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Items: 31

1.

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.

PMID:
29515000
2.

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 Apr 20;13(4):1038-1047. doi: 10.1021/acschembio.8b00168. Epub 2018 Mar 14.

PMID:
29485852
3.

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.

PMID:
27377864
4.

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.

PMID:
27128528
5.

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.

6.

A Small Molecule Inhibitor of the MITF Molecular Pathway.

Faloon PW, Bennion M, Weiner WS, Smith RA, Wurst J, Weiwer M, Hartland C, Mosher CM, Johnston S, Porubsky P, Neuenswander B, Dandapani S, Munoz B, Schoenen FJ, Metkar S, Haq R, Fisher DE, Aubé J, Palmer M, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 13 [updated 2014 Sep 18].

7.

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].

8.

Screen for Inhibitors of STK33 Kinase Activity.

Spoonamore J, Weïwer M, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Munoz B, Palmer M, Scherer C, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Dec 16 [updated 2014 May 13].

9.

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.

PMID:
24024943
10.

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.

PMID:
23672185
11.

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.

PMID:
23368884
12.

A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.

Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA, Stern AM, Schreiber SL, Munoz B.

ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038. Epub 2012 Oct 22.

13.

ML238: An Antimalarial Small Molecule of a Unique Structural Class.

Weiwer M, Mulrooney C, Massi D, Heidebrecht R, Wiegand R, Lukens AK, Dick J, Wirth D, Ekland E, Cheng CC, Zhao J, Yuan J, Su XZ, Johnson RL, Guha R, Dandapani S, Munoz B, Palmer M, Thomas C, Austin CP, Fidock D, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 14 [updated 2011 Dec 12].

14.

Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies.

Dockendorff C, Nagiec MM, Weïwer M, Buhrlage S, Ting A, Nag PP, Germain A, Kim HJ, Youngsaye W, Scherer C, Bennion M, Xue L, Stanton BZ, Lewis TA, Macpherson L, Palmer M, Foley MA, Perez JR, Schreiber SL.

ACS Med Chem Lett. 2012 Oct 11;3(10):808-813. Epub 2012 Aug 30.

15.

Screen for RAS-Selective Lethal Compounds and VDAC Ligands - Probe 2.

Bittker JA, Weiwer M, Lewis T, Shimada K, Yang WS, MacPherson L, Dandapani S, Munoz B, Palmer M, Stockwell BR, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Feb 10 [updated 2011 Dec 12].

16.

Discovery of Inhibitors of Anti-Apoptotic Protein A1.

Bittker JA, Weiwer M, Wei G, Germain A, Brown E, Dandapani S, Munoz B, Palmer M, Golub T, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 21 [updated 2011 Nov 21].

17.

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.

Heidebrecht RW Jr, Mulrooney C, Austin CP, Barker RH Jr, Beaudoin JA, Cheng KC, Comer E, Dandapani S, Dick J, Duvall JR, Ekland EH, Fidock DA, Fitzgerald ME, Foley M, Guha R, Hinkson P, Kramer M, Lukens AK, Masi D, Marcaurelle LA, Su XZ, Thomas CJ, Weïwer M, Wiegand RC, Wirth D, Xia M, Yuan J, Zhao J, Palmer M, Munoz B, Schreiber S.

ACS Med Chem Lett. 2012 Feb 9;3(2):112-117. Epub 2011 Dec 22.

18.

Development of small-molecule probes that selectively kill cells induced to express mutant RAS.

Weïwer M, Bittker JA, Lewis TA, Shimada K, Yang WS, MacPherson L, Dandapani S, Palmer M, Stockwell BR, Schreiber SL, Munoz B.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1822-6. doi: 10.1016/j.bmcl.2011.09.047. Epub 2011 Sep 28.

19.

Chemoenzymatic synthesis of uridine diphosphate-GlcNAc and uridine diphosphate-GalNAc analogs for the preparation of unnatural glycosaminoglycans.

