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Items: 1 to 50 of 154

1.

A dual-readout F2 assay that combines fluorescence resonance energy transfer and fluorescence polarization for monitoring bimolecular interactions.

Du Y, Nikolovska-Coleska Z, Qui M, Li L, Lewis I, Dingledine R, Stuckey JA, Krajewski K, Roller PP, Wang S, Fu H.

Assay Drug Dev Technol. 2011 Aug;9(4):382-93. doi: 10.1089/adt.2010.0292. Epub 2011 Mar 11.

2.

Matriptase/epithin participates in mammary epithelial cell growth and morphogenesis through HGF activation.

Lee SL, Huang PY, Roller P, Cho EG, Park D, Dickson RB.

Mech Dev. 2010 Jan-Feb;127(1-2):82-95. doi: 10.1016/j.mod.2009.10.004. Epub 2009 Oct 22.

3.

Discovery of thioether-bridged cyclic pentapeptides binding to Grb2-SH2 domain with high affinity.

Jiang S, Liao C, Bindu L, Yin B, Worthy KW, Fisher RJ, Burke TR Jr, Nicklaus MC, Roller PP.

Bioorg Med Chem Lett. 2009 May 15;19(10):2693-8. doi: 10.1016/j.bmcl.2009.03.134. Epub 2009 Mar 29.

PMID:
19362470
4.

Interaction of a cyclic, bivalent smac mimetic with the x-linked inhibitor of apoptosis protein.

Nikolovska-Coleska Z, Meagher JL, Jiang S, Yang CY, Qiu S, Roller PP, Stuckey JA, Wang S.

Biochemistry. 2008 Sep 16;47(37):9811-24. doi: 10.1021/bi800785y. Epub 2008 Aug 22.

5.

Design and characterization of bivalent Smac-based peptides as antagonists of XIAP and development and validation of a fluorescence polarization assay for XIAP containing both BIR2 and BIR3 domains.

Nikolovska-Coleska Z, Meagher JL, Jiang S, Kawamoto SA, Gao W, Yi H, Qin D, Roller PP, Stuckey JA, Wang S.

Anal Biochem. 2008 Mar 1;374(1):87-98. Epub 2007 Nov 20.

PMID:
18023397
6.

Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP.

Sun H, Nikolovska-Coleska Z, Lu J, Meagher JL, Yang CY, Qiu S, Tomita Y, Ueda Y, Jiang S, Krajewski K, Roller PP, Stuckey JA, Wang S.

J Am Chem Soc. 2007 Dec 12;129(49):15279-94. Epub 2007 Nov 14.

7.

Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.

Li P, Jiang S, Lee SL, Lin CY, Johnson MD, Dickson RB, Michejda CJ, Roller PP.

J Med Chem. 2007 Nov 29;50(24):5976-83. Epub 2007 Nov 7.

PMID:
17985858
8.

Design and synthesis of paclitaxel conjugated with an ErbB2-recognizing peptide, EC-1.

Li P, Jiang S, Pero SC, Oligino L, Krag DN, Michejda CJ, Roller PP.

Biopolymers. 2007 Nov;87(4):225-30.

PMID:
17879382
9.

Calorimetric investigation of phosphorylated and non-phosphorylated peptide ligand binding to the human Grb7-SH2 domain.

Spuches AM, Argiros HJ, Lee KH, Haas LL, Pero SC, Krag DN, Roller PP, Wilcox DE, Lyons BA.

J Mol Recognit. 2007 Jul-Aug;20(4):245-52.

PMID:
17705331
10.

Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.

Tang G, Ding K, Nikolovska-Coleska Z, Yang CY, Qiu S, Shangary S, Wang R, Guo J, Gao W, Meagher J, Stuckey J, Krajewski K, Jiang S, Roller PP, Wang S.

J Med Chem. 2007 Jul 12;50(14):3163-6. Epub 2007 Jun 7.

11.

Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.

Chen J, Nikolovska-Coleska Z, Yang CY, Gomez C, Gao W, Krajewski K, Jiang S, Roller P, Wang S.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3939-42. Epub 2007 May 3.

PMID:
17513110
12.

Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.

Tang G, Yang CY, Nikolovska-Coleska Z, Guo J, Qiu S, Wang R, Gao W, Wang G, Stuckey J, Krajewski K, Jiang S, Roller PP, Wang S.

J Med Chem. 2007 Apr 19;50(8):1723-6. Epub 2007 Mar 23.

13.

Design and synthesis of redox stable analogues of sunflower trypsin inhibitors (SFTI-1) on solid support, potent inhibitors of matriptase.

Jiang S, Li P, Lee SL, Lin CY, Long YQ, Johnson MD, Dickson RB, Roller PP.

Org Lett. 2007 Jan 4;9(1):9-12.

PMID:
17192072
14.

Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.

