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Potential Tools for Eradicating HIV Reservoirs in the Brain: Development of Trojan Horse Prodrugs for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity.

Agrawal N, Rowe J, Lan J, Yu Q, Hrycyna CA, Chmielewski J.

J Med Chem. 2019 Sep 20. doi: 10.1021/acs.jmedchem.9b00779. [Epub ahead of print]


Methyltransferase-like 21c methylates and stabilizes the heat shock protein Hspa8 in type I myofibers in mice.

Wang C, Arrington J, Ratliff AC, Chen J, Horton HE, Nie Y, Yue F, Hrycyna CA, Tao WA, Kuang S.

J Biol Chem. 2019 Sep 13;294(37):13718-13728. doi: 10.1074/jbc.RA119.008430. Epub 2019 Jul 25.


Methyltransferase-like 21e inhibits 26S proteasome activity to facilitate hypertrophy of type IIb myofibers.

Wang C, Zhang B, Ratliff AC, Arrington J, Chen J, Xiong Y, Yue F, Nie Y, Hu K, Jin W, Tao WA, Hrycyna CA, Sun X, Kuang S.

FASEB J. 2019 Aug;33(8):9672-9684. doi: 10.1096/fj.201900582R. Epub 2019 Jun 4.


A Quantitative FRET Assay for the Upstream Cleavage Activity of the Integral Membrane Proteases Human ZMPSTE24 and Yeast Ste24.

Hsu ET, Vervacke JS, Distefano MD, Hrycyna CA.

Methods Mol Biol. 2019;2009:279-293. doi: 10.1007/978-1-4939-9532-5_21.


ZMPSTE24 missense mutations that cause progeroid diseases decrease prelamin A cleavage activity and/or protein stability.

Spear ED, Hsu ET, Nie L, Carpenter EP, Hrycyna CA, Michaelis S.

Dis Model Mech. 2018 Jul 13;11(7). pii: dmm033670. doi: 10.1242/dmm.033670.


a-Factor Analogues Containing Alkyne- and Azide-Functionalized Isoprenoids Are Efficiently Enzymatically Processed and Retain Wild-Type Bioactivity.

Diaz-Rodriguez V, Hsu ET, Ganusova E, Werst ER, Becker JM, Hrycyna CA, Distefano MD.

Bioconjug Chem. 2018 Feb 21;29(2):316-323. doi: 10.1021/acs.bioconjchem.7b00648. Epub 2017 Dec 20.


Dual inhibitors of the human blood-brain barrier drug efflux transporters P-glycoprotein and ABCG2 based on the antiviral azidothymidine.

Namanja-Magliano HA, Bohn K, Agrawal N, Willoughby ME, Hrycyna CA, Chmielewski J.

Bioorg Med Chem. 2017 Oct 1;25(19):5128-5132. doi: 10.1016/j.bmc.2017.07.001. Epub 2017 Jul 6.


Dual Modulation of Human P-Glycoprotein and ABCG2 with Prodrug Dimers of the Atypical Antipsychotic Agent Paliperidone in a Model of the Blood-Brain Barrier.

Bohn K, Lange A, Chmielewski J, Hrycyna CA.

Mol Pharm. 2017 Apr 3;14(4):1107-1119. doi: 10.1021/acs.molpharmaceut.6b01044. Epub 2017 Mar 21.


Non-Substrate Based, Small Molecule Inhibitors of the Human Isoprenylcysteine Carboxyl Methyltransferase.

Butler KV, Bohn K, Hrycyna CA, Jin J.

Medchemcomm. 2016 May 1;7(5):1016-1021. Epub 2016 Apr 14.


AIM2 inflammasome is activated by pharmacological disruption of nuclear envelope integrity.

Di Micco A, Frera G, Lugrin J, Jamilloux Y, Hsu ET, Tardivel A, De Gassart A, Zaffalon L, Bujisic B, Siegert S, Quadroni M, Broz P, Henry T, Hrycyna CA, Martinon F.

Proc Natl Acad Sci U S A. 2016 Aug 9;113(32):E4671-80. doi: 10.1073/pnas.1602419113. Epub 2016 Jul 26.