Masuko S, Bera S, Green DE, Weïwer M, Liu J, DeAngelis PL, Linhardt RJ.

J Org Chem. 2012 Feb 3;77(3):1449-56. doi: 10.1021/jo202322k. Epub 2012 Jan 12.

20.

Unbiased binding assays for discovering small-molecule probes and drugs.

Kemp MM, Weïwer M, Koehler AN.

Bioorg Med Chem. 2012 Mar 15;20(6):1979-89. doi: 10.1016/j.bmc.2011.11.071. Epub 2011 Dec 24. Review.

PMID:
22230199
21.

A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.

Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, Weïwer M, Schreiber SL, Bradner JE, Koehler AN.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4164-9. doi: 10.1016/j.bmcl.2011.05.098. Epub 2011 Jun 2.

22.

Screen for RAS-Selective Lethal Compounds and VDAC Ligands - Probe 1.

Bittker JA, Weiwer M, Shimada K, Yang WS, MacPherson L, Dandapani S, Munoz B, Palmer M, Stockwell BR, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Mar 26 [updated 2011 Feb 10].

23.

Chemoenzymatic design of heparan sulfate oligosaccharides.

Liu R, Xu Y, Chen M, Weïwer M, Zhou X, Bridges AS, DeAngelis PL, Zhang Q, Linhardt RJ, Liu J.

J Biol Chem. 2010 Oct 29;285(44):34240-9. doi: 10.1074/jbc.M110.159152. Epub 2010 Aug 21.

24.

Inhibition of human vascular NADPH oxidase by apocynin derived oligophenols.

Mora-Pale M, Weïwer M, Yu J, Linhardt RJ, Dordick JS.

Bioorg Med Chem. 2009 Jul 15;17(14):5146-52. doi: 10.1016/j.bmc.2009.05.061. Epub 2009 May 30.

25.

Synthesis and Biological Evaluation of Non-Hydrolizable 1,2,3-Triazole Linked Sialic Acid Derivatives as Neuraminidase Inhibitors.

Weïwer M, Chen CC, Kemp MM, Linhardt RJ.

European J Org Chem. 2009 Jun;2009(16). doi: 10.1002/ejoc.200900117.

26.

Synthesis of uridine 5'-diphosphoiduronic acid: a potential substrate for the chemoenzymatic synthesis of heparin.

Weïwer M, Sherwood T, Green DE, Chen M, DeAngelis PL, Liu J, Linhardt RJ.

J Org Chem. 2008 Oct 3;73(19):7631-7. doi: 10.1021/jo801409c. Epub 2008 Aug 30.

27.

Oversulfated chondroitin sulfate: impact of a heparin impurity, associated with adverse clinical events, on low-molecular-weight heparin preparation.

Zhang Z, Weïwer M, Li B, Kemp MM, Daman TH, Linhardt RJ.

J Med Chem. 2008 Sep 25;51(18):5498-501. doi: 10.1021/jm800785t.

28.
29.

Lewis super-acid catalyzed cyclizations: a new route to fragrance compounds.

Coulombel L, Grau F, Weïwer M, Favier I, Chaminade X, Heumann A, Bayón JC, Aguirre PA, Duñach E.

Chem Biodivers. 2008 Jun;5(6):1070-82. doi: 10.1002/cbdv.200890086. Review.

PMID:
18618395
30.

Glycosylation in room temperature ionic liquid using unprotected and unactivated donors.

Park TJ, Weïwer M, Yuan X, Baytas SN, Munoz EM, Murugesan S, Linhardt RJ.

Carbohydr Res. 2007 Feb 26;342(3-4):614-20. Epub 2006 Nov 29.

31.

Regioselective indium(III) trifluoromethanesulfonate-catalyzed hydrothiolation of non-activated olefins.

Weïwer M, Coulombel L, Duñach E.

Chem Commun (Camb). 2006 Jan 21;(3):332-4. Epub 2005 Nov 29.

PMID:
16391751

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