Recent Publications from the Degterev Lab


Research Publications Cell Biology Neuroscience Pharmacology


Tabtieng T, Degterev A, Gaglia MM. 2018. Caspase-dependent suppression of type I interferon signaling promotes KSHV lytic replication. J Virol. Epub ahead of print.  books

Pattni BS, Jhaveri A, Dutta I, Baleja JD, Degterev A, Torchilin V. 2017. Targeting energy metabolism of cancer cells: Combined administration of NCL-240 and 2-DG. Int J Parm. Epub ahead of print.  books

Lule S, Wu L, McAllister LM, Edmiston WJ 3rd, Chung JY, Levy E, Zheng Y, Gough PJ, Bertin J, Degterev A, Lo EH, Whalen MJ. 2017. Genetic inhibition of receptor interacting protein kinase-1 reduces cell death and improves functional outcome after intracerebral hemorrhage in mice. Stroke Epub ahead of print. books

Saleh D, Najjar M, Zelic M, Shah S, Nogusa S, Polykratis A, Paczosa MK, Gough PJ, Bertin J, Whalen M, Fitzgerald KA, Slavov N, Pasparakis M, Balachandran S, Kelliher M, Mecsas J, Degterev A. 2017. Kinase activities of RIPK1 and RIPK3 can direct IFN-β synthesis induced by lipopolysaccharide. J Immunol. 198: 4435-4447.  books

Wegner KW, Saleh D, Degterev A. 2017. Complex pathologic roles of RIPK1 and RIPK3: Moving beyond necroptosis. Trends Pharmacol Sci. 38: 202-225.  books

Pattni BS, Nagelli SG, Aryasomayajula B, Deshpande PP, Kulkarni A, Hartner WC, Thakur G, Degterev A, Torchilin VP. 2016. Targeting of micelles and liposomes loaded with the pro-apoptotic drug, NCL-240, into NCI/ADR-RES cells in a 3D spheroid model. Pharm Res. 33: 2540-2551.  books

Najjar M*, Saleh D*, Zelic M, Nogusa S, Shah A, Tai A, Finger JN, Polykratis A, Gough PJ, Bertin J, Whalen M, Pasparakis, Balachandran S, Kelliher M, Poltorak A, Degterev A. 2016. RIPK1 and RIPK3 kinases promote cell death-independent inflammation by TLR4-TRIF. Immunity. 45: 46-59. * equal contribution. books

Degterev A, Linkermann A. 2016. Generation of small molecules to interfere with regulated necrosis. Cell Mol Life Sci. 73: 2251-2267.  books

Riehle R, Pattni B, Jhaveri A, Kulkarni A, Thakur G, Degterev A, Torchilin V. 2016. Combination nanopreparations of a novel proapoptotic drug - NCL-240, TRAIL and siRNA. Pharm Res. 33: 1587-1601.  books

Sriraman SK, Geraldo V, Luther E, Degterev A, Torchilin V. 2015. Cytotoxicity of PEGylated liposomes co-loaded with novel pro-apoptotic drug NCL-240 and the MEK inhibitor cobimetinib against colon carcinoma in vitro. J Control Release 220: 160-168.  books

Bullock AN, Degterev A. 2015. Targeting RIPK1,2,3 to combat inflammation. Oncotarget. 6: 34057-34058. books

Saleh D, Degterev A. 2015. Emerging roles for RIPK1 and RIPK3 in pathogen-induced cell death and host immunity. Curr Topics Microbiol Immunol. Epub ahead of print.   books

Canning P, Ruan Q, Schwerd T, Hrdinka M, Maki JL, Saleh D, Suebsuwong C, Ray S, Brennan PE, Cuny GD, Uhlig HH, Gyrd-Hansen M, Degterev A, Bullock AN. 2015. Inflammatory signaling by NOD-RIPK2 ss inhibited by clinically relevant type II kinase inhibitors. Chem Bio. 22: 1174-1184. Abstract in PubMed