Diazirine-containing photoactivatable isoprenoid: synthesis and application in studies with isoprenylcysteine carboxyl methyltransferase.

Vervacke JS, Funk AL, Wang YC, Strom M, Hrycyna CA, Distefano MD.

J Org Chem. 2014 Mar 7;79(5):1971-8. doi: 10.1021/jo402600b. Epub 2014 Feb 20.


Reversible dimers of the atypical antipsychotic quetiapine inhibit p-glycoprotein-mediated efflux in vitro with increased binding affinity and in situ at the blood-brain barrier.

Emmert D, Campos CR, Ward D, Lu P, Namanja HA, Bohn K, Miller DS, Sharom FJ, Chmielewski J, Hrycyna CA.

ACS Chem Neurosci. 2014 Apr 16;5(4):305-17. doi: 10.1021/cn4002329. Epub 2014 Feb 7.


Quinine dimers are potent inhibitors of the Plasmodium falciparum chloroquine resistance transporter and are active against quinoline-resistant P. falciparum.

Hrycyna CA, Summers RL, Lehane AM, Pires MM, Namanja H, Bohn K, Kuriakose J, Ferdig M, Henrich PP, Fidock DA, Kirk K, Chmielewski J, Martin RE.

ACS Chem Biol. 2014 Mar 21;9(3):722-30. doi: 10.1021/cb4008953. Epub 2014 Jan 6.


Homodimers of the Antiviral Abacavir as Modulators of P-glycoprotein Transport in Cell Culture: Probing Tether Length.

Namanja HA, Emmert D, Hrycyna CA, Chmielewski J.

Medchemcomm. 2013 Oct;4(10). doi: 10.1039/C3MD00196B.


Competency-based reforms of the undergraduate biology curriculum: integrating the physical and biological sciences.

Thompson KV, Chmielewski J, Gaines MS, Hrycyna CA, LaCourse WR.

CBE Life Sci Educ. 2013 Jun 1;12(2):162-9. doi: 10.1187/cbe.12-09-0143.


Biochemistry. A protease for the ages.

Michaelis S, Hrycyna CA.

Science. 2013 Mar 29;339(6127):1529-30. doi: 10.1126/science.1236764. No abstract available.


S-Farnesyl-Thiopropionic Acid (FTPA) Triazoles as Potent Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase.

Bergman JA, Hahne K, Song J, Hrycyna CA, Gibbs RA.

ACS Med Chem Lett. 2012 Jan 12;3(1):15-19. Epub 2011 Nov 28.


Human ZMPSTE24 disease mutations: residual proteolytic activity correlates with disease severity.

Barrowman J, Wiley PA, Hudon-Miller SE, Hrycyna CA, Michaelis S.

Hum Mol Genet. 2012 Sep 15;21(18):4084-93. doi: 10.1093/hmg/dds233. Epub 2012 Jun 19.


Evaluation of substrate and inhibitor binding to yeast and human isoprenylcysteine carboxyl methyltransferases (Icmts) using biotinylated benzophenone-containing photoaffinity probes.

Hahne K, Vervacke JS, Shrestha L, Donelson JL, Gibbs RA, Distefano MD, Hrycyna CA.

Biochem Biophys Res Commun. 2012 Jun 22;423(1):98-103. doi: 10.1016/j.bbrc.2012.05.089. Epub 2012 May 23.


Click chemistry-derived bivalent quinine inhibitors of P-glycoprotein-mediated cellular efflux.

Kuriakose J, Hrycyna CA, Chmielewski J.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4410-2. doi: 10.1016/j.bmcl.2012.04.125. Epub 2012 May 4.


Inhibitors of protein geranylgeranyltransferase-I lead to prelamin A accumulation in cells by inhibiting ZMPSTE24.

Chang SY, Hudon-Miller SE, Yang SH, Jung HJ, Lee JM, Farber E, Subramanian T, Andres DA, Spielmann HP, Hrycyna CA, Young SG, Fong LG.

J Lipid Res. 2012 Jun;53(6):1176-82. doi: 10.1194/jlr.M026161. Epub 2012 Mar 23.


