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Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia.

Wagner FF, Benajiba L, Campbell AJ, Weïwer M, Sacher JR, Gale JP, Ross L, Puissant A, Alexe G, Conway A, Back M, Pikman Y, Galinsky I, DeAngelo DJ, Stone RM, Kaya T, Shi X, Robers MB, Machleidt T, Wilkinson J, Hermine O, Kung A, Stein AJ, Lakshminarasimhan D, Hemann MT, Scolnick E, Zhang YL, Pan JQ, Stegmaier K, Holson EB.

Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. doi: 10.1126/scitranslmed.aam8460.


Functionally Biased D2R Antagonists: Targeting the β-Arrestin Pathway to Improve Antipsychotic Treatment.

Weïwer M, Xu Q, Gale JP, Lewis M, Campbell AJ, Schroeder FA, Van de Bittner GC, Walk M, Amaya A, Su P, D Ordevic L, Sacher JR, Skepner A, Fei D, Dennehy K, Nguyen S, Faloon PW, Perez J, Cottrell JR, Liu F, Palmer M, Pan JQ, Hooker JM, Zhang YL, Scolnick E, Wagner FF, Holson EB.

ACS Chem Biol. 2018 Mar 14. doi: 10.1021/acschembio.8b00168. [Epub ahead of print]


Two large deletions extending beyond either end of the RHD gene and their red cell phenotypes.

Srivastava K, Stiles DA, Wagner FF, Flegel WA.

J Hum Genet. 2018 Jan;63(1):27-35. doi: 10.1038/s10038-017-0345-3. Epub 2017 Nov 16.


HDAC6 Brain Mapping with [18F]Bavarostat Enabled by a Ru-Mediated Deoxyfluorination.

Strebl MG, Campbell AJ, Zhao WN, Schroeder FA, Riley MM, Chindavong PS, Morin TM, Haggarty SJ, Wagner FF, Ritter T, Hooker JM.

ACS Cent Sci. 2017 Sep 27;3(9):1006-1014. doi: 10.1021/acscentsci.7b00274. Epub 2017 Sep 6.


Isoform-selective inhibitor of histone deacetylase 3 (HDAC3) limits pancreatic islet infiltration and protects female nonobese diabetic mice from diabetes.

Dirice E, Ng RWS, Martinez R, Hu J, Wagner FF, Holson EB, Wagner BK, Kulkarni RN.

J Biol Chem. 2017 Oct 27;292(43):17598-17608. doi: 10.1074/jbc.M117.804328. Epub 2017 Aug 31.


Serologic and molecular characterization of weak D type 29.

Ouchari M, Srivastava K, Döscher A, Conradi R, Jemni Yacoub S, Wagner FF, Flegel WA.

Transfusion. 2017 Oct;57(10):2542-2544. doi: 10.1111/trf.14218. Epub 2017 Jul 3. No abstract available.


Overlapping and Divergent Actions of Structurally Distinct Histone Deacetylase Inhibitors in Cardiac Fibroblasts.

Schuetze KB, Stratton MS, Blakeslee WW, Wempe MF, Wagner FF, Holson EB, Kuo YM, Andrews AJ, Gilbert TM, Hooker JM, McKinsey TA.

J Pharmacol Exp Ther. 2017 Apr;361(1):140-150. doi: 10.1124/jpet.116.237701. Epub 2017 Feb 7.


Molecular typing for blood group antigens within 40 min by direct polymerase chain reaction from plasma or serum.

Wagner FF, Flegel WA, Bittner R, Döscher A.

Br J Haematol. 2017 Mar;176(5):814-821. doi: 10.1111/bjh.14469. Epub 2016 Dec 19.


Activity of caffeic acid phenethyl ester in Caenorhabditis elegans.

Coleman JJ, Komura T, Munro J, Wu MP, Busanelli RR, Koehler AN, Thomas M, Wagner FF, Holson EB, Mylonakis E.

Future Med Chem. 2016 Oct 14. [Epub ahead of print]


Molecular immunohaematology round table discussions at the AABB Annual Meeting, Anaheim 2015.

