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Graduate School of Biomedical Sciences

Recent Publications from the Degterev Lab

Muendlein HI, Connolly WM, Magri Z, Jetton D, Smirnova I, Degterev A, Balachandran S, Poltorak A. 2022. ZBP1 promotes inflammatory responses downstream of TLR3/TLR4 via timely delivery of RIPK1 to TRIF. Proc Natl Acad Sci U S A. Jun 14;119(24):e2113872119. doi: 10.1073/pnas.2113872119. Abstract

Delanghe T, Huyghe J, Lee S, Priem D, Van Coillie S, Gilbert B, Choi SM, Vandenabeele P, Degterev A, Cuny GD, Dondelinger Y, Bertrand MJM. Antioxidant and food additive BHA prevents TNF cytotoxicity by acting as a direct RIPK1 inhibitor. Cell Death Dis. Jul 14;12(7):699. doi: 10.1038/s41419-021-03994-0. Abstract

Siokas I, Zhang D, Poltorak A, Muendlein H, Degterev A. 2021. Immunoprecipitation strategies to isolate RIPK1/RIPK3 complexes in mouse macrophages. Curr Protoc. Jun;1(6):e156. doi: 10.1002/cpz1.156. Abstract

Zelic M, Pontarelli F, Woodworth L, Zhu C, Mahan A, Ren Y, LaMorte M, Gruber R, Keane A, Loring P, Guo L, Xia TH, Zhang B, Orning P, Lien E, Degterev A, Hammond T, Ofengeim D. 2021. RIPK1 activation mediates neuroinflammation and disease progression in multiple sclerosis. Cell Rep. 35(6):109112. doi: 10.1016/j.celrep.2021.109112. Abstract

Nikhar S, Siokas I, Schlicher L, Lee S, Gyrd-Hansen M, Degterev A, Cuny GD. 2021. Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling. Eur J Med Chem. 215:113252. doi: 10.1016/j.ejmech.2021.113252. Abstract

Muendlein HI, Connolly WM, Magri Z, Smirnova I, Ilyukha V, Gautam A, Degterev A, Poltorak A. 2021. ZBP1 promotes LPS-induced cell death and IL-1β release via RHIM-mediated interactions with RIPK1. Nat Commun. 12(1):86. doi: 10.1038/s41467-020-20357-z. Abstract

Lule S, Wu L, Sarro-Schwartz A, Edmiston Iii WJ, Izzy S, Songtachalert T, Ahn SH, Fernandes ND, Jin G, Chung JY, Balachandran S, Lo EH, Kaplan D, Degterev A, Whalen MJ. 2020. Cell-specific activation of RIPK1 and MLKL after intracerebral hemorrhage in mice. J Cereb Blood Flow Metab. 19:271678X20973609. doi: 10.1177/0271678X20973609. Abstract

Cuny GD, Degterev A. 2020. RIPK protein kinase family: Atypical lives of typical kinases. Semin Cell Dev Biol. 27: S1084-9521(19)30244-7. Abstract

Suebsuwong C, Dai B, Pinkas DM, Duddupudi AL, Li L, Bufton JC, Schlicher L, Gyrd-Hansen M, Hu M, Bullock AN, Degterev A, Cuny GD. 2020. Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold. Eur J Med Chem. 200: 112417.doi: 10.1016/j.ejmech.2020.112417. Abstract

Muendlein HI*, Sarhan J*, Liu BC, Connolly WM, Schworer SA, Smirnova I, Tang AY, Ilyukha V, Pietruska J, Tahmasebi S, Sonenberg N, Degterev A, Poltorak A. 2020. Constitutive interferon attenuates RIPK1/3-mediated cytokine translation. Cell Rep. 30: 699-713. * Equal contribution. Abstract

Degterev A, Ofengeim D, Yuan J. 2019. Targeting RIPK1 for the treatment of human diseases. Proc Natl Acad Sci USA. Epub ahead of print. Abstract

Saleh D, Degterev A. 2018. Chemical library screens to identify pharmacological modulators of necroptosis. Methods Mol Biol. 1857: 19-33. Abstract

Hrdinka M, Schlicher L, Dai B, Pinkas DM, Bufton JC, Picaud S, Ward JA, Rogers C, Suebsuwong C, Nikhar S, Cuny GD, Huber KV, Filippakopoulos P, Bullock AN, Degterev A, Gyrd-Hansen M. 2018. Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling. EMBO J Epub ahead of print. Abstract

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.  Abstract

Saleh D, Degterev A. 2018. Chemical library screens to identify pharmacological modulators of necroptosis. Methods in Molecular Biology: Programmed Necrosis. Springer Publishing, Berlin. ISBN 978-1-4939-8753-5.

von Mässenhausen A, Tonnus W, Himmerkus N, Parmentier S, Saleh D, Rodriguez D, Ousingsawat J, Ang RL, Weinberg JM, Sanz AB, Ortiz A, Zierleyn A, Becker JU, Baratte B, Desban N, Bach S, Schiessl IM, Nogusa S, Balachandran S, Anders HJ, Ting AT, Bleich M, Degterev A, Kunzelmann K, Bornstein SR, Green DR, Hugo C, Linkermann A. 2018. Phenytoin inhibits necroptosis. Cell Death Dis. 9:359. Abstract

Suebsuwong C, Pinkas DM, Ray SS, Bufton JC, Dai B, Bullock AN, Degterev A, Cuny GD. 2018. Activation loop targeting strategy for design of receptor-interacting protein kinase 2 (RIPK2) inhibitors. Bioorg Med Chem Lett. 28: 577-583. Abstract

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.  Abstract

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. Abstract

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.  Abstract

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

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.  Abstract

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. Abstract

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

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.  Abstract

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.  Abstract

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

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.   Abstract

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

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. Abstract