Najjar M, Suebsuwong C, Ray SS, Thapa RJ, Maki JL, Nogusa S, Shah S, Saleh D, Gough PJ, Bertin J, Yuan J, Balachandran S, Cuny GD, Degterev A. 2015. Structure guided design of potent and selective ponatinib-based hybrid inhibitors for RIPK1. Cell Rep. 10: 1850-1860. books

Degterev A, Zhou W, Maki JL, Yuan J. 2014. Assays for necroptosis and activity of RIP kinases. Methods Enzymol. 545:1-33. books

Zhu X, Park J, Golinski J, Qiu J, Khuman J, Lee CC, Lo EH, Degterev A, Whalen MJ. 2014. Role of Akt and mammalian target of rapamycin in functional outcome after concussive brain injury in mice. J Cereb Blood Flow Metab. 34: 1531-1539. books

Dvoriantchikova G, Degterev A, Ivanov D. 2014. Retinal ganglion cell (RGC) programmed necrosis contributes to ischemia-reperfusion-induced retinal damage. Exp Eye Res. 123: 1-7. books

Schworer SA, Smirnova II, Kurbatova I, Bagina U, Churova M, Fowler T, Roy AL, Degterev A, Poltorak A. 2014. Toll-like receptor-mediated downregulation of the deubiquitinase CYLD protects macrophages from necroptosis in wild-derived mice. J Biol Chem. 289: 14422-14433. books

Newton K, Hildebrand JM, Shen Z, Rodriguez D, Alvarez-Diaz S, Petersen S, Shah S, Dugger DL, Huang C, Auwerx J, Vandenabeele P, Green DR, Ashkenazi A, Dixit VM, Kaiser WJ, Strasser A, Degterev A, Silke J. 2014. Is SIRT2 required for necroptosis? Nature 506: E4-E6. books

Liu Q, Qiu J, Liang M, Golinski J, van Leyen K, Jung JE, You Z, Lo EH, Degterev A, Whalen MJ. 2013. Akt and mTOR mediate programmed necrosis in neurons. Cell Death Dis. 5: e1084. books

Thapa RJ, Nogusa S, Chen P, Maki JL, Lerro A, Andrake M, Rall GF, Degterev A, Balachandran S.2013. Interferon-induced RIP1/RIP3-mediated necrosis requires PKR and is licensed by FADD and caspases. Proc Natl Acad Sci USA 110: E3109-E3118. books

Riehle RD, Cornea S, Degterev A. 2013. Role of phosphatidylinositol 3,4,5-trisphosphate in cell signaling. Adv Exp Med Biol. 991: 105-139. books

Riehle RD, Cornea S, Degterev A, Torchilin V. 2013. Micellar formulations of pro-apoptotic DM-PIT-1 analogs and TRAIL in vitro and in vivo. Drug Deliv. 20: 78-85. books

Maki JL, Degterev A. 2013. Activity assays for receptor-interacting protein kinase 1:a key regulator of necroptosis. Methods Mol Biol. 1004: 31-42. books

Xie T, Peng W, Liu Y, Yan C, Maki J, Degterev A, Yuan J, Shi Y. 2013. Structural basis of RIP1 inhibition by necrostatins. Structure 21: 493-499. books

Maki JL, Tres Brazell J, Teng X, Cuny GD, Degterev A. 2013. Expression and purification of active Receptor Interacting Protein 1 kinase using a baculovirus system. Protein Expr Purif. 89: 156-161. books

McNamara CR, Ahuja R, Osafo-Addo AD, Barrows D, Kettenbach A, Skidan I, Teng X, Cuny GD, Gerber S, Degterev A. 2013. Akt regulates TNFα synthesis downstream of RIP1 kinase activation during necroptosis. PLoS One 8: e56576. books

