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Items: 1 to 50 of 60

1.

Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA.

Alexander MK, Miu A, Oh A, Reichelt M, Ho H, Chalouni C, Labadie S, Wang L, Liang J, Nickerson NN, Hu H, Yu L, Du M, Yan D, Park S, Kim J, Xu M, Sellers BD, Purkey HE, Skelton NJ, Koehler MFT, Payandeh J, Verma V, Xu Y, Koth CM, Nishiyama M.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01142-18. doi: 10.1128/AAC.01142-18. Print 2018 Nov.

PMID:
30104274
2.

Selectively Modulating Conformational States of USP7 Catalytic Domain for Activation.

Özen A, Rougé L, Bashore C, Hearn BR, Skelton NJ, Dueber EC.

Structure. 2018 Jan 2;26(1):72-84.e7. doi: 10.1016/j.str.2017.11.010. Epub 2017 Dec 14.

3.

Selective Homogeneous Assay for Circulating Endopeptidase Fibroblast Activation Protein (FAP).

Bainbridge TW, Dunshee DR, Kljavin NM, Skelton NJ, Sonoda J, Ernst JA.

Sci Rep. 2017 Oct 2;7(1):12524. doi: 10.1038/s41598-017-12900-8.

4.

Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.

Zhang Y, Ultsch M, Skelton NJ, Burdick DJ, Beresini MH, Li W, Kong-Beltran M, Peterson A, Quinn J, Chiu C, Wu Y, Shia S, Moran P, Di Lello P, Eigenbrot C, Kirchhofer D.

Nat Struct Mol Biol. 2017 Oct;24(10):848-856. doi: 10.1038/nsmb.3453. Epub 2017 Aug 21.

PMID:
28825733
5.

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2.

Foster SA, Whalen DM, Özen A, Wongchenko MJ, Yin J, Yen I, Schaefer G, Mayfield JD, Chmielecki J, Stephens PJ, Albacker LA, Yan Y, Song K, Hatzivassiliou G, Eigenbrot C, Yu C, Shaw AS, Manning G, Skelton NJ, Hymowitz SG, Malek S.

Cancer Cell. 2016 Apr 11;29(4):477-493. doi: 10.1016/j.ccell.2016.02.010. Epub 2016 Mar 17.

6.

Small-Molecule Library Subset Screening as an Aid for Accelerating Lead Identification.

Beresini MH, Liu Y, Dawes TD, Clark KR, Orren L, Schmidt S, Turincio R, Jones SW, Rodriguez RA, Thana P, Hascall D, Gross DP, Skelton NJ.

J Biomol Screen. 2014 Jun;19(5):758-70. doi: 10.1177/1087057114522515. Epub 2014 Feb 11.

PMID:
24518067
7.

Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Dragovich PS, Zhao G, Baumeister T, Bravo B, Giannetti AM, Ho YC, Hua R, Li G, Liang X, Ma X, O'Brien T, Oh A, Skelton NJ, Wang C, Wang W, Wang Y, Xiao Y, Yuen PW, Zak M, Zhao Q, Zheng X.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):954-62. doi: 10.1016/j.bmcl.2013.12.062. Epub 2013 Dec 21.

PMID:
24433859
8.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Giannetti AM, Zheng X, Skelton NJ, Wang W, Bravo BJ, Bair KW, Baumeister T, Cheng E, Crocker L, Feng Y, Gunzner-Toste J, Ho YC, Hua R, Liederer BM, Liu Y, Ma X, O'Brien T, Oeh J, Sampath D, Shen Y, Wang C, Wang L, Wu H, Xiao Y, Yuen PW, Zak M, Zhao G, Zhao Q, Dragovich PS.

J Med Chem. 2014 Feb 13;57(3):770-92. doi: 10.1021/jm4015108. Epub 2014 Jan 22.

PMID:
24405419
9.

Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor.

Zhang Y, Eigenbrot C, Zhou L, Shia S, Li W, Quan C, Tom J, Moran P, Di Lello P, Skelton NJ, Kong-Beltran M, Peterson A, Kirchhofer D.

J Biol Chem. 2014 Jan 10;289(2):942-55. doi: 10.1074/jbc.M113.514067. Epub 2013 Nov 13.

10.

Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.

Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K.

Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3.

11.

