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Items: 25

1.

Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity.

Skepper CK, Moreau RJ, Appleton BA, Benton BM, Drumm JE 3rd, Feng BY, Geng M, Hu C, Li C, Lingel A, Lu Y, Mamo M, Mergo W, Mostafavi M, Rath CM, Steffek M, Takeoka KT, Uehara K, Wang L, Wei JR, Xie L, Xu W, Zhang Q, de Vicente J.

J Med Chem. 2018 Apr 26;61(8):3325-3349. doi: 10.1021/acs.jmedchem.7b01861. Epub 2018 Apr 13.

PMID:
29551072
2.

Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.

Moreau RJ, Skepper CK, Appleton BA, Blechschmidt A, Balibar CJ, Benton BM, Drumm JE 3rd, Feng BY, Geng M, Li C, Lindvall MK, Lingel A, Lu Y, Mamo M, Mergo W, Polyakov V, Smith TM, Takeoka K, Uehara K, Wang L, Wei JR, Weiss AH, Xie L, Xu W, Zhang Q, de Vicente J.

J Med Chem. 2018 Apr 26;61(8):3309-3324. doi: 10.1021/acs.jmedchem.7b01691. Epub 2018 Apr 9.

PMID:
29498517
3.

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
4.

Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.

Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S.

J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8.

PMID:
28557458
5.

Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.

Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D.

ACS Med Chem Lett. 2015 Aug 3;6(9):961-5. doi: 10.1021/ml500526p. eCollection 2015 Sep 10.

6.

Discovery of Potent and Selective RSK Inhibitors as Biological Probes.

Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Lindvall M, Appleton BA, Shafer CM.

J Med Chem. 2015 Sep 10;58(17):6766-83. doi: 10.1021/acs.jmedchem.5b00450. Epub 2015 Aug 13.

PMID:
26270416
7.

A structural portrait of the PDZ domain family.

Ernst A, Appleton BA, Ivarsson Y, Zhang Y, Gfeller D, Wiesmann C, Sidhu SS.

J Mol Biol. 2014 Oct 23;426(21):3509-19. doi: 10.1016/j.jmb.2014.08.012. Epub 2014 Aug 23.

PMID:
25158098
8.

Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers.

Aronchik I, Appleton BA, Basham SE, Crawford K, Del Rosario M, Doyle LV, Estacio WF, Lan J, Lindvall MK, Luu CA, Ornelas E, Venetsanakos E, Shafer CM, Jefferson AB.

Mol Cancer Res. 2014 May;12(5):803-12. doi: 10.1158/1541-7786.MCR-13-0595. Epub 2014 Feb 19.

9.

2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.

Costales A, Mathur M, Ramurthy S, Lan J, Subramanian S, Jain R, Atallah G, Setti L, Lindvall M, Appleton BA, Ornelas E, Feucht P, Warne B, Doyle L, Basham SE, Aronchik I, Jefferson AB, Shafer CM.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1592-6. doi: 10.1016/j.bmcl.2014.01.058. Epub 2014 Jan 30.

PMID:
24534486
10.

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.

Tiedt R, Degenkolbe E, Furet P, Appleton BA, Wagner S, Schoepfer J, Buck E, Ruddy DA, Monahan JE, Jones MD, Blank J, Haasen D, Drueckes P, Wartmann M, McCarthy C, Sellers WR, Hofmann F.

Cancer Res. 2011 Aug 1;71(15):5255-64. doi: 10.1158/0008-5472.CAN-10-4433. Epub 2011 Jun 22.

11.

Structure of IL-33 and its interaction with the ST2 and IL-1RAcP receptors--insight into heterotrimeric IL-1 signaling complexes.

Lingel A, Weiss TM, Niebuhr M, Pan B, Appleton BA, Wiesmann C, Bazan JF, Fairbrother WJ.

Structure. 2009 Oct 14;17(10):1398-410. doi: 10.1016/j.str.2009.08.009.

12.

Variants of the antibody herceptin that interact with HER2 and VEGF at the antigen binding site.

Bostrom J, Yu SF, Kan D, Appleton BA, Lee CV, Billeci K, Man W, Peale F, Ross S, Wiesmann C, Fuh G.

Science. 2009 Mar 20;323(5921):1610-4. doi: 10.1126/science.1165480.

13.

Inhibition of Wnt signaling by Dishevelled PDZ peptides.

Zhang Y, Appleton BA, Wiesmann C, Lau T, Costa M, Hannoush RN, Sidhu SS.

Nat Chem Biol. 2009 Apr;5(4):217-9. doi: 10.1038/nchembio.152. Epub 2009 Mar 1.

PMID:
19252499
14.

A specificity map for the PDZ domain family.

Tonikian R, Zhang Y, Sazinsky SL, Currell B, Yeh JH, Reva B, Held HA, Appleton BA, Evangelista M, Wu Y, Xin X, Chan AC, Seshagiri S, Lasky LA, Sander C, Boone C, Bader GD, Sidhu SS.

PLoS Biol. 2008 Sep 30;6(9):e239. doi: 10.1371/journal.pbio.0060239.

15.

Comprehensive analysis of the factors contributing to the stability and solubility of autonomous human VH domains.

Barthelemy PA, Raab H, Appleton BA, Bond CJ, Wu P, Wiesmann C, Sidhu SS.

J Biol Chem. 2008 Feb 8;283(6):3639-54. Epub 2007 Nov 28.

16.

Structural studies of neuropilin/antibody complexes provide insights into semaphorin and VEGF binding.

Appleton BA, Wu P, Maloney J, Yin J, Liang WC, Stawicki S, Mortara K, Bowman KK, Elliott JM, Desmarais W, Bazan JF, Bagri A, Tessier-Lavigne M, Koch AW, Wu Y, Watts RJ, Wiesmann C.

EMBO J. 2007 Nov 28;26(23):4902-12. Epub 2007 Nov 8.

17.

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.

18.

Structural and functional analysis of the ligand specificity of the HtrA2/Omi PDZ domain.

Zhang Y, Appleton BA, Wu P, Wiesmann C, Sidhu SS.

Protein Sci. 2007 Aug;16(8):1738-50.

19.

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.

20.

Convergent and divergent ligand specificity among PDZ domains of the LAP and zonula occludens (ZO) families.

Zhang Y, Yeh S, Appleton BA, Held HA, Kausalya PJ, Phua DC, Wong WL, Lasky LA, Wiesmann C, Hunziker W, Sidhu SS.

J Biol Chem. 2006 Aug 4;281(31):22299-311. Epub 2006 May 31.

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The cytomegalovirus DNA polymerase subunit UL44 forms a C clamp-shaped dimer.

Appleton BA, Loregian A, Filman DJ, Coen DM, Hogle JM.

Mol Cell. 2004 Jul 23;15(2):233-44.

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