berger MS, James CD, Shokat KM, Weiss WA, Persson AI.

Mol Cancer Ther. 2015 Feb;14(2):419-28. doi: 10.1158/1535-7163.MCT-14-0526. Epub 2014 Dec 18.

48.

Druggable sensors of the unfolded protein response.

Maly DJ, Papa FR.

Nat Chem Biol. 2014 Nov;10(11):892-901. doi: 10.1038/nchembio.1664. Review.

49.

SH2-catalytic domain linker heterogeneity influences allosteric coupling across the SFK family.

Register AC, Leonard SE, Maly DJ.

Biochemistry. 2014 Nov 11;53(44):6910-23. doi: 10.1021/bi5008194. Epub 2014 Oct 29.

50.

Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress.

Ghosh R, Wang L, Wang ES, Perera BG, Igbaria A, Morita S, Prado K, Thamsen M, Caswell D, Macias H, Weiberth KF, Gliedt MJ, Alavi MV, Hari SB, Mitra AK, Bhhatarai B, Schürer SC, Snapp EL, Gould DB, German MS, Backes BJ, Maly DJ, Oakes SA, Papa FR.

Cell. 2014 Jul 31;158(3):534-48. doi: 10.1016/j.cell.2014.07.002. Epub 2014 Jul 10.

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