Disruption of PH-kinase domain interactions leads to oncogenic activation of AKT in human cancers.

Parikh C, Janakiraman V, Wu WI, Foo CK, Kljavin NM, Chaudhuri S, Stawiski E, Lee B, Lin J, Li H, Lorenzo MN, Yuan W, Guillory J, Jackson M, Rondon J, Franke Y, Bowman KK, Sagolla M, Stinson J, Wu TD, Wu J, Stokoe D, Stern HM, Brandhuber BJ, Lin K, Skelton NJ, Seshagiri S.

Proc Natl Acad Sci U S A. 2012 Nov 20;109(47):19368-73. doi: 10.1073/pnas.1204384109. Epub 2012 Nov 7.

12.

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.

PMID:
22934575
13.

Calcium-independent inhibition of PCSK9 by affinity-improved variants of the LDL receptor EGF(A) domain.

Zhang Y, Zhou L, Kong-Beltran M, Li W, Moran P, Wang J, Quan C, Tom J, Kolumam G, Elliott JM, Skelton NJ, Peterson AS, Kirchhofer D.

J Mol Biol. 2012 Oct 5;422(5):685-696. doi: 10.1016/j.jmb.2012.06.018. Epub 2012 Jun 21.

PMID:
22728257
14.

Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity.

Maurer T, Garrenton LS, Oh A, Pitts K, Anderson DJ, Skelton NJ, Fauber BP, Pan B, Malek S, Stokoe D, Ludlam MJ, Bowman KK, Wu J, Giannetti AM, Starovasnik MA, Mellman I, Jackson PK, Rudolph J, Wang W, Fang G.

Proc Natl Acad Sci U S A. 2012 Apr 3;109(14):5299-304. doi: 10.1073/pnas.1116510109. Epub 2012 Mar 19.

15.

Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Xu R, Banka A, Blake JF, Mitchell IS, Wallace EM, Bencsik JR, Kallan NC, Spencer KL, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26.

PMID:
21420856
16.

Discovery and SAR of spirochromane Akt inhibitors.

Kallan NC, Spencer KL, Blake JF, Xu R, Heizer J, Bencsik JR, Mitchell IS, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18.

PMID:
21392984
17.

Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Bencsik JR, Xiao D, Blake JF, Kallan NC, Mitchell IS, Spencer KL, Xu R, Gloor SL, Martinson M, Risom T, Woessner RD, Dizon F, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ, Prior WW, Murray LJ.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7037-41. doi: 10.1016/j.bmcl.2010.09.112. Epub 2010 Sep 29.

PMID:
20971641
18.

Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.

PMID:
20810279
19.

Noncompetitive inhibition of hepatocyte growth factor-dependent Met signaling by a phage-derived peptide.

Tam EM, Runyon ST, Santell L, Quan C, Yao X, Kirchhofer D, Skelton NJ, Lazarus RA.

J Mol Biol. 2009 Jan 9;385(1):79-90. doi: 10.1016/j.jmb.2008.09.091. Epub 2008 Oct 15.

PMID:
18973760
20.

Structural and functional analysis of the PDZ domains of human HtrA1 and HtrA3.

Runyon ST, Zhang Y, Appleton BA, Sazinsky SL, Wu P, Pan B, Wiesmann C, Skelton NJ, Sidhu SS.

Protein Sci. 2007 Nov;16(11):2454-71.

21.

Comparative structural analysis of the Erbin PDZ domain and the first PDZ domain of ZO-1. Insights into determinants of PDZ domain specificity.

Appleton BA, Zhang Y, Wu P, Yin JP, Hunziker W, Skelton NJ, Sidhu SS, Wiesmann C.

J Biol Chem. 2006 Aug 4;281(31):22312-20. Epub 2006 May 31.

22.

Structures of APRIL-receptor complexes: like BCMA, TACI employs only a single cysteine-rich domain for high affinity ligand binding.

Hymowitz SG, Patel DR, Wallweber HJ, Runyon S, Yan M, Yin J, Shriver SK, Gordon NC, Pan B, Skelton NJ, Kelley RF, Starovasnik MA.

J Biol Chem. 2005 Feb 25;280(8):7218-27. Epub 2004 Nov 12.

23.

Complex with a phage display-derived peptide provides insight into the function of insulin-like growth factor I.

