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Items: 31


Parallel signaling through IRE1α and PERK regulates pancreatic neuroendocrine tumor growth and survival.

Moore PC, Qi JY, Thamsen M, Ghosh R, Peng J, Gliedt MJ, Meza-Acevedo R, Warren RE, Hiniker A, Kim GE, Maly DJ, Backes BJ, Papa FR, Oakes SA.

Cancer Res. 2019 Oct 31. pii: canres.1116.2019. doi: 10.1158/0008-5472.CAN-19-1116. [Epub ahead of print]


Development of a Chemical Toolset for Studying the Paralog-Specific Function of IRE1.

Feldman HC, Vidadala VN, Potter ZE, Papa FR, Backes BJ, Maly DJ.

ACS Chem Biol. 2019 Oct 14. doi: 10.1021/acschembio.9b00482. [Epub ahead of print]


Small molecule inhibition of IRE1α kinase/RNase has anti-fibrotic effects in the lung.

Thamsen M, Ghosh R, Auyeung VC, Brumwell A, Chapman HA, Backes BJ, Perara G, Maly DJ, Sheppard D, Papa FR.

PLoS One. 2019 Jan 9;14(1):e0209824. doi: 10.1371/journal.pone.0209824. eCollection 2019.


Fibroblast-specific inhibition of TGF-β1 signaling attenuates lung and tumor fibrosis.

Wei Y, Kim TJ, Peng DH, Duan D, Gibbons DL, Yamauchi M, Jackson JR, Le Saux CJ, Calhoun C, Peters J, Derynck R, Backes BJ, Chapman HA.

J Clin Invest. 2017 Oct 2;127(10):3675-3688. doi: 10.1172/JCI94624. Epub 2017 Sep 5.


Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes.

Morita S, Villalta SA, Feldman HC, Register AC, Rosenthal W, Hoffmann-Petersen IT, Mehdizadeh M, Ghosh R, Wang L, Colon-Negron K, Meza-Acevedo R, Backes BJ, Maly DJ, Bluestone JA, Papa FR.

Cell Metab. 2017 May 2;25(5):1207. doi: 10.1016/j.cmet.2017.04.026. No abstract available.


Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes.

Morita S, Villalta SA, Feldman HC, Register AC, Rosenthal W, Hoffmann-Petersen IT, Mehdizadeh M, Ghosh R, Wang L, Colon-Negron K, Meza-Acevedo R, Backes BJ, Maly DJ, Bluestone JA, Papa FR.

Cell Metab. 2017 Apr 4;25(4):883-897.e8. doi: 10.1016/j.cmet.2017.03.018. Erratum in: Cell Metab. 2017 May 2;25(5):1207.


Structural and Functional Analysis of the Allosteric Inhibition of IRE1α with ATP-Competitive Ligands.

Feldman HC, Tong M, Wang L, Meza-Acevedo R, Gobillot TA, Lebedev I, Gliedt MJ, Hari SB, Mitra AK, Backes BJ, Papa FR, Seeliger MA, Maly DJ.

ACS Chem Biol. 2016 Aug 19;11(8):2195-205. doi: 10.1021/acschembio.5b00940. Epub 2016 Jun 9.


Allosteric inhibition of the IRE1α RNase preserves cell viability and function during endoplasmic reticulum stress.

Ghosh R, Wang L, Wang ES, Perera BG, Igbaria A, Morita S, Prado K, Thamsen M, Caswell D, Macias H, Weiberth KF, Gliedt MJ, Alavi MV, Hari SB, Mitra AK, Bhhatarai B, Schürer SC, Snapp EL, Gould DB, German MS, Backes BJ, Maly DJ, Oakes SA, Papa FR.

Cell. 2014 Jul 31;158(3):534-48. doi: 10.1016/j.cell.2014.07.002. Epub 2014 Jul 10.


Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors.

Wang L, Perera BG, Hari SB, Bhhatarai B, Backes BJ, Seeliger MA, Schürer SC, Oakes SA, Papa FR, Maly DJ.

Nat Chem Biol. 2012 Dec;8(12):982-9. doi: 10.1038/nchembio.1094. Epub 2012 Oct 21.


IRE1α induces thioredoxin-interacting protein to activate the NLRP3 inflammasome and promote programmed cell death under irremediable ER stress.

Lerner AG, Upton JP, Praveen PV, Ghosh R, Nakagawa Y, Igbaria A, Shen S, Nguyen V, Backes BJ, Heiman M, Heintz N, Greengard P, Hui S, Tang Q, Trusina A, Oakes SA, Papa FR.

Cell Metab. 2012 Aug 8;16(2):250-64. doi: 10.1016/j.cmet.2012.07.007.


IRE1alpha kinase activation modes control alternate endoribonuclease outputs to determine divergent cell fates.

Han D, Lerner AG, Vande Walle L, Upton JP, Xu W, Hagen A, Backes BJ, Oakes SA, Papa FR.

