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Results: 1 to 20 of 89

1.

A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases.

Feng Y, Chambers JW, Iqbal S, Koenig M, Park H, Cherry L, Hernandez P, Figuera-Losada M, LoGrasso PV.

ACS Chem Biol. 2013 Aug 16;8(8):1747-54. doi: 10.1021/cb3006165. Epub 2013 Jun 10.

PMID:
23751758
[PubMed - indexed for MEDLINE]
Free PMC Article
2.

Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein.

Yun H, Heo HY, Kim HH, DooKim N, Seol W.

Bioorg Med Chem Lett. 2011 May 15;21(10):2953-7. doi: 10.1016/j.bmcl.2011.03.061. Epub 2011 Mar 21.

PMID:
21474311
[PubMed - indexed for MEDLINE]
3.

Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).

Rosenthal AS, Tanega C, Shen M, Mott BT, Bougie JM, Nguyen DT, Misteli T, Auld DS, Maloney DJ, Thomas CJ.

Bioorg Med Chem Lett. 2011 May 15;21(10):3152-8. doi: 10.1016/j.bmcl.2011.02.114. Epub 2011 Mar 4.

PMID:
21450467
[PubMed - indexed for MEDLINE]
Free PMC Article
4.

(G2019S) LRRK2 activates MKK4-JNK pathway and causes degeneration of SN dopaminergic neurons in a transgenic mouse model of PD.

Chen CY, Weng YH, Chien KY, Lin KJ, Yeh TH, Cheng YP, Lu CS, Wang HL.

Cell Death Differ. 2012 Oct;19(10):1623-33. doi: 10.1038/cdd.2012.42. Epub 2012 Apr 27.

PMID:
22539006
[PubMed - indexed for MEDLINE]
Free PMC Article
5.

Type II kinase inhibitors show an unexpected inhibition mode against Parkinson's disease-linked LRRK2 mutant G2019S.

Liu M, Bender SA, Cuny GD, Sherman W, Glicksman M, Ray SS.

Biochemistry. 2013 Mar 12;52(10):1725-36. doi: 10.1021/bi3012077. Epub 2013 Mar 1.

PMID:
23379419
[PubMed - indexed for MEDLINE]
Free PMC Article
6.

Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.

Erlanson DA, Arndt JW, Cancilla MT, Cao K, Elling RA, English N, Friedman J, Hansen SK, Hession C, Joseph I, Kumaravel G, Lee WC, Lind KE, McDowell RS, Miatkowski K, Nguyen C, Nguyen TB, Park S, Pathan N, Penny DM, Romanowski MJ, Scott D, Silvian L, Simmons RL, Tangonan BT, Yang W, Sun L.

Bioorg Med Chem Lett. 2011 May 15;21(10):3078-83. doi: 10.1016/j.bmcl.2011.03.032. Epub 2011 Mar 17.

PMID:
21459573
[PubMed - indexed for MEDLINE]
7.

Inhibition of excessive mitochondrial fission reduced aberrant autophagy and neuronal damage caused by LRRK2 G2019S mutation.

Su YC, Qi X.

Hum Mol Genet. 2013 Nov 15;22(22):4545-61. doi: 10.1093/hmg/ddt301. Epub 2013 Jun 27.

PMID:
23813973
[PubMed - indexed for MEDLINE]
Free Article
8.

Substituting c-Jun N-terminal kinase-3 (JNK3) ATP-binding site amino acid residues with their p38 counterparts affects binding of JNK- and p38-selective inhibitors.

Fricker M, Lograsso P, Ellis S, Wilkie N, Hunt P, Pollack SJ.

Arch Biochem Biophys. 2005 Jun 15;438(2):195-205.

PMID:
15907786
[PubMed - indexed for MEDLINE]
9.

Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease.

Nichols RJ, Dzamko N, Hutti JE, Cantley LC, Deak M, Moran J, Bamborough P, Reith AD, Alessi DR.

Biochem J. 2009 Oct 23;424(1):47-60. doi: 10.1042/BJ20091035.

PMID:
19740074
[PubMed - indexed for MEDLINE]
Free PMC Article
10.

ATP-competitive LRRK2 inhibitors interfere with monoclonal antibody binding to the kinase domain of LRRK2 under native conditions. A method to directly monitor the active conformation of LRRK2?

Gillardon F, Kremmer E, Froehlich T, Ueffing M, Hengerer B, Gloeckner CJ.

J Neurosci Methods. 2013 Mar 30;214(1):62-8. doi: 10.1016/j.jneumeth.2012.12.015. Epub 2013 Jan 12.

