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Items: 40

1.

Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader.

Potjewyd F, Turner AW, Beri J, Rectenwald JM, Norris-Drouin JL, Cholensky SH, Margolis DM, Pearce KH, Herring LE, James LI.

Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15. doi: 10.1016/j.chembiol.2019.11.006. Epub 2019 Dec 9.

PMID:
31831267
2.

Small molecule screening identifies inhibitors of the Epstein-Barr virus deubiquitinating enzyme, BPLF1.

Atkins SL, Motaib S, Wiser LC, Hopcraft SE, Hardy PB, Shackelford J, Foote P, Wade AH, Damania B, Pagano JS, Pearce KH, Whitehurst CB.

Antiviral Res. 2020 Jan;173:104649. doi: 10.1016/j.antiviral.2019.104649. Epub 2019 Nov 8.

3.

Targeting Regorafenib-Induced Toxicity through Inhibition of Gut Microbial β-Glucuronidases.

Ervin SM, Hanley RP, Lim L, Walton WG, Pearce KH, Bhatt AP, James LI, Redinbo MR.

ACS Chem Biol. 2019 Dec 20;14(12):2737-2744. doi: 10.1021/acschembio.9b00663. Epub 2019 Nov 12.

PMID:
31663730
4.

Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7.

Lamb KN, Bsteh D, Dishman SN, Moussa HF, Fan H, Stuckey JI, Norris JL, Cholensky SH, Li D, Wang J, Sagum C, Stanton BZ, Bedford MT, Pearce KH, Kenakin TP, Kireev DB, Wang GG, James LI, Bell O, Frye SV.

Cell Chem Biol. 2019 Oct 17;26(10):1365-1379.e22. doi: 10.1016/j.chembiol.2019.07.013. Epub 2019 Aug 15.

PMID:
31422906
5.

Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer.

Blake DR, Vaseva AV, Hodge RG, Kline MP, Gilbert TSK, Tyagi V, Huang D, Whiten GC, Larson JE, Wang X, Pearce KH, Herring LE, Graves LM, Frye SV, Emanuele MJ, Cox AD, Der CJ.

Sci Signal. 2019 Jul 16;12(590). pii: eaav7259. doi: 10.1126/scisignal.aav7259.

6.

A General TR-FRET Assay Platform for High-Throughput Screening and Characterizing Inhibitors of Methyl-Lysine Reader Proteins.

Rectenwald JM, Hardy PB, Norris-Drouin JL, Cholensky SH, James LI, Frye SV, Pearce KH.

SLAS Discov. 2019 Jul;24(6):693-700. doi: 10.1177/2472555219844569. Epub 2019 Apr 24.

7.

BacMam production and crystal structure of nonglycosylated apo human furin at 1.89 Å resolution.

Pearce KH, Overton LK, Gampe RT, Barrett GB, Taylor JD, McKee DD, Campobasso N, Nolte RT, Reid RA.

Acta Crystallogr F Struct Biol Commun. 2019 Apr 1;75(Pt 4):239-245. doi: 10.1107/S2053230X19001419. Epub 2019 Mar 13.

PMID:
30950824
8.

Inhibition of Inositol Polyphosphate Kinases by Quercetin and Related Flavonoids: A Structure-Activity Analysis.

Gu C, Stashko MA, Puhl-Rubio AC, Chakraborty M, Chakraborty A, Frye SV, Pearce KH, Wang X, Shears SB, Wang H.

J Med Chem. 2019 Feb 14;62(3):1443-1454. doi: 10.1021/acs.jmedchem.8b01593. Epub 2019 Jan 25.

9.

KRAS Suppression-Induced Degradation of MYC Is Antagonized by a MEK5-ERK5 Compensatory Mechanism.

Vaseva AV, Blake DR, Gilbert TSK, Ng S, Hostetter G, Azam SH, Ozkan-Dagliyan I, Gautam P, Bryant KL, Pearce KH, Herring LE, Han H, Graves LM, Witkiewicz AK, Knudsen ES, Pecot CV, Rashid N, Houghton PJ, Wennerberg K, Cox AD, Der CJ.

Cancer Cell. 2018 Nov 12;34(5):807-822.e7. doi: 10.1016/j.ccell.2018.10.001.

10.

Identification of Cosalane as an Inhibitor of Human and Murine CC-Chemokine Receptor 7 Signaling via a High-Throughput Screen.

Hull-Ryde EA, Porter MA, Fowler KA, Kireev D, Li K, Simpson CD, Sassano MF, Suto MJ, Pearce KH, Janzen W, Coghill JM.

SLAS Discov. 2018 Dec;23(10):1083-1091. doi: 10.1177/2472555218780917. Epub 2018 Jun 29.

