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Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.

Osko JD, Christianson DW.

Bioorg Med Chem Lett. 2020 Feb 11:127023. doi: 10.1016/j.bmcl.2020.127023. [Epub ahead of print] Review.


Higher-Order Oligomerization of a Chimeric αβγ Bifunctional Diterpene Synthase with Prenyltransferase and Class II Cyclase Activities is Concentration-Dependent.

Ronnebaum TA, Gupta K, Christianson DW.

J Struct Biol. 2020 Jan 21:107463. doi: 10.1016/j.jsb.2020.107463. [Epub ahead of print]


Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6.

Osko JD, Porter NJ, Narayana Reddy PA, Xiao YC, Rokka J, Jung M, Hooker JM, Salvino JM, Christianson DW.

J Med Chem. 2020 Jan 9;63(1):295-308. doi: 10.1021/acs.jmedchem.9b01540. Epub 2019 Dec 19.


Structural Basis of Catalysis and Inhibition of HDAC6 CD1, the Enigmatic Catalytic Domain of Histone Deacetylase 6.

Osko JD, Christianson DW.

Biochemistry. 2019 Dec 10;58(49):4912-4924. doi: 10.1021/acs.biochem.9b00934. Epub 2019 Dec 2.


Binding of N8-Acetylspermidine Analogues to Histone Deacetylase 10 Reveals Molecular Strategies for Blocking Polyamine Deacetylation.

Herbst-Gervasoni CJ, Christianson DW.

Biochemistry. 2019 Dec 10;58(49):4957-4969. doi: 10.1021/acs.biochem.9b00906. Epub 2019 Dec 2.


Phosphorylation of Histone Deacetylase 8: Structural and Mechanistic Analysis of the Phosphomimetic S39E Mutant.

Welker Leng KR, Castañeda CA, Decroos C, Islam B, Haider SM, Christianson DW, Fierke CA.

Biochemistry. 2019 Nov 12;58(45):4480-4493. doi: 10.1021/acs.biochem.9b00653. Epub 2019 Nov 4.


Preparation of a new construct of human histone deacetylase 8 for the crystallization of enzyme-inhibitor complexes.

Porter NJ, Christianson DW.

Methods Enzymol. 2019;626:561-585. doi: 10.1016/bs.mie.2019.06.029. Epub 2019 Jul 18.


Methods for the expression, purification, and crystallization of histone deacetylase 6-inhibitor complexes.

Osko JD, Christianson DW.

Methods Enzymol. 2019;626:447-474. doi: 10.1016/bs.mie.2019.06.028. Epub 2019 Jul 18.


Structure and Function of the Acetylpolyamine Amidohydrolase from the Deep Earth Halophile Marinobacter subterrani.

Osko JD, Roose BW, Shinsky SA, Christianson DW.

Biochemistry. 2019 Sep 10;58(36):3755-3766. doi: 10.1021/acs.biochem.9b00582. Epub 2019 Aug 27.


Structural Basis of Tryptophan Reverse N-Prenylation Catalyzed by CymD.

Roose BW, Christianson DW.

Biochemistry. 2019 Jul 30;58(30):3232-3242. doi: 10.1021/acs.biochem.9b00399. Epub 2019 Jul 15.


Crystal structure of F95Q epi-isozizaene synthase, an engineered sesquiterpene cyclase that generates biofuel precursors β- and γ-curcumene.

Blank PN, Barrow GH, Christianson DW.

J Struct Biol. 2019 Aug 1;207(2):218-224. doi: 10.1016/j.jsb.2019.05.011. Epub 2019 May 29.


Structure of Sesquisabinene Synthase 1, a Terpenoid Cyclase That Generates a Strained [3.1.0] Bridged-Bicyclic Product.

Blank PN, Shinsky SA, Christianson DW.

ACS Chem Biol. 2019 May 17;14(5):1011-1019. doi: 10.1021/acschembio.9b00218. Epub 2019 Apr 17.


Structure, mechanism, and inhibition of the zinc-dependent histone deacetylases.

Porter NJ, Christianson DW.

Curr Opin Struct Biol. 2019 Dec;59:9-18. doi: 10.1016/ Epub 2019 Feb 8. Review. No abstract available.


Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.

Vögerl K, Ong N, Senger J, Herp D, Schmidtkunz K, Marek M, Müller M, Bartel K, Shaik TB, Porter NJ, Robaa D, Christianson DW, Romier C, Sippl W, Jung M, Bracher F.

J Med Chem. 2019 Feb 14;62(3):1138-1166. doi: 10.1021/acs.jmedchem.8b01090. Epub 2019 Feb 1.


Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.

