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Items: 34

1.

The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.

Wylie AA, Schoepfer J, Jahnke W, Cowan-Jacob SW, Loo A, Furet P, Marzinzik AL, Pelle X, Donovan J, Zhu W, Buonamici S, Hassan AQ, Lombardo F, Iyer V, Palmer M, Berellini G, Dodd S, Thohan S, Bitter H, Branford S, Ross DM, Hughes TP, Petruzzelli L, Vanasse KG, Warmuth M, Hofmann F, Keen NJ, Sellers WR.

Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22.

PMID:
28329763
2.

Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization.

Davies NG, Browne H, Davis B, Drysdale MJ, Foloppe N, Geoffrey S, Gibbons B, Hart T, Hubbard R, Jensen MR, Mansell H, Massey A, Matassova N, Moore JD, Murray J, Pratt R, Ray S, Robertson A, Roughley SD, Schoepfer J, Scriven K, Simmonite H, Stokes S, Surgenor A, Webb P, Wood M, Wright L, Brough P.

Bioorg Med Chem. 2012 Nov 15;20(22):6770-89. doi: 10.1016/j.bmc.2012.08.050. Epub 2012 Sep 4.

PMID:
23018093
3.

The G-protein-coupled estrogen receptor (GPER) is expressed in normal human ovaries and is upregulated in ovarian endometriosis and pelvic inflammatory disease involving the ovary.

Heublein S, Lenhard M, Vrekoussis T, Schoepfer J, Kuhn C, Friese K, Makrigiannakis A, Mayr D, Jeschke U.

Reprod Sci. 2012 Nov;19(11):1197-204. doi: 10.1177/1933719112446085. Epub 2012 May 9.

PMID:
22573494
4.

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.

Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F.

Cancer Res. 2011 Aug 1;71(15):5255-64. doi: 10.1158/0008-5472.CAN-10-4433. Epub 2011 Jun 22.

5.

Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800.

Massey AJ, Schoepfer J, Brough PA, Brueggen J, Chène P, Drysdale MJ, Pfaar U, Radimerski T, Ruetz S, Schweitzer A, Wood M, Garcia-Echeverria C, Jensen MR.

Mol Cancer Ther. 2010 Apr;9(4):906-19. doi: 10.1158/1535-7163.MCT-10-0055. Epub 2010 Apr 6.

6.

Anti-myeloma activity of the novel 2-aminothienopyrimidine Hsp90 inhibitor NVP-BEP800.

Stühmer T, Chatterjee M, Grella E, Seggewiss R, Langer C, Müller S, Schoepfer J, Garcia-Echeverria C, Quadt C, Jensen MR, Einsele H, Bargou RC.

Br J Haematol. 2009 Nov;147(3):319-27. doi: 10.1111/j.1365-2141.2009.07852.x. Epub 2009 Aug 13.

PMID:
19686236
7.

Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

Brough PA, Barril X, Borgognoni J, Chene P, Davies NG, Davis B, Drysdale MJ, Dymock B, Eccles SA, Garcia-Echeverria C, Fromont C, Hayes A, Hubbard RE, Jordan AM, Jensen MR, Massey A, Merrett A, Padfield A, Parsons R, Radimerski T, Raynaud FI, Robertson A, Roughley SD, Schoepfer J, Simmonite H, Sharp SY, Surgenor A, Valenti M, Walls S, Webb P, Wood M, Workman P, Wright L.

J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y.

PMID:
19610616
8.

Discovery of a new class of catalytic topoisomerase II inhibitors targeting the ATP-binding site by structure based design. Part I.

Furet P, Schoepfer J, Radimerski T, Chène P.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4014-7. doi: 10.1016/j.bmcl.2009.06.034. Epub 2009 Jun 13.

PMID:
19560355
9.

Catalytic inhibition of topoisomerase II by a novel rationally designed ATP-competitive purine analogue.

Chène P, Rudloff J, Schoepfer J, Furet P, Meier P, Qian Z, Schlaeppi JM, Schmitz R, Radimerski T.

BMC Chem Biol. 2009 Jan 7;9:1. doi: 10.1186/1472-6769-9-1.

10.

Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma.

Stühmer T, Zöllinger A, Siegmund D, Chatterjee M, Grella E, Knop S, Kortüm M, Unzicker C, Jensen MR, Quadt C, Chène P, Schoepfer J, García-Echeverría C, Einsele H, Wajant H, Bargou RC.

Leukemia. 2008 Aug;22(8):1604-12. doi: 10.1038/leu.2008.111. Epub 2008 May 15.

PMID:
18480838
11.

NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models.

Jensen MR, Schoepfer J, Radimerski T, Massey A, Guy CT, Brueggen J, Quadt C, Buckler A, Cozens R, Drysdale MJ, Garcia-Echeverria C, Chène P.

Breast Cancer Res. 2008;10(2):R33. doi: 10.1186/bcr1996. Epub 2008 Apr 22.

12.

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Furet P, Caravatti G, Guagnano V, Lang M, Meyer T, Schoepfer J.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.

PMID:
18248988
13.

Targeting Hsp90 for the treatment of cancer.

Drysdale MJ, Brough PA, Massey A, Jensen MR, Schoepfer J.

Curr Opin Drug Discov Devel. 2006 Jul;9(4):483-95. Review.

PMID:
16889231
14.