Degterev A, Huang Z, Boyce M, Li Y, Jagtap P, Mizushima N, Cuny GD, Mitchison TJ, Moskowitz MA, Yuan J. 2013. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 9: 192. books

Degterev A, Maki JL, Yuan J. 2013. Activity and specificity of necrostatin-1, small-molecule inhibitor of RIP1 kinase. Cell Death Differ. 20: 366. books

Takahashi N, Duprez L, Grootjans S, Cauwels A, Nerinckx W, Duhadaway JB, Goossens V, Roelandt R, Van Hauwermeiren F, Libert C, Declercq W, Callewaert N, Prendergast GC, Degterev A, Yuan J, Vandenabeele P. 2012. Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models. Cell Death Dis. 3: e437. books

Choi S, Keys H, Staples RJ, Yuan J, Degterev A, Cuny GD. 2012. Optimization of tricyclic Nec-3 necroptosis inhibitors for in vitro liver microsomal stability. Bioorg Med Chem Lett. 22: 5685-5688. books

Maki JL, Smith EE, Teng X, Ray SS, Cuny GD, Degterev A. 2012. Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1. Anal Biochem. 427: 164-174. books

Miao B, Skidan I, Yang J, You Z, Fu X, Famulok M, Schaffhausen B, Torchilin V, Yuan J, Degterev A. 2012. Inhibition of cell migration by PITENINs: the role of ARF6. Oncogene 31: 4317-4332. books

Park J, Zhang J, Qiu J, Zhu X, Degterev A, Lo EH, Whalen MJ. 2012. Combination therapy targeting Akt and mammalian target of rapamycin improves functional outcome after controlled cortical impact in mice. J Cereb Blood Flow Metab. 32: 330-340. books

Ofengeim D, Shi P, Miao B, Fan J, Xia X, Fan Y, Lipinski MM, Hashimoto T, Polydoro M, Yuan J, Wong ST, Degterev A. 2012. Identification of small molecule inhibitors of neurite loss induced by Aβ peptide using high-content screening. J Biol Chem. 287: 8714-8723. books

Miao B, Skidan I, Yang J, You Z, Fu X, Famulok M, Schaffhausen B, Torchilin V, Yuan J, Degterev A. 2011. Inhibition of cell migration by PITENINs: the role of ARF6. Oncogene. 31: 4317-4332. books

Badr CE, Wurdinger T, Nilsson J, Niers JM, Whalen M, Degterev A, Tannous BA. 2011. Lanatoside C sensitizes glioblastoma cells to tumor necrosis factor-related apoptosis-inducing ligand and induces an alternative cell death pathway. Neuro Oncol. 13: 1213-1234. books

Miao B, Degterev A. 2011. Targeting phopshatidylinositol 3-kinase signaling with novel phosphatidylinositol 3,4,5-triphosphate antagonists. Autophagy. 7: 650-651.  books

Miao B, Skidan I, Yang J, Lugovskoy A, Reibarkh M, Long K, Brazell T, Durugkar KA, Maki J, Ramana CV, Schaffhausen B, Wagner G, Torchilin V, Yuan J, Degterev A. 2010. Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains. Proc Natl Acad Sci USA 107: 21026-21031. books

Huang Y, Zhou X, Miao B, Lipinski M, Zhang Y, Li F, Degterev A, Yuan J, Hu G, Wong ST. 2010. A computational framework for studying neuron morphology from in vitro high content neuron-based screening. J Neurosci Methods 190: 299-309. books

Rosenbaum DM, Degterev A, David J, Rosenbaum PS, Roth S, Grotta JC, Cuny GD, Yuan J, Savitz SI. 2010. Necroptosis, a novel form of caspase-independent cell death, contributes to neuronal damage in a retinal ischemia-reperfusion injury model. J Neurosci Res. 88: 156901576. books

Sánchez-Olea R, Calera MR, Degterev A. 2009. Molecular pathways involved in cell death after chemically induced DNA damage. EXS 99: 209-230. books

