Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 37

1.

Including explicit water molecules as part of the protein structure in MM/PBSA calculations.

Zhu YL, Beroza P, Artis DR.

J Chem Inf Model. 2014 Feb 24;54(2):462-9. doi: 10.1021/ci4001794. Epub 2014 Jan 16.

PMID:
24432790
2.

Thermodynamic and kinetic characterization of hydroxyethylamine β-secretase-1 inhibitors.

Mondal K, Regnstrom K, Morishige W, Barbour R, Probst G, Xu YZ, Artis DR, Yao N, Beroza P, Bova MP.

Biochem Biophys Res Commun. 2013 Nov 15;441(2):291-6. doi: 10.1016/j.bbrc.2013.09.081. Epub 2013 Sep 23.

PMID:
24070613
3.

Label free fragment screening using surface plasmon resonance as a tool for fragment finding - analyzing parkin, a difficult CNS target.

Regnström K, Yan J, Nguyen L, Callaway K, Yang Y, Diep L, Xing W, Adhikari A, Beroza P, Hom RK, Riley B, Rudolph D, Jobling MF, Baker J, Johnston J, Konradi A, Bova MP, Artis DR.

PLoS One. 2013 Jul 5;8(7):e66879. doi: 10.1371/journal.pone.0066879. Print 2013. Erratum in: PLoS One. 2013;8(7). doi:10.1371/annotation/590bbe38-3a12-45bd-bc5d-83b766c968b3. Artis, Rick D [corrected to Artis, Dean R].

4.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.

Ng RA, Sun M, Bowers S, Hom RK, Probst GD, John V, Fang LY, Maillard M, Gailunas A, Brogley L, Neitz RJ, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Adler M, Yao N, Zmolek W, Nakamura D, Quinn KP, Sauer JM, Bova MP, Ruslim L, Artis DR, Yednock TA.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4674-9. doi: 10.1016/j.bmcl.2013.06.006. Epub 2013 Jun 11.

PMID:
23856050
5.

Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.

Aubele DL, Hom RK, Adler M, Galemmo RA Jr, Bowers S, Truong AP, Pan H, Beroza P, Neitz RJ, Yao N, Lin M, Tonn G, Zhang H, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Diep L, Fitzgerald K, Hoffman J, Motter R, Fauss D, Tanaka P, Dappen M, Jagodzinski J, Chan W, Konradi AW, Latimer L, Zhu YL, Sham HL, Anderson JP, Bergeron M, Artis DR.

ChemMedChem. 2013 Aug;8(8):1295-313. doi: 10.1002/cmdc.201300166. Epub 2013 Jun 21.

PMID:
23794260
6.

Structure and function of Parkin E3 ubiquitin ligase reveals aspects of RING and HECT ligases.

Riley BE, Lougheed JC, Callaway K, Velasquez M, Brecht E, Nguyen L, Shaler T, Walker D, Yang Y, Regnstrom K, Diep L, Zhang Z, Chiou S, Bova M, Artis DR, Yao N, Baker J, Yednock T, Johnston JA.

Nat Commun. 2013;4:1982. doi: 10.1038/ncomms2982.

7.

Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.

Xu YZ, Yuan S, Bowers S, Hom RK, Chan W, Sham HL, Zhu YL, Beroza P, Pan H, Brecht E, Yao N, Lougheed J, Yan J, Tam D, Ren Z, Ruslim L, Bova MP, Artis DR.

Bioorg Med Chem Lett. 2013 May 15;23(10):3075-80. doi: 10.1016/j.bmcl.2013.03.009. Epub 2013 Mar 21.

PMID:
23570791
8.

Development of a novel β-secretase binding assay using the AlphaScreen platform.

Ren Z, Tam D, Xu YZ, Wone D, Yuan S, Sham HL, Cheung H, Regnstrom K, Chen X, Rudolph D, Jobling MF, Artis DR, Bova MP.

J Biomol Screen. 2013 Jul;18(6):695-704. doi: 10.1177/1087057113482138. Epub 2013 Mar 29.

PMID:
23543430
9.

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.

Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA Jr, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M.

Bioorg Med Chem Lett. 2013 May 1;23(9):2743-9. doi: 10.1016/j.bmcl.2013.02.065. Epub 2013 Feb 24.

PMID:
23522834
10.

Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor.