Porter NJ, Shen S, Barinka C, Kozikowski AP, Christianson DW.

ACS Med Chem Lett. 2018 Nov 21;9(12):1301-1305. doi: 10.1021/acsmedchemlett.8b00487. eCollection 2018 Dec 13.


Correction to Structural and Chemical Biology of Terpenoid Cyclases.

Christianson DW.

Chem Rev. 2018 Dec 26;118(24):11795. doi: 10.1021/acs.chemrev.8b00682. Epub 2018 Dec 12. No abstract available.


Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.

Bhatia S, Krieger V, Groll M, Osko JD, Reßing N, Ahlert H, Borkhardt A, Kurz T, Christianson DW, Hauer J, Hansen FK.

J Med Chem. 2018 Nov 21;61(22):10299-10309. doi: 10.1021/acs.jmedchem.8b01487. Epub 2018 Nov 8.


Crystal Structure of Cucumene Synthase, a Terpenoid Cyclase That Generates a Linear Triquinane Sesquiterpene.

Blank PN, Pemberton TA, Chow JY, Poulter CD, Christianson DW.

Biochemistry. 2018 Nov 6;57(44):6326-6335. doi: 10.1021/acs.biochem.8b00899. Epub 2018 Oct 22.


Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity.

Porter NJ, Osko JD, Diedrich D, Kurz T, Hooker JM, Hansen FK, Christianson DW.

J Med Chem. 2018 Sep 13;61(17):8054-8060. doi: 10.1021/acs.jmedchem.8b01013. Epub 2018 Aug 17.


Multicomponent Synthesis and Binding Mode of Imidazo[1,2- a]pyridine-Capped Selective HDAC6 Inhibitors.

Mackwitz MKW, Hamacher A, Osko JD, Held J, Schöler A, Christianson DW, Kassack MU, Hansen FK.

Org Lett. 2018 Jun 1;20(11):3255-3258. doi: 10.1021/acs.orglett.8b01118. Epub 2018 May 23.


Entropy as a Driver of Selectivity for Inhibitor Binding to Histone Deacetylase 6.

Porter NJ, Wagner FF, Christianson DW.

Biochemistry. 2018 Jul 3;57(26):3916-3924. doi: 10.1021/acs.biochem.8b00367. Epub 2018 May 18.


Polyamine Deacetylase Structure and Catalysis: Prokaryotic Acetylpolyamine Amidohydrolase and Eukaryotic HDAC10.

Shinsky SA, Christianson DW.

Biochemistry. 2018 Jun 5;57(22):3105-3114. doi: 10.1021/acs.biochem.8b00079. Epub 2018 Mar 21. Review.


Unusual zinc-binding mode of HDAC6-selective hydroxamate inhibitors.

Porter NJ, Mahendran A, Breslow R, Christianson DW.

Proc Natl Acad Sci U S A. 2017 Dec 19;114(51):13459-13464. doi: 10.1073/pnas.1718823114. Epub 2017 Dec 4.


Substitution of Aromatic Residues with Polar Residues in the Active Site Pocket of epi-Isozizaene Synthase Leads to the Generation of New Cyclic Sesquiterpenes.

Blank PN, Barrow GH, Chou WKW, Duan L, Cane DE, Christianson DW.

Biochemistry. 2017 Oct 31;56(43):5798-5811. doi: 10.1021/acs.biochem.7b00895. Epub 2017 Oct 17.


Binding of the Microbial Cyclic Tetrapeptide Trapoxin A to the Class I Histone Deacetylase HDAC8.

Porter NJ, Christianson DW.

ACS Chem Biol. 2017 Sep 15;12(9):2281-2286. doi: 10.1021/acschembio.7b00330. Epub 2017 Aug 30.


Structural and Chemical Biology of Terpenoid Cyclases.

Christianson DW.

Chem Rev. 2017 Sep 13;117(17):11570-11648. doi: 10.1021/acs.chemrev.7b00287. Epub 2017 Aug 25. Review. Erratum in: Chem Rev. 2018 Dec 26;118(24):11795.


ARID1A-mutated ovarian cancers depend on HDAC6 activity.

Bitler BG, Wu S, Park PH, Hai Y, Aird KM, Wang Y, Zhai Y, Kossenkov AV, Vara-Ailor A, Rauscher FJ III, Zou W, Speicher DW, Huntsman DG, Conejo-Garcia JR, Cho KR, Christianson DW, Zhang R.

Nat Cell Biol. 2017 Aug;19(8):962-973. doi: 10.1038/ncb3582. Epub 2017 Jul 24.


Histone deacetylase 10 structure and molecular function as a polyamine deacetylase.

Hai Y, Shinsky SA, Porter NJ, Christianson DW.