Hitomi J, Christofferson DE, Ng A, Yao J, Degterev A, Xavier RJ, Yuan J. 2008. Identification of a molecular signaling network that regulates a cellular necrotic cell death pathway. Cell 135: 1311-1323. books

Skidan I, Miao B, Thekkedath RV, Dholakia P, Degterev A, Torchilin V. 2009. In vitro cytotoxicity of novel pro-apoptotic agent DM-PIT-1 in PEG-PE-based micelles alone and in combination with TRAIL. Drug Deliv. 16:45-51. books

Miao B, Degterev A.  2008. Methods to analyze cellular necroptosis. Methods Mol Biol.  559: 79-93. books

Ch'en I, Beisner D, Degterev A, Lynch C, Yuan J, Hoffmann A,  Hedrick SM. 2008. A second form of T cell death regulated by caspase-8. Proc Natl Acad Sci USA 105: 17463-17468. books

Korkina O, Degterev A. 2009. Cell death: apoptosis and necrosis.  Wiley Encyclopedia of Chemical Biology.

Zheng W, Degterev A, Hsu E, Yuan J, Yuan C. 2008. Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7. Bioorg Med Chem Lett. 18: 4932-4935. books

You Z, Savitz S, Yang J, Degterev A, Yuan J, Cuny G, Moskowitz M, Whalen M. 2008. Necrostatin-1 reduces histopathology and improves functional outcome after controlled cortical impact in mice. J Cereb Blood Flow Metab. 28: 1564-1573. books

Cuny GD, Degterev A, Yuan J. 2008. Necroptosis – a novel cell death mechanism. Drugs of the Future 33: 225-233.

Teng X, Keys, H, Yuan J, Degterev A. Cuny GD. 2008. Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors. Bioorg Med Chem Lett. 18: 3219-3223. books

Degterev A, Yuan J. 2008. Expansion and evolution of cell death programs. Nat Reviews Mol Cell Biol. 9: 378-390. books

Degterev A, Hitomi J, Ch'en I, Germscheid M, Korkina O, Teng X, Cuny G, Yuan C, Wagner G, Hedrick S, Gerber S, Lugovskoy A, Yuan J. 2008. Identification of RIP1 kinase as a cellular target of necrostatins. Nat Chem Biol. 4: 313-321. books

Yi C, Sogah D, Boyce M, Degterev A, Christofferson D, Yuan J. 2007. A genome-wide RNAi screen reveals critical regulators of caspase activation. J. Cell Biol. 179: 619-626. books

Teng X, Keys H, Jeevanandam A, Porco J, Degterev A, Yuan J, Cuny G. 2007. Structure activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 17: 6836-6840. books

Jagtap P, Degterev A, Choi S, Keys H, Yuan J, Cuny G. 2007. Structure-activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 50: 1886-1895. books

Zhang Y, Zhou X, Degterev A, Lipinski M, Adjeroh D, Yuan J, Wong ST. 2007. Automated neurite extraction using dynamic programming for high-throughput screening of neuron-based assays. NeuroImage, 35: 1502-1515. books

Wang K, Li J, Degterev A, Hsu E, Yuan J, Yuan C. 2007. Structure-activity relationship analysis of a novel necroptosis inhibitor, Necrostatin-5. Bioorg Med Chem Lett. 17: 1455-1465. books

Moerke NJ, Aktas H, Chen H, Cantel S, Reibarkh MY, Fahmy A, Gross JD, Degterev A, Yuan J, Chorev M, Halperin JA, Wagner G. 2007. A small molecule inhibitor of the eIF4E/eIF4G interaction with anti-tumour activity. Cell 128: 257-267. books

Zhou X, Degterev A, Lipinski M, Adjeroh D, Yuan J, Wong ST. 2007. Automated neurite extraction using dynamic programming for high-throughput screening of neuron-based assays. NeuroImage 35: 1502-1515. books

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