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Items: 24


Beyond Traditional Structure-Based Drug Design: The Role of Iron Complexation, Strain, and Water in the Binding of Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylase 2.

Bembenek SD, Venkatesan H, Peltier HM, Rosen MD, Barrett TD, Kanelakis KC, Palomino HL, Brondstetter TI, Mirzadegan T, Rabinowitz MH.

ACS Omega. 2019 Apr 30;4(4):6703-6708. doi: 10.1021/acsomega.9b00199. Epub 2019 Apr 12.


Prolyl hydroxylase inhibition corrects functional iron deficiency and inflammation-induced anaemia in rats.

Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Yan W, Merton KP, Schoetens F, Ma JY, Skaptason J, Gao J, Tran DT, Venkatesan H, Rosen MD, Shankley NP, Rabinowitz MH.

Br J Pharmacol. 2015 Aug;172(16):4078-88. doi: 10.1111/bph.13188. Epub 2015 Jun 26.


Regulation of G protein signaling by the 70kDa heat shock protein.

Lim WK, Kanelakis KC, Neubig RR.

Cell Signal. 2013 Feb;25(2):389-96. doi: 10.1016/j.cellsig.2012.11.002. Epub 2012 Nov 12.


Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor.

Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Haug PV, Yan W, Young A, Hua H, Hart JC, Tran DT, Venkatesan H, Rosen MD, Peltier HM, Sepassi K, Rizzolio MC, Bembenek SD, Mirzadegan T, Rabinowitz MH, Shankley NP.

Mol Pharmacol. 2011 Jun;79(6):910-20. doi: 10.1124/mol.110.070508. Epub 2011 Mar 3.


Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.

Rosen MD, Venkatesan H, Peltier HM, Bembenek SD, Kanelakis KC, Zhao LX, Leonard BE, Hocutt FM, Wu X, Palomino HL, Brondstetter TI, Haugh PV, Cagnon L, Yan W, Liotta LA, Young A, Mirzadegan T, Shankley NP, Barrett TD, Rabinowitz MH.

ACS Med Chem Lett. 2010 Oct 5;1(9):526-9. doi: 10.1021/ml100198y. eCollection 2010 Dec 9.


Functional Characterization of the Canine Heme-Regulated eIF2alpha Kinase: Regulation of Protein Synthesis.

Kanelakis KC, Pyati J, Wagaman PC, Chuang JC, Yang Y, Shankley NP.

Adv Hematol. 2009;2009:251915. doi: 10.1155/2009/251915. Epub 2009 Jun 22.


Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase.

Rosen MD, Woods CR, Goldberg SD, Hack MD, Bounds AD, Yang Y, Wagaman PC, Phuong VK, Ameriks AP, Barrett TD, Kanelakis KC, Chuang JC, Shankley NP, Rabinowitz MH.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6548-51. doi: 10.1016/j.bmcl.2009.10.033. Epub 2009 Oct 13. Erratum in: Bioorg Med Chem Lett. 2010 Jun 15;20(12):3834. Chang, Jui [corrected to Chuang, Jui Chang].


Characterization of a robust enzymatic assay for inhibitors of 2-oxoglutarate-dependent hydroxylases.

Kanelakis KC, Palomino HL, Li L, Wu J, Yan W, Rosen MD, Rizzolio MC, Trivedi M, Morton MF, Yang Y, Venkatesan H, Rabinowitz MH, Shankley NP, Barrett TD.

J Biomol Screen. 2009 Jul;14(6):627-35. doi: 10.1177/1087057109333976. Epub 2009 Jun 4.


Molecular mechanism of activation and nuclear translocation of the mineralocorticoid receptor upon binding of pregnanesteroids.

Galigniana MD, Piwien Pilipuk G, Kanelakis KC, Burton G, Lantos CP.

Mol Cell Endocrinol. 2004 Mar 31;217(1-2):167-79. Review.


Regulation of glucocorticoid receptor ligand-binding activity by the hsp90/hsp70-based chaperone machinery.

Kanelakis KC, Pratt WB.

Methods Enzymol. 2003;364:159-73. No abstract available.


The hsp90 cochaperone p23 is the limiting component of the multiprotein hsp90/hsp70-based chaperone system in vivo where it acts to stabilize the client protein: hsp90 complex.

Morishima Y, Kanelakis KC, Murphy PJ, Lowe ER, Jenkins GJ, Osawa Y, Sunahara RK, Pratt WB.

J Biol Chem. 2003 Dec 5;278(49):48754-63. Epub 2003 Sep 24.


Characterization of a plant homolog of hop, a cochaperone of hsp90.

Zhang Z, Quick MK, Kanelakis KC, Gijzen M, Krishna P.

Plant Physiol. 2003 Feb;131(2):525-35.


Correlation between pregnanesteroid conformation, receptor affinity, and anti-natriuretic effect.

Piwien-Pilipuk G, Kanelakis KC, Galigniana MD.

Eur J Pharmacol. 2002 Nov 15;454(2-3):131-43.


hsp90 is required for heme binding and activation of apo-neuronal nitric-oxide synthase: geldanamycin-mediated oxidant generation is unrelated to any action of hsp90.

Billecke SS, Bender AT, Kanelakis KC, Murphy PJ, Lowe ER, Kamada Y, Pratt WB, Osawa Y.

J Biol Chem. 2002 Jun 7;277(23):20504-9. Epub 2002 Mar 28.


Stoichiometry, abundance, and functional significance of the hsp90/hsp70-based multiprotein chaperone machinery in reticulocyte lysate.

Murphy PJ, Kanelakis KC, Galigniana MD, Morishima Y, Pratt WB.

J Biol Chem. 2001 Aug 10;276(32):30092-8. Epub 2001 Jun 12.


hsp70 interacting protein Hip does not affect glucocorticoid receptor folding by the hsp90-based chaperone machinery except to oppose the effect of BAG-1.

Kanelakis KC, Murphy PJ, Galigniana MD, Morishima Y, Takayama S, Reed JC, Toft DO, Pratt WB.

Biochemistry. 2000 Nov 21;39(46):14314-21.


The Hsp organizer protein hop enhances the rate of but is not essential for glucocorticoid receptor folding by the multiprotein Hsp90-based chaperone system.

Morishima Y, Kanelakis KC, Silverstein AM, Dittmar KD, Estrada L, Pratt WB.

J Biol Chem. 2000 Mar 10;275(10):6894-900.


Tissue- and gender-specific expression of N-acetyltransferase 2 (Nat2*) during development of the outbred mouse strain CD-1.

Estrada L, Kanelakis KC, Levy GN, Weber WW.

Drug Metab Dispos. 2000 Feb;28(2):139-46.


Different regions of the immunophilin FKBP52 determine its association with the glucocorticoid receptor, hsp90, and cytoplasmic dynein.

Silverstein AM, Galigniana MD, Kanelakis KC, Radanyi C, Renoir JM, Pratt WB.

J Biol Chem. 1999 Dec 24;274(52):36980-6.


Differential effects of the hsp70-binding protein BAG-1 on glucocorticoid receptor folding by the hsp90-based chaperone machinery.

Kanelakis KC, Morishima Y, Dittmar KD, Galigniana MD, Takayama S, Reed JC, Pratt WB.

J Biol Chem. 1999 Nov 26;274(48):34134-40.


Neuronal nitric-oxide synthase is regulated by the Hsp90-based chaperone system in vivo.

Bender AT, Silverstein AM, Demady DR, Kanelakis KC, Noguchi S, Pratt WB, Osawa Y.

J Biol Chem. 1999 Jan 15;274(3):1472-8.

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