Flegel WA, Castilho L, Heaton WA, Keller MA, Klapper EB, Lane WJ, Pirenne F, Shehata N, Stack G, St-Louis M, Tormey CA, Wagner FF, Waxman DA, Denomme GA.

Blood Transfus. 2016 Jul 29;14(6):557-565. doi: 10.2450/2016.0063-16. [Epub ahead of print] No abstract available.


The DAU cluster: a comparative analysis of 18 RHD alleles, some forming partial D antigens.

Srivastava K, Polin H, Sheldon SL, Wagner FF, Grabmer C, Gabriel C, Denomme GA, Flegel WA.

Transfusion. 2016 Oct;56(10):2520-2531. doi: 10.1111/trf.13739. Epub 2016 Aug 2.


Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors.

Wagner FF, Weïwer M, Steinbacher S, Schomburg A, Reinemer P, Gale JP, Campbell AJ, Fisher SL, Zhao WN, Reis SA, Hennig KM, Thomas M, Müller P, Jefson MR, Fass DM, Haggarty SJ, Zhang YL, Holson EB.

Bioorg Med Chem. 2016 Sep 15;24(18):4008-4015. doi: 10.1016/j.bmc.2016.06.040. Epub 2016 Jun 22.


Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.

Liang SH, Chen JM, Normandin MD, Chang JS, Chang GC, Taylor CK, Trapa P, Plummer MS, Para KS, Conn EL, Lopresti-Morrow L, Lanyon LF, Cook JM, Richter KE, Nolan CE, Schachter JB, Janat F, Che Y, Shanmugasundaram V, Lefker BA, Enerson BE, Livni E, Wang L, Guehl NJ, Patnaik D, Wagner FF, Perlis R, Holson EB, Haggarty SJ, El Fakhri G, Kurumbail RG, Vasdev N.

Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9601-5. doi: 10.1002/anie.201603797. Epub 2016 Jun 29.


Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects.

Wagner FF, Bishop JA, Gale JP, Shi X, Walk M, Ketterman J, Patnaik D, Barker D, Walpita D, Campbell AJ, Nguyen S, Lewis M, Ross L, Weïwer M, An WF, Germain AR, Nag PP, Metkar S, Kaya T, Dandapani S, Olson DE, Barbe AL, Lazzaro F, Sacher JR, Cheah JH, Fei D, Perez J, Munoz B, Palmer M, Stegmaier K, Schreiber SL, Scolnick E, Zhang YL, Haggarty SJ, Holson EB, Pan JQ.

ACS Chem Biol. 2016 Jul 15;11(7):1952-63. doi: 10.1021/acschembio.6b00306. Epub 2016 May 13.


An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection.

Wagner FF, Lundh M, Kaya T, McCarren P, Zhang YL, Chattopadhyay S, Gale JP, Galbo T, Fisher SL, Meier BC, Vetere A, Richardson S, Morgan NG, Christensen DP, Gilbert TJ, Hooker JM, Leroy M, Walpita D, Mandrup-Poulsen T, Wagner BK, Holson EB.

ACS Chem Biol. 2016 Feb 19;11(2):363-74. doi: 10.1021/acschembio.5b00640. Epub 2015 Dec 7.


Hydroxamate-based histone deacetylase inhibitors can protect neurons from oxidative stress via a histone deacetylase-independent catalase-like mechanism.

Olson DE, Sleiman SF, Bourassa MW, Wagner FF, Gale JP, Zhang YL, Ratan RR, Holson EB.

Chem Biol. 2015 Apr 23;22(4):439-445. doi: 10.1016/j.chembiol.2015.03.014. Epub 2015 Apr 16.


Kinetically Selective Inhibitors of Histone Deacetylase 2 (HDAC2) as Cognition Enhancers.

Wagner FF, Zhang YL, Fass DM, Joseph N, Gale JP, Weïwer M, McCarren P, Fisher SL, Kaya T, Zhao WN, Reis SA, Hennig KM, Thomas M, Lemercier BC, Lewis MC, Guan JS, Moyer MP, Scolnick E, Haggarty SJ, Tsai LH, Holson EB.

Chem Sci. 2015 Jan 1;6(1):804-815.


Molecular immunohaematology round table discussions at the AABB Annual Meeting, Denver 2013.