Schaffer ML, Deshayes K, Nakamura G, Sidhu S, Skelton NJ.

Biochemistry. 2003 Aug 12;42(31):9324-34.

PMID:
12899619
24.
25.

Stability of cyclic beta-hairpins: asymmetric contributions from side chains of a hydrogen-bonded cross-strand residue pair.

Russell SJ, Blandl T, Skelton NJ, Cochran AG.

J Am Chem Soc. 2003 Jan 15;125(2):388-95.

PMID:
12517150
26.

Origins of PDZ domain ligand specificity. Structure determination and mutagenesis of the Erbin PDZ domain.

Skelton NJ, Koehler MF, Zobel K, Wong WL, Yeh S, Pisabarro MT, Yin JP, Lasky LA, Sidhu SS.

J Biol Chem. 2003 Feb 28;278(9):7645-54. Epub 2002 Nov 20.

27.

Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.

Dubree NJ, Artis DR, Castanedo G, Marsters J, Sutherlin D, Caris L, Clark K, Keating SM, Beresini MH, Chiu H, Fong S, Lowman HB, Skelton NJ, Jackson DY.

J Med Chem. 2002 Aug 1;45(16):3451-7.

PMID:
12139455
28.
29.

Rapid identification of small binding motifs with high-throughput phage display: discovery of peptidic antagonists of IGF-1 function.

Deshayes K, Schaffer ML, Skelton NJ, Nakamura GR, Kadkhodayan S, Sidhu SS.

Chem Biol. 2002 Apr;9(4):495-505.

30.

Amino acid determinants of beta-hairpin conformation in erythropoeitin receptor agonist peptides derived from a phage display library.

Skelton NJ, Russell S, de Sauvage F, Cochran AG.

J Mol Biol. 2002 Mar 8;316(5):1111-25.

PMID:
11884148
31.

Generation of an LFA-1 antagonist by the transfer of the ICAM-1 immunoregulatory epitope to a small molecule.

Gadek TR, Burdick DJ, McDowell RS, Stanley MS, Marsters JC Jr, Paris KJ, Oare DA, Reynolds ME, Ladner C, Zioncheck KA, Lee WP, Gribling P, Dennis MS, Skelton NJ, Tumas DB, Clark KR, Keating SM, Beresini MH, Tilley JW, Presta LG, Bodary SC.

Science. 2002 Feb 8;295(5557):1086-9.

32.

Crystal structure of human insulin-like growth factor-1: detergent binding inhibits binding protein interactions.

Vajdos FF, Ultsch M, Schaffer ML, Deshayes KD, Liu J, Skelton NJ, de Vos AM.

Biochemistry. 2001 Sep 18;40(37):11022-9.

PMID:
11551198
33.

A minimal peptide scaffold for beta-turn display: optimizing a strand position in disulfide-cyclized beta-hairpins.

Cochran AG, Tong RT, Starovasnik MA, Park EJ, McDowell RS, Theaker JE, Skelton NJ.

J Am Chem Soc. 2001 Jan 31;123(4):625-32.

PMID:
11456574
34.

Structure-function analysis of a phage display-derived peptide that binds to insulin-like growth factor binding protein 1.

Skelton NJ, Chen YM, Dubree N, Quan C, Jackson DY, Cochran A, Zobel K, Deshayes K, Baca M, Pisabarro MT, Lowman HB.

Biochemistry. 2001 Jul 24;40(29):8487-98.

PMID:
11456486
35.

Tryptophan zippers: stable, monomeric beta -hairpins.

Cochran AG, Skelton NJ, Starovasnik MA.

Proc Natl Acad Sci U S A. 2001 May 8;98(10):5578-83. Epub 2001 May 1. Erratum in: Proc Natl Acad Sci U S A 2002 Jun 25;99(13):9081.

36.

FIZZ1, a novel cysteine-rich secreted protein associated with pulmonary inflammation, defines a new gene family.

Holcomb IN, Kabakoff RC, Chan B, Baker TW, Gurney A, Henzel W, Nelson C, Lowman HB, Wright BD, Skelton NJ, Frantz GD, Tumas DB, Peale FV Jr, Shelton DL, Hébert CC.

EMBO J. 2000 Aug 1;19(15):4046-55.

37.