Cell. 2009 Aug 7;138(3):562-75. doi: 10.1016/j.cell.2009.07.017.


Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy of enzymes associated with bradykinin-mediated angioedema.

Fryer RM, Segreti J, Banfor PN, Widomski DL, Backes BJ, Lin CW, Ballaron SJ, Cox BF, Trevillyan JM, Reinhart GA, von Geldern TW.

Br J Pharmacol. 2008 Mar;153(5):947-55. Epub 2007 Dec 17.


Synthesis of C-11 modified mifepristone analog libraries.

Hamilton GL, Backes BJ.

Mol Divers. 2007 May;11(2):107-11. Epub 2007 Jun 6.


Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.

Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM.

J Med Chem. 2007 Apr 19;50(8):1983-7. Epub 2007 Mar 17.


Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.

Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.


Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.

Backes BJ, Hamilton GL, Nguyen P, Wilcox D, Fung S, Wang J, Grynfarb M, Goos-Nilsson A, Jacobson PB, von Geldern TW.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):40-4. Epub 2006 Oct 5.


Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM.

J Med Chem. 2006 Nov 2;49(22):6439-42.


A strategy to profile prime and non-prime proteolytic substrate specificity.

Petrassi HM, Williams JA, Li J, Tumanut C, Ek J, Nakai T, Masick B, Backes BJ, Harris JL.

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3162-6.


Purifying the masses: integrating prepurification quality control, high-throughput LC/MS purification, and compound plating to feed high-throughput screening.

Isbell JJ, Zhou Y, Guintu C, Rynd M, Jiang S, Petrov D, Micklash K, Mainquist J, Ek J, Chang J, Weselak M, Backes BJ, Brailsford A, Shave D.

J Comb Chem. 2005 Mar-Apr;7(2):210-7.


Activity profile of dust mite allergen extract using substrate libraries and functional proteomic microarrays.

Harris J, Mason DE, Li J, Burdick KW, Backes BJ, Chen T, Shipway A, Van Heeke G, Gough L, Ghaemmaghami A, Shakib F, Debaene F, Winssinger N.

Chem Biol. 2004 Oct;11(10):1361-72.


Biochemical characterization of prostasin, a channel activating protease.

Shipway A, Danahay H, Williams JA, Tully DC, Backes BJ, Harris JL.

Biochem Biophys Res Commun. 2004 Nov 12;324(2):953-63.


Biochemical analysis of the 20 S proteasome of Trypanosoma brucei.

Wang CC, Bozdech Z, Liu CL, Shipway A, Backes BJ, Harris JL, Bogyo M.

J Biol Chem. 2003 May 2;278(18):15800-8. Epub 2003 Feb 24.


Expedient solid-phase synthesis of fluorogenic protease substrates using the 7-amino-4-carbamoylmethylcoumarin (ACC) fluorophore.

Maly DJ, Leonetti F, Backes BJ, Dauber DS, Harris JL, Craik CS, Ellman JA.

J Org Chem. 2002 Feb 8;67(3):910-5.


Substrate specificity of the human proteasome.

Harris JL, Alper PB, Li J, Rechsteiner M, Backes BJ.

Chem Biol. 2001 Dec;8(12):1131-41.


Chiral N-Acyl-tert-butanesulfinamides: The "Safety-Catch" Principle Applied to Diastereoselective Enolate Alkylations.

Backes BJ, Dragoli DR, Ellman JA.

J Org Chem. 1999 Jul 23;64(15):5472-5478.


From Split-Pool Libraries to Spatially Addressable Microarrays and Its Application to Functional Proteomic Profiling.

Winssinger N, Harris JL, Backes BJ, Schultz PG.

Angew Chem Int Ed Engl. 2001 Sep 3;40(17):3152-3155. doi: 10.1002/1521-3773(20010903)40:17<3152::AID-ANIE3152>3.0.CO;2-P.


Definition of the extended substrate specificity determinants for beta-tryptases I and II.

Harris JL, Niles A, Burdick K, Maffitt M, Backes BJ, Ellman JA, Kuntz I, Haak-Frendscho M, Craik CS.

J Biol Chem. 2001 Sep 14;276(37):34941-7. Epub 2001 Jul 3.


Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries.

Harris JL, Backes BJ, Leonetti F, Mahrus S, Ellman JA, Craik CS.

Proc Natl Acad Sci U S A. 2000 Jul 5;97(14):7754-9.


Synthesis of positional-scanning libraries of fluorogenic peptide substrates to define the extended substrate specificity of plasmin and thrombin.

Backes BJ, Harris JL, Leonetti F, Craik CS, Ellman JA.

Nat Biotechnol. 2000 Feb;18(2):187-93. Erratum in: Nat Biotechnol 2000 May;18(5):559.


Solid support linker strategies.

Backes BJ, Ellman JA.

Curr Opin Chem Biol. 1997 Jun;1(1):86-93. Review.


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