PMID:
29958052
11.

Use of Protein Kinase-Focused Compound Libraries for the Discovery of New Inositol Phosphate Kinase Inhibitors.

Puhl-Rubio AC, Stashko MA, Wang H, Hardy PB, Tyagi V, Li B, Wang X, Kireev D, Jessen HJ, Frye SV, Shears SB, Pearce KH.

SLAS Discov. 2018 Oct;23(9):982-988. doi: 10.1177/2472555218775323. Epub 2018 May 29.

12.

Retraction: A High-Throughput Screening-Compatible Strategy for the Identification of Inositol Pyrophosphate Kinase Inhibitors.

Baughman BM, Wang H, An Y, Kireev D, Stashko MA, Jessen HJ, Pearce KH, Frye SV, Shears SB.

PLoS One. 2017 Jun 21;12(6):e0180272. doi: 10.1371/journal.pone.0180272. eCollection 2017. No abstract available.

13.

A High-Throughput Screening-Compatible Strategy for the Identification of Inositol Pyrophosphate Kinase Inhibitors.

Baughman BM, Wang H, An Y, Kireev D, Stashko MA, Jessen HJ, Pearce KH, Frye SV, Shears SB.

PLoS One. 2016 Oct 13;11(10):e0164378. doi: 10.1371/journal.pone.0164378. eCollection 2016. Retraction in: PLoS One. 2017 Jun 21;12 (6):e0180272.

14.

Structure-Activity Relationships and Kinetic Studies of Peptidic Antagonists of CBX Chromodomains.

Stuckey JI, Simpson C, Norris-Drouin JL, Cholensky SH, Lee J, Pasca R, Cheng N, Dickson BM, Pearce KH, Frye SV, James LI.

J Med Chem. 2016 Oct 13;59(19):8913-8923. Epub 2016 Sep 19.

15.

A neomorphic cancer cell-specific role of MAGE-A4 in trans-lesion synthesis.

Gao Y, Mutter-Rottmayer E, Greenwalt AM, Goldfarb D, Yan F, Yang Y, Martinez-Chacin RC, Pearce KH, Tateishi S, Major MB, Vaziri C.

Nat Commun. 2016 Jul 5;7:12105. doi: 10.1038/ncomms12105.

16.

DNA methylation status predicts cell type-specific enhancer activity.

Wiench M, John S, Baek S, Johnson TA, Sung MH, Escobar T, Simmons CA, Pearce KH, Biddie SC, Sabo PJ, Thurman RE, Stamatoyannopoulos JA, Hager GL.

EMBO J. 2011 Jun 24;30(15):3028-39. doi: 10.1038/emboj.2011.210.

17.

Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.

Chao EY, Caravella JA, Watson MA, Campobasso N, Ghisletti S, Billin AN, Galardi C, Wang P, Laffitte BA, Iannone MA, Goodwin BJ, Nichols JA, Parks DJ, Stewart E, Wiethe RW, Williams SP, Smallwood A, Pearce KH, Glass CK, Willson TM, Zuercher WJ, Collins JL.

J Med Chem. 2008 Sep 25;51(18):5758-65. doi: 10.1021/jm800612u.

PMID:
18800767
18.

Expression, purification, and characterization of multiple, multifunctional human glucocorticoid receptor proteins.

Simmons CA, Bledsoe RK, Guex N, Pearce KH.

Protein Expr Purif. 2008 Nov;62(1):29-35. doi: 10.1016/j.pep.2008.07.008. Epub 2008 Jul 30.

PMID:
18694832
19.

Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways.

Yin L, Wu N, Curtin JC, Qatanani M, Szwergold NR, Reid RA, Waitt GM, Parks DJ, Pearce KH, Wisely GB, Lazar MA.

Science. 2007 Dec 14;318(5857):1786-9. Epub 2007 Nov 15.

20.

Co-crystal structure guided array synthesis of PPARgamma inverse agonists.

Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18.

PMID:
17533125
21.

The nuclear receptor superfamily and drug discovery.

Moore JT, Collins JL, Pearce KH.

ChemMedChem. 2006 May;1(5):504-23. Review. No abstract available.

PMID:
16892386
22.

Recent applications of protein crystallography and structure-guided drug design.

Williams SP, Kuyper LF, Pearce KH.

Curr Opin Chem Biol. 2005 Aug;9(4):371-80. Review.

PMID:
16006182
23.

A ligand-mediated hydrogen bond network required for the activation of the mineralocorticoid receptor.

Bledsoe RK, Madauss KP, Holt JA, Apolito CJ, Lambert MH, Pearce KH, Stanley TB, Stewart EL, Trump RP, Willson TM, Williams SP.