Wang G, Nikolovska-Coleska Z, Yang CY, Wang R, Tang G, Guo J, Shangary S, Qiu S, Gao W, Yang D, Meagher J, Stuckey J, Krajewski K, Jiang S, Roller PP, Abaan HO, Tomita Y, Wang S.

J Med Chem. 2006 Oct 19;49(21):6139-42.

PMID:
17034116
15.

Covalent binding of the natural antimicrobial peptide indolicidin to DNA abasic sites.

Marchand C, Krajewski K, Lee HF, Antony S, Johnson AA, Amin R, Roller P, Kvaratskhelia M, Pommier Y.

Nucleic Acids Res. 2006;34(18):5157-65. Epub 2006 Sep 22.

16.

Design and concise synthesis of fully protected analogues of l-gamma-carboxyglutamic acid.

Jiang S, Li P, Lai CC, Kelley JA, Roller PP.

J Org Chem. 2006 Sep 15;71(19):7307-14.

PMID:
16958524
17.

Structure-based design of potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.

Jiang S, Li P, Peach ML, Bindu L, Worthy KW, Fisher RJ, Burke TR Jr, Nicklaus M, Roller PP.

Biochem Biophys Res Commun. 2006 Oct 20;349(2):497-503. Epub 2006 Aug 22.

PMID:
16945340
18.

Lipid metabolism in human endothelial cells.

Héliès-Toussaint C, Gambert S, Roller P, Tricot S, Lacour B, Grynberg A.

Biochim Biophys Acta. 2006 Jul;1761(7):765-74. Epub 2006 May 27.

PMID:
16843721
19.

Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.

Ding K, Lu Y, Nikolovska-Coleska Z, Wang G, Qiu S, Shangary S, Gao W, Qin D, Stuckey J, Krajewski K, Roller PP, Wang S.

J Med Chem. 2006 Jun 15;49(12):3432-5.

PMID:
16759082
20.

New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.

Krajewski K, Zhang Y, Parrish D, Deschamps J, Roller PP, Pathak VK.

Bioorg Med Chem Lett. 2006 Jun 1;16(11):3034-8. Epub 2006 Mar 9.

PMID:
16527484
21.
22.

Structure-based design of potent non-peptide MDM2 inhibitors.

Ding K, Lu Y, Nikolovska-Coleska Z, Qiu S, Ding Y, Gao W, Stuckey J, Krajewski K, Roller PP, Tomita Y, Parrish DA, Deschamps JR, Wang S.

J Am Chem Soc. 2005 Jul 27;127(29):10130-1.

PMID:
16028899
23.

Binding affinity difference induced by the stereochemistry of the sulfoxide bridge of the cyclic peptide inhibitors of Grb2-SH2 domain: NMR studies for the structural origin.

Shi YH, Song YL, Lin DH, Tan J, Roller PP, Li Q, Long YQ, Song GQ.

Biochem Biophys Res Commun. 2005 May 20;330(4):1254-61.

PMID:
15823578
24.

Structure-based design, synthesis and biochemical testing of novel and potent Smac peptido-mimetics.

Sun H, Nikolovska-Coleska Z, Chen J, Yang CY, Tomita Y, Pan H, Yoshioka Y, Krajewski K, Roller PP, Wang S.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):793-7.

PMID:
15664859
25.

Small nonphosphorylated Grb2-SH2 domain antagonists evaluated by surface plasmon resonance technology.

Lung FD, Chang CW, Chong MC, Liou CC, Li P, Peach ML, Nicklaus MC, Lou BS, Roller PP.

Biopolymers. 2005;80(5):628-35.

PMID:
15660381
26.

Structure-based design of potent, conformationally constrained Smac mimetics.

Sun H, Nikolovska-Coleska Z, Yang CY, Xu L, Liu M, Tomita Y, Pan H, Yoshioka Y, Krajewski K, Roller PP, Wang S.

J Am Chem Soc. 2004 Dec 29;126(51):16686-7.

PMID:
15612682
27.

Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.

Krajewski K, Marchand C, Long YQ, Pommier Y, Roller PP.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5595-8.

PMID:
15482931
28.

Structure-based discovery of nonpeptidic small organic compounds to block the T cell response to myelin basic protein.

Koehler NK, Yang CY, Varady J, Lu Y, Wu XW, Liu M, Yin D, Bartels M, Xu BY, Roller PP, Long YQ, Li P, Kattah M, Cohn ML, Moran K, Tilley E, Richert JR, Wang S.

J Med Chem. 2004 Oct 7;47(21):4989-97.

PMID:
15456243
29.

Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization.

Nikolovska-Coleska Z, Wang R, Fang X, Pan H, Tomita Y, Li P, Roller PP, Krajewski K, Saito NG, Stuckey JA, Wang S.

Anal Biochem. 2004 Sep 15;332(2):261-73.

PMID:
15325294
32.

Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.

