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Items: 23

1.

Blockade of activin type II receptors with a dual anti-ActRIIA/IIB antibody is critical to promote maximal skeletal muscle hypertrophy.

Morvan F, Rondeau JM, Zou C, Minetti G, Scheufler C, Scharenberg M, Jacobi C, Brebbia P, Ritter V, Toussaint G, Koelbing C, Leber X, Schilb A, Witte F, Lehmann S, Koch E, Geisse S, Glass DJ, Lach-Trifilieff E.

Proc Natl Acad Sci U S A. 2017 Nov 21;114(47):12448-12453. doi: 10.1073/pnas.1707925114. Epub 2017 Nov 6.

2.

Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.

Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20.

PMID:
29107542
3.

Identification of a Novel Allosteric Inhibitory Site on Tryptophan Hydroxylase 1 Enabling Unprecedented Selectivity Over all Related Hydroxylases.

Petrassi M, Barber R, Be C, Beach S, Cox B, D'Souza AM, Duggan N, Hussey M, Fox R, Hunt P, Jarai G, Kosaka T, Oakley P, Patel V, Press N, Rowlands D, Scheufler C, Schmidt O, Srinivas H, Turner M, Turner R, Westwick J, Wolfreys A, Pathan N, Watson S, Thomas M.

Front Pharmacol. 2017 May 5;8:240. doi: 10.3389/fphar.2017.00240. eCollection 2017.

4.

Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.

Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C.

ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9.

5.

Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.

Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C.

ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11.

6.

Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket.

Scheufler C, Möbitz H, Gaul C, Ragot C, Be C, Fernández C, Beyer KS, Tiedt R, Stauffer F.

ACS Med Chem Lett. 2016 Jun 6;7(8):730-4. doi: 10.1021/acsmedchemlett.6b00168. eCollection 2016 Aug 11.

7.

Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.

Stauffer F, Cowan-Jacob SW, Scheufler C, Furet P.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2065-7. doi: 10.1016/j.bmcl.2016.02.074. Epub 2016 Feb 26.

PMID:
26951750
8.

Large scale meta-analysis of fragment-based screening campaigns: privileged fragments and complementary technologies.

Kutchukian PS, Wassermann AM, Lindvall MK, Wright SK, Ottl J, Jacob J, Scheufler C, Marzinzik A, Brooijmans N, Glick M.

J Biomol Screen. 2015 Jun;20(5):588-96. doi: 10.1177/1087057114565080. Epub 2014 Dec 30.

PMID:
25550355
9.

Applications of Biophysics in High-Throughput Screening Hit Validation.

Genick CC, Barlier D, Monna D, Brunner R, Bé C, Scheufler C, Ottl J.

J Biomol Screen. 2014 Jun;19(5):707-14. doi: 10.1177/1087057114529462. Epub 2014 Apr 2.

PMID:
24695619
10.

Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.

Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T.

Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3.

11.

Detecting S-adenosyl-L-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay.

Lin Y, Fan H, Frederiksen M, Zhao K, Jiang L, Wang Z, Zhou S, Guo W, Gao J, Li S, Harrington E, Meier P, Scheufler C, Xu YC, Atadja P, Lu C, Li E, Gu XJ.

Anal Biochem. 2012 Apr 1;423(1):171-7. doi: 10.1016/j.ab.2012.01.019. Epub 2012 Jan 27.

PMID:
22342622
12.

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.

Revesz L, Schlapbach A, Aichholz R, Feifel R, Hawtin S, Heng R, Hiestand P, Jahnke W, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4715-8. doi: 10.1016/j.bmcl.2010.04.024. Epub 2010 Apr 13.

PMID:
20594847
13.

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.

Revesz L, Schlapbach A, Aichholz R, Dawson J, Feifel R, Hawtin S, Littlewood-Evans A, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4719-23. doi: 10.1016/j.bmcl.2010.04.023. Epub 2010 Apr 11.

PMID:
20591669
14.

Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.

Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. doi: 10.1016/j.bmcl.2009.10.138. Epub 2009 Nov 3.

PMID:
20060294
15.

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.

Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R, Huppertz C.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6142-6. doi: 10.1016/j.bmcl.2008.10.039. Epub 2008 Oct 11.

PMID:
18945615
17.

Ligand discrimination by TPR domains. Relevance and selectivity of EEVD-recognition in Hsp70 x Hop x Hsp90 complexes.

Brinker A, Scheufler C, Von Der Mulbe F, Fleckenstein B, Herrmann C, Jung G, Moarefi I, Hartl FU.

J Biol Chem. 2002 May 31;277(22):19265-75. Epub 2002 Mar 4.

18.

Structure of interleukin 4 mutant E9A suggests polar steering in receptor-complex formation.

Hülsmeyer M, Scheufler C, Dreyer MK.

Acta Crystallogr D Biol Crystallogr. 2001 Sep;57(Pt 9):1334-6. Epub 2001 Aug 23.

PMID:
11526337
19.

Structure of a Bag/Hsc70 complex: convergent functional evolution of Hsp70 nucleotide exchange factors.

Sondermann H, Scheufler C, Schneider C, Hohfeld J, Hartl FU, Moarefi I.

Science. 2001 Feb 23;291(5508):1553-7.

20.

Structure of the molecular chaperone prefoldin: unique interaction of multiple coiled coil tentacles with unfolded proteins.

Siegert R, Leroux MR, Scheufler C, Hartl FU, Moarefi I.

Cell. 2000 Nov 10;103(4):621-32.

21.

Structure of TPR domain-peptide complexes: critical elements in the assembly of the Hsp70-Hsp90 multichaperone machine.

Scheufler C, Brinker A, Bourenkov G, Pegoraro S, Moroder L, Bartunik H, Hartl FU, Moarefi I.

Cell. 2000 Apr 14;101(2):199-210.

22.

Crystal structure of human bone morphogenetic protein-2 at 2.7 A resolution.

Scheufler C, Sebald W, Hülsmeyer M.

J Mol Biol. 1999 Mar 19;287(1):103-15.

PMID:
10074410
23.

[Quartz-dust determination in the dental technician's workplace].

Scheufler C, Knirck HD.

Zahntechnik (Berl). 1986 Mar;27(2):84-6. German. No abstract available.

PMID:
3022500

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