Flegel WA, Castilho L, Delaney M, Klapper EB, Moulds JM, Noizat-Pirenne F, Shehata N, Stack G, Tormey CA, Wagner FF, Waxman DA, Weinstock C, Wendel S, Denomme GA.

Blood Transfus. 2015 Jul;13(3):514-20. doi: 10.2450/2014.0213-14. Epub 2014 Dec 2. No abstract available.


The Rhesus Site.

Wagner FF, Flegel WA.

Transfus Med Hemother. 2014 Oct;41(5):357-63. doi: 10.1159/000366176. Epub 2014 Sep 15. Review.


Hydroxamic acid-based histone deacetylase (HDAC) inhibitors can mediate neuroprotection independent of HDAC inhibition.

Sleiman SF, Olson DE, Bourassa MW, Karuppagounder SS, Zhang YL, Gale J, Wagner FF, Basso M, Coppola G, Pinto JT, Holson EB, Ratan RR.

J Neurosci. 2014 Oct 22;34(43):14328-37. doi: 10.1523/JNEUROSCI.1010-14.2014. Erratum in: J Neurosci. 2015 Jan 7;35(1):438.


In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs.

Wang C, Schroeder FA, Wey HY, Borra R, Wagner FF, Reis S, Kim SW, Holson EB, Haggarty SJ, Hooker JM.

J Med Chem. 2014 Oct 9;57(19):7999-8009. doi: 10.1021/jm500872p. Epub 2014 Sep 18.


Selective HDAC inhibition for the disruption of latent HIV-1 infection.

Barton KM, Archin NM, Keedy KS, Espeseth AS, Zhang YL, Gale J, Wagner FF, Holson EB, Margolis DM.

PLoS One. 2014 Aug 19;9(8):e102684. doi: 10.1371/journal.pone.0102684. eCollection 2014.


An unbiased approach to identify endogenous substrates of "histone" deacetylase 8.

Olson DE, Udeshi ND, Wolfson NA, Pitcairn CA, Sullivan ED, Jaffe JD, Svinkina T, Natoli T, Lu X, Paulk J, McCarren P, Wagner FF, Barker D, Howe E, Lazzaro F, Gale JP, Zhang YL, Subramanian A, Fierke CA, Carr SA, Holson EB.

ACS Chem Biol. 2014 Oct 17;9(10):2210-6. doi: 10.1021/cb500492r. Epub 2014 Aug 11.


Studies toward the total synthesis of dihydrolycolucine. Preparation of AB and CEF ring fragments.

Cash BM, Prevost N, Wagner FF, Comins DL.

J Org Chem. 2014 Jun 20;79(12):5740-5. doi: 10.1021/jo500878v. Epub 2014 May 29.


Discovery of Potent and Highly Selective Inhibitors of GSK3b.

An WF, Germain AR, Bishop JA, Nag PP, Metkar S, Ketterman J, Walk M, Weiwer M, Liu X, Patnaik D, Zhang YL, Gale J, Zhao W, Kaya T, Barker D, Wagner FF, Holson EB, Dandapani S, Perez J, Munoz B, Palmer M, Pan JQ, Haggarty SJ, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2014 May 13].


Why do we use serological blood group phenotype determination in chronically transfused patients?

Wagner FF.

Blood Transfus. 2014 Jan;12(1):1-2. doi: 10.2450/2013.0186-13. Epub 2013 Dec 11. No abstract available.


Design, synthesis, and evaluation of hydroxamic acid-based molecular probes for in vivo imaging of histone deacetylase (HDAC) in brain.

Wang C, Eessalu TE, Barth VN, Mitch CH, Wagner FF, Hong Y, Neelamegam R, Schroeder FA, Holson EB, Haggarty SJ, Hooker JM.

Am J Nucl Med Mol Imaging. 2013 Dec 15;4(1):29-38. eCollection 2013.


Two molecular polymorphisms to detect the (C)ce(s) type 1 haplotype.

Flegel WA, Wagner FF.

Blood Transfus. 2014 Jan;12(1):136-7. doi: 10.2450/2013.0149-13. Epub 2013 Nov 15. No abstract available.


Molecular immunohaematology round table discussions at the AABB Annual Meeting, Boston 2012.

