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Items: 16


Effects of Oncogenic Gαq and Gα11 Inhibition by FR900359 in Uveal Melanoma.

Lapadula D, Farias E, Randolph CE, Purwin TJ, McGrath D, Charpentier TH, Zhang L, Wu S, Terai M, Sato T, Tall GG, Zhou N, Wedegaertner PB, Aplin AE, Aguirre-Ghiso J, Benovic JL.

Mol Cancer Res. 2019 Apr;17(4):963-973. doi: 10.1158/1541-7786.MCR-18-0574. Epub 2018 Dec 19.


Potent and Selective Peptide-based Inhibition of the G Protein Gαq.

Charpentier TH, Waldo GL, Lowery-Gionta EG, Krajewski K, Strahl BD, Kash TL, Harden TK, Sondek J.

J Biol Chem. 2016 Dec 2;291(49):25608-25616. Epub 2016 Oct 14.


Small Molecule Inhibitors of Ca(2+)-S100B Reveal Two Protein Conformations.

Cavalier MC, Ansari MI, Pierce AD, Wilder PT, McKnight LE, Raman EP, Neau DB, Bezawada P, Alasady MJ, Charpentier TH, Varney KM, Toth EA, MacKerell AD Jr, Coop A, Weber DJ.

J Med Chem. 2016 Jan 28;59(2):592-608. doi: 10.1021/acs.jmedchem.5b01369. Epub 2016 Jan 13.


The experimental power of FR900359 to study Gq-regulated biological processes.

Schrage R, Schmitz AL, Gaffal E, Annala S, Kehraus S, Wenzel D, Büllesbach KM, Bald T, Inoue A, Shinjo Y, Galandrin S, Shridhar N, Hesse M, Grundmann M, Merten N, Charpentier TH, Martz M, Butcher AJ, Slodczyk T, Armando S, Effern M, Namkung Y, Jenkins L, Horn V, Stößel A, Dargatz H, Tietze D, Imhof D, Galés C, Drewke C, Müller CE, Hölzel M, Milligan G, Tobin AB, Gomeza J, Dohlman HG, Sondek J, Harden TK, Bouvier M, Laporte SA, Aoki J, Fleischmann BK, Mohr K, König GM, Tüting T, Kostenis E.

Nat Commun. 2015 Dec 14;6:10156. doi: 10.1038/ncomms10156.


Membrane-induced allosteric control of phospholipase C-β isozymes.

Charpentier TH, Waldo GL, Barrett MO, Huang W, Zhang Q, Harden TK, Sondek J.

J Biol Chem. 2014 Oct 24;289(43):29545-57. doi: 10.1074/jbc.M114.586784. Epub 2014 Sep 5.


A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformation.

Schmitz AL, Schrage R, Gaffal E, Charpentier TH, Wiest J, Hiltensperger G, Morschel J, Hennen S, Häußler D, Horn V, Wenzel D, Grundmann M, Büllesbach KM, Schröder R, Brewitz HH, Schmidt J, Gomeza J, Galés C, Fleischmann BK, Tüting T, Imhof D, Tietze D, Gütschow M, Holzgrabe U, Sondek J, Harden TK, Mohr K, Kostenis E.

Chem Biol. 2014 Jul 17;21(7):890-902. doi: 10.1016/j.chembiol.2014.06.003.


Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes.

Hajicek N, Charpentier TH, Rush JR, Harden TK, Sondek J.

Biochemistry. 2013 Jul 16;52(28):4810-9. doi: 10.1021/bi400433b. Epub 2013 Jul 9.


In vitro screening and structural characterization of inhibitors of the S100B-p53 interaction.

Wilder PT, Charpentier TH, Liriano MA, Gianni K, Varney KM, Pozharski E, Coop A, Toth EA, Mackerell AD, Weber DJ.

Int J High Throughput Screen. 2010 Jul 7;2010(1):109-126.


The effects of CapZ peptide (TRTK-12) binding to S100B-Ca2+ as examined by NMR and X-ray crystallography.

Charpentier TH, Thompson LE, Liriano MA, Varney KM, Wilder PT, Pozharski E, Toth EA, Weber DJ.

J Mol Biol. 2010 Mar 12;396(5):1227-43. doi: 10.1016/j.jmb.2009.12.057. Epub 2010 Jan 4.


Small molecules bound to unique sites in the target protein binding cleft of calcium-bound S100B as characterized by nuclear magnetic resonance and X-ray crystallography.

Charpentier TH, Wilder PT, Liriano MA, Varney KM, Zhong S, Coop A, Pozharski E, MacKerell AD Jr, Toth EA, Weber DJ.

Biochemistry. 2009 Jul 7;48(26):6202-12. doi: 10.1021/bi9005754.


Divalent metal ion complexes of S100B in the absence and presence of pentamidine.

Charpentier TH, Wilder PT, Liriano MA, Varney KM, Pozharski E, MacKerell AD Jr, Coop A, Toth EA, Weber DJ.

J Mol Biol. 2008 Sep 26;382(1):56-73. doi: 10.1016/j.jmb.2008.06.047. Epub 2008 Jun 24.


Structure of Ca2+-bound S100A4 and its interaction with peptides derived from nonmuscle myosin-IIA.

Malashkevich VN, Varney KM, Garrett SC, Wilder PT, Knight D, Charpentier TH, Ramagopal UA, Almo SC, Weber DJ, Bresnick AR.

Biochemistry. 2008 May 6;47(18):5111-26. doi: 10.1021/bi702537s. Epub 2008 Apr 15.


Getting a grip on calcium regulation.

Blaustein MP, Charpentier TH, Weber DJ.

Proc Natl Acad Sci U S A. 2007 Nov 20;104(47):18349-50. Epub 2007 Nov 14. No abstract available.


Hydrocarbon-stapled helices: a novel approach for blocking protein-protein interactions.

Wilder PT, Charpentier TH, Weber DJ.

ChemMedChem. 2007 Aug;2(8):1149-51. No abstract available.


Recognition of the tumor suppressor protein p53 and other protein targets by the calcium-binding protein S100B.

Wilder PT, Lin J, Bair CL, Charpentier TH, Yang D, Liriano M, Varney KM, Lee A, Oppenheim AB, Adhya S, Carrier F, Weber DJ.

Biochim Biophys Acta. 2006 Nov;1763(11):1284-97. Epub 2006 Aug 25.


Design of Inhibitors for S100B.

Markowitz J, Mackerell AD Jr, Carrier F, Charpentier TH, Weber DJ.

Curr Top Med Chem. 2005;5(12):1093-108. Review.


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