Zhang C, Ibrahim PN, Zhang J, Burton EA, Habets G, Zhang Y, Powell B, West BL, Matusow B, Tsang G, Shellooe R, Carias H, Nguyen H, Marimuthu A, Zhang KY, Oh A, Bremer R, Hurt CR, Artis DR, Wu G, Nespi M, Spevak W, Lin P, Nolop K, Hirth P, Tesch GH, Bollag G.

Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. doi: 10.1073/pnas.1219457110. Epub 2013 Mar 14.

11.

Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.

Bowers S, Xu YZ, Yuan S, Probst GD, Hom RK, Chan W, Konradi AW, Sham HL, Zhu YL, Beroza P, Pan H, Brecht E, Yao N, Lougheed J, Tam D, Ren Z, Ruslim L, Bova MP, Artis DR.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2181-6. doi: 10.1016/j.bmcl.2013.01.103. Epub 2013 Feb 4.

PMID:
23465612
12.

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.

Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7.

PMID:
21813278
13.

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.

Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1838-43. doi: 10.1016/j.bmcl.2011.01.046. Epub 2011 Jan 20.

PMID:
21316234
14.

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.

Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA Jr, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):315-9. doi: 10.1016/j.bmcl.2010.11.010. Epub 2010 Nov 5.

PMID:
21112785
15.

Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.

Hom RK, Bowers S, Sealy JM, Truong AP, Probst GD, Neitzel ML, Neitz RJ, Fang L, Brogley L, Wu J, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Quinn K, Sauer JM, Powell K, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7303-7. doi: 10.1016/j.bmcl.2010.10.066. Epub 2010 Oct 21.

PMID:
21071223
16.

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.

Bollag G, Hirth P, Tsai J, Zhang J, Ibrahim PN, Cho H, Spevak W, Zhang C, Zhang Y, Habets G, Burton EA, Wong B, Tsang G, West BL, Powell B, Shellooe R, Marimuthu A, Nguyen H, Zhang KY, Artis DR, Schlessinger J, Su F, Higgins B, Iyer R, D'Andrea K, Koehler A, Stumm M, Lin PS, Lee RJ, Grippo J, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, Chapman PB, Flaherty KT, Xu X, Nathanson KL, Nolop K.

Nature. 2010 Sep 30;467(7315):596-9. doi: 10.1038/nature09454.

17.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.

Probst GD, Bowers S, Sealy JM, Stupi B, Dressen D, Jagodzinska BM, Aquino J, Gailunas A, Truong AP, Tso L, Xu YZ, Hom RK, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Sham HL, Jagodzinski J, Toth G, Brecht E, Yao N, Pan H, Lin M, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Gauby S, Zmolek W, Quinn KP, Sauer JM.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6034-9. doi: 10.1016/j.bmcl.2010.08.070. Epub 2010 Aug 19.

PMID:
20822903
18.

Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.

Truong AP, Probst GD, Aquino J, Fang L, Brogley L, Sealy JM, Hom RK, Tucker JA, John V, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Tóth G, Yao N, Brecht E, Pan H, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Zmolek W, Quinn KP, Sauer JM.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4789-94. doi: 10.1016/j.bmcl.2010.06.112. Epub 2010 Jun 25.

PMID:
20634069
19.

Modulation of nutrient sensing nuclear hormone receptors promotes weight loss through appetite suppression in mice.

Perreault M, Will S, Panza D, Gareski T, Harding K, Kubasiak D, Jalenak M, Gartrell K, Wang S, Bollag G, Artis DR, Ibrahim PN, Womack P, Lin JJ, Saiah E, Mansour TS, Vlasuk GP, Erbe DV, Tobin JF.

Diabetes Obes Metab. 2010 Mar;12(3):234-45. doi: 10.1111/j.1463-1326.2009.01157.x.

PMID:
20152000
20.

Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent.

Artis DR, Lin JJ, Zhang C, Wang W, Mehra U, Perreault M, Erbe D, Krupka HI, England BP, Arnold J, Plotnikov AN, Marimuthu A, Nguyen H, Will S, Signaevsky M, Kral J, Cantwell J, Settachatgull C, Yan DS, Fong D, Oh A, Shi S, Womack P, Powell B, Habets G, West BL, Zhang KY, Milburn MV, Vlasuk GP, Hirth KP, Nolop K, Bollag G, Ibrahim PN, Tobin JF.

Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106. Epub 2008 Dec 30.

21.