Nat Commun. 2017 May 18;8:15368. doi: 10.1038/ncomms15368.


Exploring the Influence of Domain Architecture on the Catalytic Function of Diterpene Synthases.

Pemberton TA, Chen M, Harris GG, Chou WK, Duan L, Köksal M, Genshaft AS, Cane DE, Christianson DW.

Biochemistry. 2017 Apr 11;56(14):2010-2023. doi: 10.1021/acs.biochem.7b00137. Epub 2017 Mar 31.


Structural and Functional Influence of the Glycine-Rich Loop G302GGGY on the Catalytic Tyrosine of Histone Deacetylase 8.

Porter NJ, Christianson NH, Decroos C, Christianson DW.

Biochemistry. 2016 Dec 6;55(48):6718-6729. Epub 2016 Nov 28.


Structural aspects of HDAC8 mechanism and dysfunction in Cornelia de Lange syndrome spectrum disorders.

Deardorff MA, Porter NJ, Christianson DW.

Protein Sci. 2016 Nov;25(11):1965-1976. doi: 10.1002/pro.3030. Epub 2016 Sep 16. Review.


Editorial overview: Catalysis and regulation: enzyme structure, mechanism, and biosynthetic pathways.

Christianson DW, Scrutton NS.

Curr Opin Struct Biol. 2016 Dec;41:viii-x. doi: 10.1016/ Epub 2016 Sep 16. No abstract available.


Histone deacetylase 6 structure and molecular basis of catalysis and inhibition.

Hai Y, Christianson DW.

Nat Chem Biol. 2016 Sep;12(9):741-7. doi: 10.1038/nchembio.2134. Epub 2016 Jul 25.


Multi-domain terpenoid cyclase architecture and prospects for proximity in bifunctional catalysis.

Chen M, Harris GG, Pemberton TA, Christianson DW.

Curr Opin Struct Biol. 2016 Dec;41:27-37. doi: 10.1016/ Epub 2016 Jun 7. Review.


Probing the Role of Active Site Water in the Sesquiterpene Cyclization Reaction Catalyzed by Aristolochene Synthase.

Chen M, Chou WK, Al-Lami N, Faraldos JA, Allemann RK, Cane DE, Christianson DW.

Biochemistry. 2016 May 24;55(20):2864-74. doi: 10.1021/acs.biochem.6b00343. Epub 2016 May 12.


General base-general acid catalysis by terpenoid cyclases.

Pemberton TA, Christianson DW.

J Antibiot (Tokyo). 2016 Jul;69(7):486-93. doi: 10.1038/ja.2016.39. Epub 2016 Apr 13. Review.


Crystal structures of Leishmania mexicana arginase complexed with α,α-disubstituted boronic amino-acid inhibitors.

Hai Y, Christianson DW.

Acta Crystallogr F Struct Biol Commun. 2016 Apr;72(Pt 4):300-6. doi: 10.1107/S2053230X16003630. Epub 2016 Mar 16.


Mechanism of Germacradien-4-ol Synthase-Controlled Water Capture.

Grundy DJ, Chen M, González V, Leoni S, Miller DJ, Christianson DW, Allemann RK.

Biochemistry. 2016 Apr 12;55(14):2112-21. doi: 10.1021/acs.biochem.6b00115. Epub 2016 Mar 30.


General Base-General Acid Catalysis in Human Histone Deacetylase 8.

Gantt SM, Decroos C, Lee MS, Gullett LE, Bowman CM, Christianson DW, Fierke CA.

Biochemistry. 2016 Feb 9;55(5):820-32. doi: 10.1021/acs.biochem.5b01327. Epub 2016 Jan 25.


Structure and Function of Fusicoccadiene Synthase, a Hexameric Bifunctional Diterpene Synthase.

Chen M, Chou WK, Toyomasu T, Cane DE, Christianson DW.

ACS Chem Biol. 2016 Apr 15;11(4):889-99. doi: 10.1021/acschembio.5b00960. Epub 2016 Jan 6.


Structural Studies of Geosmin Synthase, a Bifunctional Sesquiterpene Synthase with αα Domain Architecture That Catalyzes a Unique Cyclization-Fragmentation Reaction Sequence.

Harris GG, Lombardi PM, Pemberton TA, Matsui T, Weiss TM, Cole KE, Köksal M, Murphy FV 4th, Vedula LS, Chou WK, Cane DE, Christianson DW.

Biochemistry. 2015 Dec 8;54(48):7142-55. doi: 10.1021/acs.biochem.5b01143. Epub 2015 Nov 24.


Biochemical and structural characterization of HDAC8 mutants associated with Cornelia de Lange syndrome spectrum disorders.

