Bradley Backes, PhD
Associate Professor
Publications
Auyeung VC, Downey MS, Thamsen M, Wenger TA, Backes BJ, Sheppard D, Papa FR. IRE1α drives lung epithelial progenitor dysfunction to establish a niche for pulmonary fibrosis. 2022. PMID: 35170357
Feldman HC, Ghosh R, Auyeung VC, Mueller JL, Kim JH, Potter ZE, Vidadala VN, Perera BGK, Olivier A, Backes BJ, Zikherman J, Papa FR, Maly DJ. ATP-competitive partial antagonists of the IRE1α RNase segregate outputs of the UPR. Nature chemical biology 2021. PMID: 34556859
Deng Z, Chong Z, Law CS, Mukai K, Ho FO, Martinu T, Backes BJ, Eckalbar WL, Taguchi T, Shum AK. A defect in COPI-mediated transport of STING causes immune dysregulation in COPA syndrome. The Journal of experimental medicine 2020. PMID: 32725126
Yamashita Y, Morita S, Hosoi H, Kobata H, Kishimoto S, Ishibashi T, Mishima H, Kinoshita A, Backes BJ, Yoshiura KI, Papa FR, Sonoki T, Tamura S. Targeting Adaptive IRE1a Signaling and PLK2 in Multiple Myeloma: Possible Anti-Tumor Mechanisms of KIRA8 and Nilotinib. International journal of molecular sciences 2020. PMID: 32878237
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. Parallel signaling through IRE1a and PERK regulates pancreatic neuroendocrine tumor growth and survival. Cancer research 2019. PMID: 31672843
Feldman HC, Vidadala VN, Potter ZE, Papa FR, Backes BJ, Maly DJ. Development of a Chemical Toolset for Studying the Paralog-Specific Function of IRE1. ACS chemical biology 2019. PMID: 31609569
Thamsen M, Ghosh R, Auyeung VC, Brumwell A, Chapman HA, Backes BJ, Perara G, Maly DJ, Sheppard D, Papa FR. Small molecule inhibition of IRE1a kinase/RNase has anti-fibrotic effects in the lung. PloS one 2019. PMID: 30625178
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. Fibroblast-specific inhibition of TGF-ß1 signaling attenuates lung and tumor fibrosis. The Journal of clinical investigation 2017. PMID: 28872461
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. Targeting ABL-IRE1a Signaling Spares ER-Stressed Pancreatic ß Cells to Reverse Autoimmune Diabetes. Cell metabolism 2017. PMID: 28467938
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. Targeting ABL-IRE1a Signaling Spares ER-Stressed Pancreatic ß Cells to Reverse Autoimmune Diabetes. Cell metabolism 2017. PMID: 28380378
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. Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands. ACS chemical biology 2016. PMID: 27227314
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. Allosteric inhibition of the IRE1a RNase preserves cell viability and function during endoplasmic reticulum stress. Cell 2014. PMID: 25018104
Wang L, Perera BG, Hari SB, Bhhatarai B, Backes BJ, Seeliger MA, Schürer SC, Oakes SA, Papa FR, Maly DJ. Divergent allosteric control of the IRE1a endoribonuclease using kinase inhibitors. Nature chemical biology 2012. PMID: 23086298
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. IRE1a induces thioredoxin-interacting protein to activate the NLRP3 inflammasome and promote programmed cell death under irremediable ER stress. Cell metabolism 2012. PMID: 22883233
Han D, Lerner AG, Vande Walle L, Upton JP, Xu W, Hagen A, Backes BJ, Oakes SA, Papa FR. IRE1alpha kinase activation modes control alternate endoribonuclease outputs to determine divergent cell fates. Cell 2009. PMID: 19665977
Fryer RM, Segreti J, Banfor PN, Widomski DL, Backes BJ, Lin CW, Ballaron SJ, Cox BF, Trevillyan JM, Reinhart GA, von Geldern TW. Effect of bradykinin metabolism inhibitors on evoked hypotension in rats: rank efficacy of enzymes associated with bradykinin-mediated angioedema. British journal of pharmacology 2007. PMID: 18084312
Hamilton GL, Backes BJ. Synthesis of C-11 modified mifepristone analog libraries. Molecular diversity 2007. PMID: 17549597
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. Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors. Journal of medicinal chemistry 2007. PMID: 17367123
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. Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit. Bioorganic & medicinal chemistry letters 2007. PMID: 17276063
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. 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 inhibi Journal of medicinal chemistry 2006. PMID: 17064063
Backes BJ, Hamilton GL, Nguyen P, Wilcox D, Fung S, Wang J, Grynfarb M, Goos-Nilsson A, Jacobson PB, von Geldern TW. Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists. Bioorganic & medicinal chemistry letters 2006. PMID: 17070047
Petrassi HM, Williams JA, Li J, Tumanut C, Ek J, Nakai T, Masick B, Backes BJ, Harris JL. A strategy to profile prime and non-prime proteolytic substrate specificity. Bioorganic & medicinal chemistry letters 2005. PMID: 15878267
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. Purifying the masses: integrating prepurification quality control, high-throughput LC/MS purification, and compound plating to feed high-throughput screening. Journal of combinatorial chemistry 2005. PMID: 15762748
Shipway A, Danahay H, Williams JA, Tully DC, Backes BJ, Harris JL. Biochemical characterization of prostasin, a channel activating protease. Biochemical and biophysical research communications 2004. PMID: 15474520
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. Activity profile of dust mite allergen extract using substrate libraries and functional proteomic microarrays. Chemistry & biology 2004. PMID: 15489163
Wang CC, Bozdech Z, Liu CL, Shipway A, Backes BJ, Harris JL, Bogyo M. Biochemical analysis of the 20 S proteasome of Trypanosoma brucei. The Journal of biological chemistry 2003. PMID: 12600991
Maly DJ, Leonetti F, Backes BJ, Dauber DS, Harris JL, Craik CS, Ellman JA. Expedient solid-phase synthesis of fluorogenic protease substrates using the 7-amino-4-carbamoylmethylcoumarin (ACC) fluorophore. The Journal of organic chemistry 2002. PMID: 11856036
Harris JL, Alper PB, Li J, Rechsteiner M, Backes BJ. Substrate specificity of the human proteasome. Chemistry & biology 2001. PMID: 11755392
Winssinger N, Harris JL, Backes BJ, Schultz PG. From Split-Pool Libraries to Spatially Addressable Microarrays and Its Application to Functional Proteomic Profiling. Angewandte Chemie (International ed. in English) 2001. PMID: 29712061
Harris JL, Niles A, Burdick K, Maffitt M, Backes BJ, Ellman JA, Kuntz I, Haak-Frendscho M, Craik CS. Definition of the extended substrate specificity determinants for beta-tryptases I and II. The Journal of biological chemistry 2001. PMID: 11438529
Harris JL, Backes BJ, Leonetti F, Mahrus S, Ellman JA, Craik CS. Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries. Proceedings of the National Academy of Sciences of the United States of America 2000. PMID: 10869434
Backes BJ, Harris JL, Leonetti F, Craik CS, Ellman JA. Synthesis of positional-scanning libraries of fluorogenic peptide substrates to define the extended substrate specificity of plasmin and thrombin. Nature biotechnology 2000. PMID: 10657126
Backes BJ, Dragoli DR, Ellman JA. Chiral N-Acyl-tert-butanesulfinamides: The "Safety-Catch" Principle Applied to Diastereoselective Enolate Alkylations. The Journal of organic chemistry 1999. PMID: 11674609
Backes BJ, Ellman JA. Solid support linker strategies. Current opinion in chemical biology 1997. PMID: 9667836