PMID:
23318290
[PubMed - indexed for MEDLINE]
11.

Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.

Troxler T, Greenidge P, Zimmermann K, Desrayaud S, Drückes P, Schweizer T, Stauffer D, Rovelli G, Shimshek DR.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4085-90. doi: 10.1016/j.bmcl.2013.05.054. Epub 2013 May 24.

PMID:
23768909
[PubMed - indexed for MEDLINE]
12.

Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.

Chen H, Chan BK, Drummond J, Estrada AA, Gunzner-Toste J, Liu X, Liu Y, Moffat J, Shore D, Sweeney ZK, Tran T, Wang S, Zhao G, Zhu H, Burdick DJ.

J Med Chem. 2012 Jun 14;55(11):5536-45. doi: 10.1021/jm300452p. Epub 2012 Jun 1.

PMID:
22591441
[PubMed - indexed for MEDLINE]
13.

Inhibition of LRRK2 kinase activity leads to dephosphorylation of Ser(910)/Ser(935), disruption of 14-3-3 binding and altered cytoplasmic localization.

Dzamko N, Deak M, Hentati F, Reith AD, Prescott AR, Alessi DR, Nichols RJ.

Biochem J. 2010 Sep 15;430(3):405-13. doi: 10.1042/BJ20100784.

PMID:
20659021
[PubMed - indexed for MEDLINE]
Free PMC Article
14.

LRRK2 enhances oxidative stress-induced neurotoxicity via its kinase activity.

Heo HY, Park JM, Kim CH, Han BS, Kim KS, Seol W.

Exp Cell Res. 2010 Feb 15;316(4):649-56. doi: 10.1016/j.yexcr.2009.09.014. Epub 2009 Sep 19.

PMID:
19769964
[PubMed - indexed for MEDLINE]
15.

Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

Zhang J, Deng X, Choi HG, Alessi DR, Gray NS.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1864-9. doi: 10.1016/j.bmcl.2012.01.084. Epub 2012 Jan 28.

PMID:
22335897
[PubMed - indexed for MEDLINE]
Free PMC Article
16.

Inhibitors of LRRK2 kinase attenuate neurodegeneration and Parkinson-like phenotypes in Caenorhabditis elegans and Drosophila Parkinson's disease models.

Liu Z, Hamamichi S, Lee BD, Yang D, Ray A, Caldwell GA, Caldwell KA, Dawson TM, Smith WW, Dawson VL.

Hum Mol Genet. 2011 Oct 15;20(20):3933-42. doi: 10.1093/hmg/ddr312. Epub 2011 Jul 18.

PMID:
21768216
[PubMed - indexed for MEDLINE]
Free PMC Article
17.

Small molecule kinase inhibitors for LRRK2 and their application to Parkinson's disease models.

Kramer T, Lo Monte F, Göring S, Okala Amombo GM, Schmidt B.

ACS Chem Neurosci. 2012 Mar 21;3(3):151-60. doi: 10.1021/cn200117j. Epub 2012 Jan 18. Review.

PMID:
22860184
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

Unique functional and structural properties of the LRRK2 protein ATP-binding pocket.

Liu Z, Galemmo RA Jr, Fraser KB, Moehle MS, Sen S, Volpicelli-Daley LA, DeLucas LJ, Ross LJ, Valiyaveettil J, Moukha-Chafiq O, Pathak AK, Ananthan S, Kezar H, White EL, Gupta V, Maddry JA, Suto MJ, West AB.

J Biol Chem. 2014 Nov 21;289(47):32937-51. doi: 10.1074/jbc.M114.602318. Epub 2014 Sep 16.

PMID:
25228699
[PubMed - in process]
19.

De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.

Urich R, Wishart G, Kiczun M, Richters A, Tidten-Luksch N, Rauh D, Sherborne B, Wyatt PG, Brenk R.

ACS Chem Biol. 2013 May 17;8(5):1044-52. doi: 10.1021/cb300729y. Epub 2013 Mar 27.

PMID:
23534475
[PubMed - indexed for MEDLINE]
Free PMC Article
20.

Leucine-rich repeat kinase 2 mutants I2020T and G2019S exhibit altered kinase inhibitor sensitivity.

Reichling LJ, Riddle SM.

Biochem Biophys Res Commun. 2009 Jun 26;384(2):255-8. doi: 10.1016/j.bbrc.2009.04.098. Epub 2009 May 3.

PMID:
19397894
[PubMed - indexed for MEDLINE]

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