Flegel WA, Johnson ST, Keller MA, Klapper EB, Khuu HM, Moulds JM, Seltsam AW, Stack G, St-Louis M, Tormey CA, Wagner FF, Weinstock C, Yazer MH, Denomme GA.

Blood Transfus. 2014 Apr;12(2):280-6. doi: 10.2450/2013.0022-13. Epub 2013 Oct 18. No abstract available.


Small molecule inhibitors of zinc-dependent histone deacetylases.

Wagner FF, Weїwer M, Lewis MC, Holson EB.

Neurotherapeutics. 2013 Oct;10(4):589-604. doi: 10.1007/s13311-013-0226-1. Review.


Therapeutic potential of isoform selective HDAC inhibitors for the treatment of schizophrenia.

Weïwer M, Lewis MC, Wagner FF, Holson EB.

Future Med Chem. 2013 Sep;5(13):1491-508. doi: 10.4155/fmc.13.141. Review.


A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests.

Schroeder FA, Lewis MC, Fass DM, Wagner FF, Zhang YL, Hennig KM, Gale J, Zhao WN, Reis S, Barker DD, Berry-Scott E, Kim SW, Clore EL, Hooker JM, Holson EB, Haggarty SJ, Petryshen TL.

PLoS One. 2013 Aug 14;8(8):e71323. doi: 10.1371/journal.pone.0071323. eCollection 2013.


RHD PCR of D-Negative Blood Donors.

Wagner FF.

Transfus Med Hemother. 2013 Jun;40(3):172-81. doi: 10.1159/000351604. Epub 2013 May 8.


FDG-PET imaging reveals local brain glucose utilization is altered by class I histone deacetylase inhibitors.

Schroeder FA, Chonde DB, Riley MM, Moseley CK, Granda ML, Wilson CM, Wagner FF, Zhang YL, Gale J, Holson EB, Haggarty SJ, Hooker JM.

Neurosci Lett. 2013 Aug 29;550:119-24. doi: 10.1016/j.neulet.2013.06.016. Epub 2013 Jun 25.


Signal-dependent repression of DUSP5 by class I HDACs controls nuclear ERK activity and cardiomyocyte hypertrophy.

Ferguson BS, Harrison BC, Jeong MY, Reid BG, Wempe MF, Wagner FF, Holson EB, McKinsey TA.

Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9806-11. doi: 10.1073/pnas.1301509110. Epub 2013 May 29.


Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation.

Frumm SM, Fan ZP, Ross KN, Duvall JR, Gupta S, VerPlank L, Suh BC, Holson E, Wagner FF, Smith WB, Paranal RM, Bassil CF, Qi J, Roti G, Kung AL, Bradner JE, Tolliday N, Stegmaier K.

Chem Biol. 2013 May 23;20(5):713-25. doi: 10.1016/j.chembiol.2013.03.020.


Discovery of the first histone deacetylase 6/8 dual inhibitors.

Olson DE, Wagner FF, Kaya T, Gale JP, Aidoud N, Davoine EL, Lazzaro F, Weïwer M, Zhang YL, Holson EB.

J Med Chem. 2013 Jun 13;56(11):4816-20. doi: 10.1021/jm400390r. Epub 2013 May 29.


D category IV: a group of clinically relevant and phylogenetically diverse partial D.

von Zabern I, Wagner FF, Moulds JM, Moulds JJ, Flegel WA.

Transfusion. 2013 Nov;53(11 Suppl 2):2960-73. doi: 10.1111/trf.12145. Epub 2013 Mar 5.


Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif.

Wagner FF, Olson DE, Gale JP, Kaya T, Weïwer M, Aidoud N, Thomas M, Davoine EL, Lemercier BC, Zhang YL, Holson EB.

J Med Chem. 2013 Feb 28;56(4):1772-6. doi: 10.1021/jm301355j. Epub 2013 Feb 18.


Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.

Lowe JT, Lee MD 4th, Akella LB, Davoine E, Donckele EJ, Durak L, Duvall JR, Gerard B, Holson EB, Joliton A, Kesavan S, Lemercier BC, Liu H, Marié JC, Mulrooney CA, Muncipinto G, Welzel-O'Shea M, Panko LM, Rowley A, Suh BC, Thomas M, Wagner FF, Wei J, Foley MA, Marcaurelle LA.