Peptide exosite inhibitors of factor VIIa as anticoagulants.

Dennis MS, Eigenbrot C, Skelton NJ, Ultsch MH, Santell L, Dwyer MA, O'Connell MP, Lazarus RA.

Nature. 2000 Mar 30;404(6777):465-70.

PMID:
10761907
38.

Characterization of the binding interface between the E-domain of staphylococcal protein A and an antibody Fv-fragment

Meininger DP, Rance M, Starovasnik MA, Fairbrother WJ, Skelton NJ.

Biochemistry. 2000 Feb 15;39(6):1541. No abstract available.

PMID:
10684636
39.

Characterization of the binding interface between the E-domain of Staphylococcal protein A and an antibody Fv-fragment.

Meininger DP, Rance M, Starovasnik MA, Fairbrother WJ, Skelton NJ.

Biochemistry. 2000 Jan 11;39(1):26-36. Erratum in: Biochemistry 2000 Feb 15;39(6):1541.

PMID:
10625476
40.

Solution structure of the VEGF-binding domain of Flt-1: comparison of its free and bound states.

Starovasnik MA, Christinger HW, Wiesmann C, Champe MA, de Vos AM, Skelton NJ.

J Mol Biol. 1999 Oct 29;293(3):531-44.

PMID:
10543948
41.

Structure of a CXC chemokine-receptor fragment in complex with interleukin-8.

Skelton NJ, Quan C, Reilly D, Lowman H.

Structure. 1999 Feb 15;7(2):157-68.

42.

Transfer of a protein binding epitope to a minimal designed peptide.

Quan C, Skelton NJ, Clark K, Jackson DY, Renz ME, Chiu HH, Keating SM, Beresini MH, Fong S, Artis DR.

Biopolymers. 1998;47(4):265-75.

PMID:
10036968
43.

Molecular mimics of insulin-like growth factor 1 (IGF-1) for inhibiting IGF-1: IGF-binding protein interactions.

Lowman HB, Chen YM, Skelton NJ, Mortensen DL, Tomlinson EE, Sadick MD, Robinson IC, Clark RG.

Biochemistry. 1998 Jun 23;37(25):8870-8.

PMID:
9636028
44.

High-resolution NMR structure and backbone dynamics of the Bacillus subtilis response regulator, Spo0F: implications for phosphorylation and molecular recognition.

Feher VA, Zapf JW, Hoch JA, Whiteley JM, McIntosh LP, Rance M, Skelton NJ, Dahlquist FW, Cavanagh J.

Biochemistry. 1997 Aug 19;36(33):10015-25.

PMID:
9254596
45.

Distinct but overlapping epitopes for the interaction of a CC-chemokine with CCR1, CCR3 and CCR5.

Pakianathan DR, Kuta EG, Artis DR, Skelton NJ, Hébert CA.

Biochemistry. 1997 Aug 12;36(32):9642-8.

PMID:
9289016
46.

Model peptide studies demonstrate that amphipathic secondary structures can be recognized by the chaperonin GroEL (cpn60).

Brazil BT, Cleland JL, McDowell RS, Skelton NJ, Paris K, Horowitz PM.

J Biol Chem. 1997 Feb 21;272(8):5105-11.

47.

Solution structure of the E-domain of staphylococcal protein A.

Starovasnik MA, Skelton NJ, O'Connell MP, Kelley RF, Reilly D, Fairbrother WJ.

Biochemistry. 1996 Dec 3;35(48):15558-69.

PMID:
8952510
48.

RhNGF slow unfolding is not due to proline isomerization: possibility of a cystine knot loop-threading mechanism.

De Young LR, Burton LE, Liu J, Powell MF, Schmelzer CH, Skelton NJ.

Protein Sci. 1996 Aug;5(8):1554-66.

49.

High-resolution solution structure of the EGF-like domain of heregulin-alpha.

Jacobsen NE, Abadi N, Sliwkowski MX, Reilly D, Skelton NJ, Fairbrother WJ.

Biochemistry. 1996 Mar 19;35(11):3402-17.

PMID:
8639490
50.

Determination of the solution structure of Apo calbindin D9k by NMR spectroscopy.

Skelton NJ, Kördel J, Chazin WJ.

J Mol Biol. 1995 Jun 2;249(2):441-62.

PMID:
7783203

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