Decroos C, Christianson NH, Gullett LE, Bowman CM, Christianson KE, Deardorff MA, Christianson DW.

Biochemistry. 2015 Oct 27;54(42):6501-13. doi: 10.1021/acs.biochem.5b00881. Epub 2015 Oct 14.


Design, Synthesis, and Evaluation of Polyamine Deacetylase Inhibitors, and High-Resolution Crystal Structures of Their Complexes with Acetylpolyamine Amidohydrolase.

Decroos C, Christianson DW.

Biochemistry. 2015 Aug 4;54(30):4692-703. doi: 10.1021/acs.biochem.5b00536. Epub 2015 Jul 22.


Variable active site loop conformations accommodate the binding of macrocyclic largazole analogues to HDAC8.

Decroos C, Clausen DJ, Haines BE, Wiest O, Williams RM, Christianson DW.

Biochemistry. 2015 Mar 31;54(12):2126-35. doi: 10.1021/acs.biochem.5b00010. Epub 2015 Mar 20.


Crystal structure of an arginase-like protein from Trypanosoma brucei that evolved without a binuclear manganese cluster.

Hai Y, Kerkhoven EJ, Barrett MP, Christianson DW.

Biochemistry. 2015 Jan 20;54(2):458-71. doi: 10.1021/bi501366a. Epub 2014 Dec 23.


Compromised structure and function of HDAC8 mutants identified in Cornelia de Lange Syndrome spectrum disorders.

Decroos C, Bowman CM, Moser JA, Christianson KE, Deardorff MA, Christianson DW.

ACS Chem Biol. 2014 Sep 19;9(9):2157-64. doi: 10.1021/cb5003762. Epub 2014 Jul 30.


Crystal structure of Schistosoma mansoni arginase, a potential drug target for the treatment of schistosomiasis.

Hai Y, Edwards JE, Van Zandt MC, Hoffmann KF, Christianson DW.

Biochemistry. 2014 Jul 22;53(28):4671-84. doi: 10.1021/bi5004519. Epub 2014 Jul 9.


Reprogramming the chemodiversity of terpenoid cyclization by remolding the active site contour of epi-isozizaene synthase.

Li R, Chou WK, Himmelberger JA, Litwin KM, Harris GG, Cane DE, Christianson DW.

Biochemistry. 2014 Feb 25;53(7):1155-68. doi: 10.1021/bi401643u. Epub 2014 Feb 11.


Loss-of-function HDAC8 mutations cause a phenotypic spectrum of Cornelia de Lange syndrome-like features, ocular hypertelorism, large fontanelle and X-linked inheritance.

Kaiser FJ, Ansari M, Braunholz D, Concepción Gil-Rodríguez M, Decroos C, Wilde JJ, Fincher CT, Kaur M, Bando M, Amor DJ, Atwal PS, Bahlo M, Bowman CM, Bradley JJ, Brunner HG, Clark D, Del Campo M, Di Donato N, Diakumis P, Dubbs H, Dyment DA, Eckhold J, Ernst S, Ferreira JC, Francey LJ, Gehlken U, Guillén-Navarro E, Gyftodimou Y, Hall BD, Hennekam R, Hudgins L, Hullings M, Hunter JM, Yntema H, Innes AM, Kline AD, Krumina Z, Lee H, Leppig K, Lynch SA, Mallozzi MB, Mannini L, McKee S, Mehta SG, Micule I; Care4Rare Canada Consortium, Mohammed S, Moran E, Mortier GR, Moser JA, Noon SE, Nozaki N, Nunes L, Pappas JG, Penney LS, Pérez-Aytés A, Petersen MB, Puisac B, Revencu N, Roeder E, Saitta S, Scheuerle AE, Schindeler KL, Siu VM, Stark Z, Strom SP, Thiese H, Vater I, Willems P, Williamson K, Wilson LC; University of Washington Center for Mendelian Genomics, Hakonarson H, Quintero-Rivera F, Wierzba J, Musio A, Gillessen-Kaesbach G, Ramos FJ, Jackson LG, Shirahige K, Pié J, Christianson DW, Krantz ID, Fitzpatrick DR, Deardorff MA.

Hum Mol Genet. 2014 Jun 1;23(11):2888-900. doi: 10.1093/hmg/ddu002. Epub 2014 Jan 8.


Formiminoglutamase from Trypanosoma cruzi is an arginase-like manganese metalloenzyme.

Hai Y, Dugery RJ, Healy D, Christianson DW.

Biochemistry. 2013 Dec 23;52(51):9294-309. doi: 10.1021/bi401352h. Epub 2013 Nov 21.

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