J Org Chem. 2012 Sep 7;77(17):7187-211. doi: 10.1021/jo300974j. Epub 2012 Aug 10.


Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis.

Chou DH, Holson EB, Wagner FF, Tang AJ, Maglathlin RL, Lewis TA, Schreiber SL, Wagner BK.

Chem Biol. 2012 Jun 22;19(6):669-73. doi: 10.1016/j.chembiol.2012.05.010.


Evaluation of single-nucleotide polymorphisms as internal controls in prenatal diagnosis of fetal blood groups.

Doescher A, Petershofen EK, Wagner FF, Schunter M, Müller TH.

Transfusion. 2013 Feb;53(2):353-62. doi: 10.1111/j.1537-2995.2012.03738.x. Epub 2012 Jun 13.


Chromatin-targeting small molecules cause class-specific transcriptional changes in pancreatic endocrine cells.

Kubicek S, Gilbert JC, Fomina-Yadlin D, Gitlin AD, Yuan Y, Wagner FF, Holson EB, Luo T, Lewis TA, Taylor B, Gupta S, Shamji AF, Wagner BK, Clemons PA, Schreiber SL.

Proc Natl Acad Sci U S A. 2012 Apr 3;109(14):5364-9. doi: 10.1073/pnas.1201079109. Epub 2012 Mar 20.


AKT kinase activity is required for lithium to modulate mood-related behaviors in mice.

Pan JQ, Lewis MC, Ketterman JK, Clore EL, Riley M, Richards KR, Berry-Scott E, Liu X, Wagner FF, Holson EB, Neve RL, Biechele TL, Moon RT, Scolnick EM, Petryshen TL, Haggarty SJ.

Neuropsychopharmacology. 2011 Jun;36(7):1397-411. doi: 10.1038/npp.2011.24. Epub 2011 Mar 9.


Hdac3 is essential for the maintenance of chromatin structure and genome stability.

Bhaskara S, Knutson SK, Jiang G, Chandrasekharan MB, Wilson AJ, Zheng S, Yenamandra A, Locke K, Yuan JL, Bonine-Summers AR, Wells CE, Kaiser JF, Washington MK, Zhao Z, Wagner FF, Sun ZW, Xia F, Holson EB, Khabele D, Hiebert SW.

Cancer Cell. 2010 Nov 16;18(5):436-47. doi: 10.1016/j.ccr.2010.10.022.


Molecular testing in transfusion medicine.

Wagner FF.

Expert Opin Med Diagn. 2010 Sep;4(5):411-28. doi: 10.1517/17530059.2010.506509. Epub 2010 Aug 5.


Specific amino acid substitutions cause distinct expression of JAL (RH48) and JAHK (RH53) antigens in RhCE and not in RhD.

Schmid P, von Zabern I, Scharberg EA, Wagner FF, Flegel WA.

Transfusion. 2010 Jan;50(1):267-9. doi: 10.1111/j.1537-2995.2009.02446.x. No abstract available.


Characterization of plant-derived saponin natural products against Candida albicans.

Coleman JJ, Okoli I, Tegos GP, Holson EB, Wagner FF, Hamblin MR, Mylonakis E.

ACS Chem Biol. 2010 Mar 19;5(3):321-32. doi: 10.1021/cb900243b.


Blood donor screening with cobas s 201/cobas TaqScreen MPX under routine conditions at German Red Cross institutes.

Schmidt M, Pichl L, Jork C, Hourfar MK, Schottstedt V, Wagner FF, Seifried E, Müller TH, Bux J, Saldanha J.

Vox Sang. 2010 Jan;98(1):37-46. doi: 10.1111/j.1423-0410.2009.01219.x. Epub 2009 Aug 4.


RHCE alleles detected after weak and/or discrepant results in automated Rh blood grouping of blood donors in Northern Germany.

Döscher A, Vogt C, Bittner R, Gerdes I, Petershofen EK, Wagner FF.

Transfusion. 2009 Sep;49(9):1803-11. doi: 10.1111/j.1537-2995.2009.02221.x. Epub 2009 May 18.


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