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Tsai J, Lee JT, Wang W, Zhang J, Cho H, Mamo S, Bremer R, Gillette S, Kong J, Haass NK, Sproesser K, Li L, Smalley KS, Fong D, Zhu YL, Marimuthu A, Nguyen H, Lam B, Liu J, Cheung I, Rice J, Suzuki Y, Luu C, Settachatgul C, Shellooe R, Cantwell J, Kim SH, Schlessinger J, Zhang KY, West BL, Powell B, Habets G, Zhang C, Ibrahim PN, Hirth P, Artis DR, Herlyn M, Bollag G.

Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. doi: 10.1073/pnas.0711741105. Epub 2008 Feb 19.

22.

Comprehensive and quantitative mapping of energy landscapes for protein-protein interactions by rapid combinatorial scanning.

Pál G, Kouadio JL, Artis DR, Kossiakoff AA, Sidhu SS.

J Biol Chem. 2006 Aug 4;281(31):22378-85. Epub 2006 Jun 8.

23.

Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma.

Kumar A, Mandiyan V, Suzuki Y, Zhang C, Rice J, Tsai J, Artis DR, Ibrahim P, Bremer R.

J Mol Biol. 2005 Apr 22;348(1):183-93.

PMID:
15808862
24.

A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design.

Card GL, Blasdel L, England BP, Zhang C, Suzuki Y, Gillette S, Fong D, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY.

Nat Biotechnol. 2005 Feb;23(2):201-7. Epub 2005 Jan 30.

25.

A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.

Olivero AG, Eigenbrot C, Goldsmith R, Robarge K, Artis DR, Flygare J, Rawson T, Sutherlin DP, Kadkhodayan S, Beresini M, Elliott LO, DeGuzman GG, Banner DW, Ultsch M, Marzec U, Hanson SR, Refino C, Bunting S, Kirchhofer D.

J Biol Chem. 2005 Mar 11;280(10):9160-9. Epub 2005 Jan 4.

26.

Structural basis for the activity of drugs that inhibit phosphodiesterases.

Card GL, England BP, Suzuki Y, Fong D, Powell B, Lee B, Luu C, Tabrizizad M, Gillette S, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY.

Structure. 2004 Dec;12(12):2233-47.

27.

A glutamine switch mechanism for nucleotide selectivity by phosphodiesterases.

Zhang KY, Card GL, Suzuki Y, Artis DR, Fong D, Gillette S, Hsieh D, Neiman J, West BL, Zhang C, Milburn MV, Kim SH, Schlessinger J, Bollag G.

Mol Cell. 2004 Jul 23;15(2):279-86. Erratum in: Mol Cell. 2004 Aug 27;15(4):659.

28.

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
29.

Structure-based design of six novel classes of nonpeptide antagonists of the bradykinin B2 receptor.

Artis DR, Brotherton-Pleiss C, Pease JH, Lin CJ, Ferla SW, Newman SR, Bhakta S, Ostrelich H, Jarnagin K.

Bioorg Med Chem Lett. 2000 Nov 6;10(21):2421-5.

PMID:
11078192
30.

Receptor-binding conformation of the "ELR" motif of IL-8: X-ray structure of the L5C/H33C variant at 2.35 A resolution.

Gerber N, Lowman H, Artis DR, Eigenbrot C.

Proteins. 2000 Mar 1;38(4):361-7.

PMID:
10707023
31.

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
32.

Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.

Jackson DY, Quan C, Artis DR, Rawson T, Blackburn B, Struble M, Fitzgerald G, Chan K, Mullins S, Burnier JP, Fairbrother WJ, Clark K, Berisini M, Chui H, Renz M, Jones S, Fong S.

J Med Chem. 1997 Oct 10;40(21):3359-68.

PMID:
9341911
33.

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
34.
35.

Synthesis and Chemistry of Bicyclo[4.1.0]hept-1,6-ene.

Billups WE, Luo W, Lee GA, Chee J, Arney BE Jr, Wiberg KB, Artis DR.

J Org Chem. 1996 Jan 26;61(2):764-770.

PMID:
11667002
36.

Differential effect of halide anions on the hydrolysis of different dansyl substrates by thermolysin.

Yang JJ, Artis DR, Van Wart HE.

Biochemistry. 1994 May 31;33(21):6516-23.

PMID:
8204586
37.

Stimulation of prostaglandin D2 receptors on human platelets by analogs of prostacyclin.

Alvarez R, Eglen RM, Chang LF, Bruno JJ, Artis DR, Kluge AF, Whiting RL.

Prostaglandins. 1991 Aug;42(2):105-19. Erratum in: Prostaglandins 1991 Nov;42(5):487.

PMID:
1775633

Supplemental Content

Loading ...
Support Center