Nikolovska-Coleska Z, Xu L, Hu Z, Tomita Y, Li P, Roller PP, Wang R, Fang X, Guo R, Zhang M, Lippman ME, Yang D, Wang S.

J Med Chem. 2004 May 6;47(10):2430-40.

PMID:
15115387
33.

Potentiating effect of distant sites in non-phosphorylated cyclic peptide antagonists of the Grb2-SH2 domain.

Long YQ, Guo R, Luo JH, Yang D, Roller PP.

Biochem Biophys Res Commun. 2003 Oct 17;310(2):334-40.

PMID:
14521914
34.

Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.

Krajewski K, Long YQ, Marchand C, Pommier Y, Roller PP.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3203-5.

PMID:
12951093
35.
36.

Concise and enantioselective synthesis of Fmoc-Pmp(But)2-OH and design of potent Pmp-containing Grb2-SH2 domain antagonists.

Li P, Zhang M, Peach ML, Liu H, Yang D, Roller PP.

Org Lett. 2003 Aug 21;5(17):3095-8.

PMID:
12916990
37.

Structural basis for a non-phosphorus-containing cyclic peptide binding to Grb2-SH2 domain with high affinity.

Li P, Zhang M, Peach ML, Zhang X, Liu H, Nicklaus M, Yang D, Roller PP.

Biochem Biophys Res Commun. 2003 Aug 8;307(4):1038-44.

PMID:
12878216
38.

Molecular mechanism of gossypol-induced cell growth inhibition and cell death of HT-29 human colon carcinoma cells.

Zhang M, Liu H, Guo R, Ling Y, Wu X, Li B, Roller PP, Wang S, Yang D.

Biochem Pharmacol. 2003 Jul 1;66(1):93-103.

PMID:
12818369
39.

Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.

Li P, Zhang M, Long YQ, Peach ML, Liu H, Yang D, Nicklaus M, Roller PP.

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2173-7.

PMID:
12798329
40.

Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain.

Li P, Peach ML, Zhang M, Liu H, Yang D, Nicklaus M, Roller PP.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):895-9.

PMID:
12617916
41.

Novel peptide inhibitors for Grb2 SH2 domain and their detection by surface plasmon resonance.

Lung FD, Tsai JY, Wei SY, Cheng JW, Chen C, Li P, Roller PP.

J Pept Res. 2002 Sep;60(3):143-9.

PMID:
12213123
42.

Cyclization strategies in peptide derived drug design.

Li P, Roller PP.

Curr Top Med Chem. 2002 Mar;2(3):325-41. Review.

PMID:
11944823
43.

Identification of novel non-phosphorylated ligands, which bind selectively to the SH2 domain of Grb7.

Pero SC, Oligino L, Daly RJ, Soden AL, Liu C, Roller PP, Li P, Krag DN.

J Biol Chem. 2002 Apr 5;277(14):11918-26. Epub 2002 Jan 24.

44.

Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.

Enyedy IJ, Ling Y, Nacro K, Tomita Y, Wu X, Cao Y, Guo R, Li B, Zhu X, Huang Y, Long YQ, Roller PP, Yang D, Wang S.

J Med Chem. 2001 Dec 6;44(25):4313-24.

PMID:
11728179
45.

Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.

Long YQ, Lee SL, Lin CY, Enyedy IJ, Wang S, Li P, Dickson RB, Roller PP.

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2515-9.

PMID:
11549459
46.

Oligomerization of human Gadd45a protein.

Kovalsky O, Lung FD, Roller PP, Fornace AJ Jr.

J Biol Chem. 2001 Oct 19;276(42):39330-9. Epub 2001 Aug 9.

47.

Functional preference of the constituent amino acid residues in a phage-library-based nonphosphorylated inhibitor of the Grb2-SH2 domain.

Lung FD, Long YQ, Roller PP, King CR, Varady J, Wu XW, Wang S.

J Pept Res. 2001 Jun;57(6):447-54.

PMID:
11437948
48.

Symptom management in older primary care patients: feasibility of an experimental, written self-disclosure protocol.

Klapow JC, Schmidt SM, Taylor LA, Roller P, Li Q, Calhoun JW, Wallander J, Pennebaker J.

Ann Intern Med. 2001 May 1;134(9 Pt 2):905-11.

PMID:
11346327
49.

Stability and peptide binding specificity of Btk SH2 domain: molecular basis for X-linked agammaglobulinemia.

Tzeng SR, Pai MT, Lung FD, Wu CW, Roller PP, Lei B, Wei CJ, Tu SC, Chen SH, Soong WJ, Cheng JW.

Protein Sci. 2000 Dec;9(12):2377-85.

50.

The central region of Gadd45 is required for its interaction with p21/WAF1.

Zhao H, Jin S, Antinore MJ, Lung FD, Fan F, Blanck P, Roller P, Fornace AJ Jr, Zhan Q.

Exp Cell Res. 2000 Jul 10;258(1):92-100.

PMID:
10912791

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