Inhibition of DNA helicases with DNA-competitive inhibitors.

Dubaele S, Jahnke W, Schoepfer J, Fuchs J, Chène P.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):923-7. Epub 2005 Nov 21.

PMID:
16300943
15.
16.

Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).

Sarno S, de Moliner E, Ruzzene M, Pagano MA, Battistutta R, Bain J, Fabbro D, Schoepfer J, Elliott M, Furet P, Meggio F, Zanotti G, Pinna LA.

Biochem J. 2003 Sep 15;374(Pt 3):639-46.

17.

Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking.

Vangrevelinghe E, Zimmermann K, Schoepfer J, Portmann R, Fabbro D, Furet P.

J Med Chem. 2003 Jun 19;46(13):2656-62.

PMID:
12801229
18.

Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.

Schoepfer J, Fretz H, Chaudhuri B, Muller L, Seeber E, Meijer L, Lozach O, Vangrevelinghe E, Furet P.

J Med Chem. 2002 Apr 25;45(9):1741-7.

PMID:
11960485
19.

Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne.

Schoepfer J, Gay B, End N, Muller E, Scheffel G, Caravatti G, Furet P.

Bioorg Med Chem Lett. 2001 May 7;11(9):1201-3.

PMID:
11354377
20.

Structure-based design of compounds inhibiting Grb2-SH2 mediated protein-protein interactions in signal transduction pathways.

Fretz H, Furet P, Garcia-Echeverria C, Schoepfer J, Rahuel J.

Curr Pharm Des. 2000 Dec;6(18):1777-96. Review.

PMID:
11102562
21.

Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1.

Furet P, Caravatti G, Denholm AA, Faessler A, Fretz H, García-Echeverría C, Gay B, Irving E, Press NJ, Rahuel J, Schoepfer J, Walker CV.

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2337-41.

PMID:
11055351
22.

Inhibition of cyclin-dependent kinase 4 (Cdk4) by fascaplysin, a marine natural product.

Soni R, Muller L, Furet P, Schoepfer J, Stephan C, Zumstein-Mecker S, Fretz H, Chaudhuri B.

Biochem Biophys Res Commun. 2000 Sep 7;275(3):877-84.

PMID:
10973815
23.

Novel Cdk inhibitors restore TGF-beta sensitivity in cdk4 overexpressing epithelial cells.

Soni R, Fretz H, Muller L, Schoepfer J, Chaudhuri B.

Biochem Biophys Res Commun. 2000 Jun 16;272(3):794-800.

PMID:
10860833
24.

Selective GRB2 SH2 inhibitors as anti-Ras therapy.

Gay B, Suarez S, Caravatti G, Furet P, Meyer T, Schoepfer J.

Int J Cancer. 1999 Oct 8;83(2):235-41.

25.

Effect of potent and selective inhibitors of the Grb2 SH2 domain on cell motility.

Gay B, Suarez S, Weber C, Rahuel J, Fabbro D, Furet P, Caravatti G, Schoepfer J.

J Biol Chem. 1999 Aug 13;274(33):23311-5.

26.

Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.

Furet P, García-Echeverría C, Gay B, Schoepfer J, Zeller M, Rahuel J.

J Med Chem. 1999 Jul 1;42(13):2358-63.

PMID:
10395476
27.

Highly potent inhibitors of the Grb2-SH2 domain.

Schoepfer J, Fretz H, Gay B, Furet P, García-Echeverría C, End N, Caravatti G.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):221-6.

PMID:
10021933
28.

Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain.

Schoepfer J, Gay B, Caravatti G, Garcia-Echeverria C, Fretz H, Rahuel J, Furet P.

Bioorg Med Chem Lett. 1998 Oct 20;8(20):2865-70.

PMID:
9873638
29.

Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.

Furet P, Gay B, Caravatti G, García-Echeverría C, Rahuel J, Schoepfer J, Fretz H.

J Med Chem. 1998 Aug 27;41(18):3442-9.

PMID:
9719597
30.

Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands.

Rahuel J, García-Echeverría C, Furet P, Strauss A, Caravatti G, Fretz H, Schoepfer J, Gay B.

J Mol Biol. 1998 Jun 19;279(4):1013-22.

PMID:
9642078
31.

Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.

García-Echeverría C, Furet P, Gay B, Fretz H, Rahuel J, Schoepfer J, Caravatti G.

J Med Chem. 1998 May 21;41(11):1741-4. No abstract available.

PMID:
9599224
32.

Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain.

Furet P, Gay B, García-Echeverría C, Rahuel J, Fretz H, Schoepfer J, Caravatti G.

J Med Chem. 1997 Oct 24;40(22):3551-6.

PMID:
9357522
33.

Dual specificity of Src homology 2 domains for phosphotyrosine peptide ligands.

Gay B, Furet P, García-Echeverría C, Rahuel J, Chène P, Fretz H, Schoepfer J, Caravatti G.

Biochemistry. 1997 May 13;36(19):5712-8.

PMID:
9153411
34.

Structural basis for specificity of Grb2-SH2 revealed by a novel ligand binding mode.

Rahuel J, Gay B, Erdmann D, Strauss A, Garcia-Echeverría C, Furet P, Caravatti G, Fretz H, Schoepfer J, Grütter MG.

Nat Struct Biol. 1996 Jul;3(7):586-9. No abstract available.

PMID:
8673601

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