Amide-modified prenylcysteine based Icmt inhibitors: Structure-activity relationships, kinetic analysis and cellular characterization.

Majmudar JD, Hodges-Loaiza HB, Hahne K, Donelson JL, Song J, Shrestha L, Harrison ML, Hrycyna CA, Gibbs RA.

Bioorg Med Chem. 2012 Jan 1;20(1):283-95. doi: 10.1016/j.bmc.2011.10.087. Epub 2011 Nov 6.


Toward eradicating HIV reservoirs in the brain: inhibiting P-glycoprotein at the blood-brain barrier with prodrug abacavir dimers.

Namanja HA, Emmert D, Davis DA, Campos C, Miller DS, Hrycyna CA, Chmielewski J.

J Am Chem Soc. 2012 Feb 15;134(6):2976-80. doi: 10.1021/ja206867t. Epub 2011 Sep 9.


Lipid and sulfur substituted prenylcysteine analogs as human Icmt inhibitors.

Bergman JA, Hahne K, Hrycyna CA, Gibbs RA.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5616-9. doi: 10.1016/j.bmcl.2011.06.053. Epub 2011 Jun 21.


Recombinant synthesis of human ABCG2 expressed in the yeast Saccharomyces cerevisiae: an experimental methodological study.

Jacobs A, Emmert D, Wieschrath S, Hrycyna CA, Wiese M.

Protein J. 2011 Mar;30(3):201-11. doi: 10.1007/s10930-011-9321-5.


Probing the isoprenylcysteine carboxyl methyltransferase (Icmt) binding pocket: sulfonamide modified farnesyl cysteine (SMFC) analogs as Icmt inhibitors.

Majmudar JD, Hahne K, Hrycyna CA, Gibbs RA.

Bioorg Med Chem Lett. 2011 May 1;21(9):2616-20. doi: 10.1016/j.bmcl.2011.01.078. Epub 2011 Jan 22.


Functional oligomerization of the Saccharomyces cerevisiae isoprenylcysteine carboxyl methyltransferase, Ste14p.

Griggs AM, Hahne K, Hrycyna CA.

J Biol Chem. 2010 Apr 30;285(18):13380-7. doi: 10.1074/jbc.M109.061366. Epub 2010 Mar 3.


Inhibition of human P-glycoprotein transport and substrate binding using a galantamine dimer.

Namanja HA, Emmert D, Pires MM, Hrycyna CA, Chmielewski J.

Biochem Biophys Res Commun. 2009 Oct 30;388(4):672-6. doi: 10.1016/j.bbrc.2009.08.056. Epub 2009 Aug 14.


Solid-phase synthesis of prenylcysteine analogs.

Donelson JL, Hodges-Loaiza HB, Henriksen BS, Hrycyna CA, Gibbs RA.

J Org Chem. 2009 Apr 17;74(8):2975-81. doi: 10.1021/jo8021692.


Inhibition of P-glycoprotein-mediated paclitaxel resistance by reversibly linked quinine homodimers.

Pires MM, Emmert D, Hrycyna CA, Chmielewski J.

Mol Pharmacol. 2009 Jan;75(1):92-100. doi: 10.1124/mol.108.050492. Epub 2008 Oct 22.


HIV-protease inhibitors block the enzymatic activity of purified Ste24p.

Hudon SE, Coffinier C, Michaelis S, Fong LG, Young SG, Hrycyna CA.

Biochem Biophys Res Commun. 2008 Sep 19;374(2):365-8. doi: 10.1016/j.bbrc.2008.07.033. Epub 2008 Jul 17.


A potent HIV protease inhibitor, darunavir, does not inhibit ZMPSTE24 or lead to an accumulation of farnesyl-prelamin A in cells.

Coffinier C, Hudon SE, Lee R, Farber EA, Nobumori C, Miner JH, Andres DA, Spielmann HP, Hrycyna CA, Fong LG, Young SG.

J Biol Chem. 2008 Apr 11;283(15):9797-804. doi: 10.1074/jbc.M709629200. Epub 2008 Jan 28.


HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.

Coffinier C, Hudon SE, Farber EA, Chang SY, Hrycyna CA, Young SG, Fong LG.

Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13432-7. Epub 2007 Jul 25.


Substrate overlap between Mrp4 and Abcg2/Bcrp affects purine analogue drug cytotoxicity and tissue distribution.

Takenaka K, Morgan JA, Scheffer GL, Adachi M, Stewart CF, Sun D, Leggas M, Ejendal KF, Hrycyna CA, Schuetz JD.

Cancer Res. 2007 Jul 15;67(14):6965-72.


Therapeutic intervention based on protein prenylation and associated modifications.

Gelb MH, Brunsveld L, Hrycyna CA, Michaelis S, Tamanoi F, Van Voorhis WC, Waldmann H.

Nat Chem Biol. 2006 Oct;2(10):518-28. Review.


Bivalent probes of the human multidrug transporter P-glycoprotein.

Pires MM, Hrycyna CA, Chmielewski J.

Biochemistry. 2006 Sep 26;45(38):11695-702.


Multidrug ABC transporters from bacteria to man: an emerging hypothesis for the universality of molecular mechanism and function.

Hrycyna CA, Gottesman MM.

Drug Resist Updat. 1998;1(2):81-3. No abstract available.


Amide-substituted farnesylcysteine analogs as inhibitors of human isoprenylcysteine carboxyl methyltransferase.

Donelson JL, Hodges HB, Macdougall DD, Henriksen BS, Hrycyna CA, Gibbs RA.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4420-3. Epub 2006 Jun 13.


9 Structure and function of isoprenylcysteine carboxylmethyltransferase (Icmt): A key enzyme in CaaX processing.

Anderson JL, Hrycyna CA.

Enzymes. 2006;24:245-72. doi: 10.1016/S1874-6047(06)80011-9. Epub 2007 Jun 4.


Cellular efflux of auxin catalyzed by the Arabidopsis MDR/PGP transporter AtPGP1.

Geisler M, Blakeslee JJ, Bouchard R, Lee OR, Vincenzetti V, Bandyopadhyay A, Titapiwatanakun B, Peer WA, Bailly A, Richards EL, Ejendal KF, Smith AP, Baroux C, Grossniklaus U, Müller A, Hrycyna CA, Dudler R, Murphy AS, Martinoia E.

Plant J. 2005 Oct;44(2):179-94.


Synthesis of desthio prenylcysteine analogs: sulfur is important for biological activity.

Henriksen BS, Anderson JL, Hrycyna CA, Gibbs RA.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5080-3. Epub 2005 Sep 23.


Oligomerization of the human ABC transporter ABCG2: evaluation of the native protein and chimeric dimers.

Bhatia A, Schäfer HJ, Hrycyna CA.

Biochemistry. 2005 Aug 16;44(32):10893-904.


The isoprenoid substrate specificity of isoprenylcysteine carboxylmethyltransferase: development of novel inhibitors.

Anderson JL, Henriksen BS, Gibbs RA, Hrycyna CA.

J Biol Chem. 2005 Aug 19;280(33):29454-61. Epub 2005 Jun 9.


Transmembrane inhibitors of P-glycoprotein, an ABC transporter.

Tarasova NI, Seth R, Tarasov SG, Kosakowska-Cholody T, Hrycyna CA, Gottesman MM, Michejda CJ.

J Med Chem. 2005 Jun 2;48(11):3768-75.


Inhibition of membrane-associated methyltransferases by a cholesterol-based metal chelator.

Hodges HB, Zhou M, Haldar S, Anderson JL, Thompson DH, Hrycyna CA.

Bioconjug Chem. 2005 May-Jun;16(3):490-3.


A general fluorescence-based coupled assay for S-adenosylmethionine-dependent methyltransferases.

Wang C, Leffler S, Thompson DH, Hrycyna CA.

Biochem Biophys Res Commun. 2005 May 27;331(1):351-6.


Purification, functional reconstitution, and characterization of the Saccharomyces cerevisiae isoprenylcysteine carboxylmethyltransferase Ste14p.

Anderson JL, Frase H, Michaelis S, Hrycyna CA.

J Biol Chem. 2005 Feb 25;280(8):7336-45. Epub 2004 Dec 20.

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