J Biol Chem. 2005 Sep 2;280(35):31283-93. Epub 2005 Jun 20.

24.

Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.

Hoekstra WJ, Patel HS, Liang X, Blanc JB, Heyer DO, Willson TM, Iannone MA, Kadwell SH, Miller LA, Pearce KH, Simmons CA, Shearin J.

J Med Chem. 2005 Mar 24;48(6):2243-7.

PMID:
15771467
25.

Discovery of novel nuclear receptor modulating ligands: an integral role for peptide interaction profiling.

Pearce KH, Iannone MA, Simmons CA, Gray JG.

Drug Discov Today. 2004 Sep 1;9(17):741-51. Review.

PMID:
15450240
26.

Structure and function of the glucocorticoid receptor ligand binding domain.

Bledsoe RK, Stewart EL, Pearce KH.

Vitam Horm. 2004;68:49-91. Review.

PMID:
15193451
27.

Correlation between in vitro peptide binding profiles and cellular activities for estrogen receptor-modulating compounds.

Iannone MA, Simmons CA, Kadwell SH, Svoboda DL, Vanderwall DE, Deng SJ, Consler TG, Shearin J, Gray JG, Pearce KH.

Mol Endocrinol. 2004 May;18(5):1064-81. Epub 2004 Feb 19.

PMID:
14976226
28.

Identification of peptides that inhibit the DNA binding, trans-activator, and DNA replication functions of the human papillomavirus type 11 E2 protein.

Deng SJ, Pearce KH, Dixon EP, Hartley KA, Stanley TB, Lobe DC, Garvey EP, Kost TA, Petty RL, Rocque WJ, Alexander KA, Underwood MR.

J Virol. 2004 Mar;78(5):2637-41.

29.

Crystal structure of the glucocorticoid receptor ligand binding domain reveals a novel mode of receptor dimerization and coactivator recognition.

Bledsoe RK, Montana VG, Stanley TB, Delves CJ, Apolito CJ, McKee DD, Consler TG, Parks DJ, Stewart EL, Willson TM, Lambert MH, Moore JT, Pearce KH, Xu HE.

Cell. 2002 Jul 12;110(1):93-105.

PMID:
12151000
30.

Multiplexed molecular interactions of nuclear receptors using fluorescent microspheres.

Iannone MA, Consler TG, Pearce KH, Stimmel JB, Parks DJ, Gray JG.

Cytometry. 2001 Aug 1;44(4):326-37.

31.

A conserved residue at the extreme C-terminus of FtsZ is critical for the FtsA-FtsZ interaction in Staphylococcus aureus.

Yan K, Pearce KH, Payne DJ.

Biochem Biophys Res Commun. 2000 Apr 13;270(2):387-92.

PMID:
10753635
32.

Self-activation of guanosine triphosphatase activity by oligomerization of the bacterial cell division protein FtsZ.

Sossong TM Jr, Brigham-Burke MR, Hensley P, Pearce KH Jr.

Biochemistry. 1999 Nov 9;38(45):14843-50.

PMID:
10555966
33.

Growth hormone binding affinity for its receptor surpasses the requirements for cellular activity.

Pearce KH Jr, Cunningham BC, Fuh G, Teeri T, Wells JA.

Biochemistry. 1999 Jan 5;38(1):81-9.

PMID:
9890885
34.

Mutational analysis of thrombopoietin for identification of receptor and neutralizing antibody sites.

Pearce KH Jr, Potts BJ, Presta LG, Bald LN, Fendly BM, Wells JA.

J Biol Chem. 1997 Aug 15;272(33):20595-602.

35.

Structural and mutational analysis of affinity-inert contact residues at the growth hormone-receptor interface.

Pearce KH Jr, Ultsch MH, Kelley RF, de Vos AM, Wells JA.

Biochemistry. 1996 Aug 13;35(32):10300-7.

PMID:
8756685
37.

Comparison of the membrane binding kinetics of bovine prothrombin and its fragment 1.

Pearce KH, Hof M, Lentz BR, Thompson NL.

J Biol Chem. 1993 Nov 5;268(31):22984-91.

38.

Total internal reflection fluorescence microscopy: application to substrate-supported planar membranes.

Thompson NL, Pearce KH, Hsieh HV.

Eur Biophys J. 1993;22(5):367-78. Review.

PMID:
8112222
39.

Effect of bovine prothrombin fragment 1 on the translational diffusion of phospholipids in Langmuir-Blodgett monolayers.

Huang Z, Pearce KH, Thompson NL.

Biochim Biophys Acta. 1992 Dec 9;1112(2):259-65.

PMID:
1457457
40.

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