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Items: 1 to 20 of 27

1.

RIPK1 Mediates TNF-Induced Intestinal Crypt Apoptosis During Chronic NF-κB Activation.

Wong J, Garcia-Carbonell R, Zelic M, Ho SB, Boland BS, Yao SJ, Desai SA, Das S, Planell N, Harris PA, Font-Burgada J, Taniguchi K, Bertin J, Salas A, Pasparakis M, Gough PJ, Kelliher M, Karin M, Guma M.

Cell Mol Gastroenterol Hepatol. 2020;9(2):295-312. doi: 10.1016/j.jcmgh.2019.10.002. Epub 2019 Oct 10.

2.

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.

Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU, Kang J, Kasparcova V, Leister LK, Mahajan MK, Miller G, Nagilla R, Ouellette MT, Reilly MA, Rendina AR, Rivera EJ, Sun HH, Thorpe JH, Totoritis RD, Wang W, Wu D, Zhang D, Bertin J, Marquis RW.

ACS Med Chem Lett. 2019 May 9;10(6):857-862. doi: 10.1021/acsmedchemlett.9b00108. eCollection 2019 Jun 13.

3.

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.

J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2.

PMID:
31013427
4.

RIPK1 and Caspase-8 Ensure Chromosome Stability Independently of Their Role in Cell Death and Inflammation.

Liccardi G, Ramos Garcia L, Tenev T, Annibaldi A, Legrand AJ, Robertson D, Feltham R, Anderton H, Darding M, Peltzer N, Dannappel M, Schünke H, Fava LL, Haschka MD, Glatter T, Nesvizhskii A, Schmidt A, Harris PA, Bertin J, Gough PJ, Villunger A, Silke J, Pasparakis M, Bianchi K, Meier P.

Mol Cell. 2019 Feb 7;73(3):413-428.e7. doi: 10.1016/j.molcel.2018.11.010. Epub 2018 Dec 28.

5.

RIP1 Kinase Drives Macrophage-Mediated Adaptive Immune Tolerance in Pancreatic Cancer.

Wang W, Marinis JM, Beal AM, Savadkar S, Wu Y, Khan M, Taunk PS, Wu N, Su W, Wu J, Ahsan A, Kurz E, Chen T, Yaboh I, Li F, Gutierrez J, Diskin B, Hundeyin M, Reilly M, Lich JD, Harris PA, Mahajan MK, Thorpe JH, Nassau P, Mosley JE, Leinwand J, Kochen Rossi JA, Mishra A, Aykut B, Glacken M, Ochi A, Verma N, Kim JI, Vasudevaraja V, Adeegbe D, Almonte C, Bagdatlioglu E, Cohen DJ, Wong KK, Bertin J, Miller G.

Cancer Cell. 2018 Nov 12;34(5):757-774.e7. doi: 10.1016/j.ccell.2018.10.006.

6.

Elevated A20 promotes TNF-induced and RIPK1-dependent intestinal epithelial cell death.

Garcia-Carbonell R, Wong J, Kim JY, Close LA, Boland BS, Wong TL, Harris PA, Ho SB, Das S, Ernst PB, Sasik R, Sandborn WJ, Bertin J, Gough PJ, Chang JT, Kelliher M, Boone D, Guma M, Karin M.

Proc Natl Acad Sci U S A. 2018 Sep 25;115(39):E9192-E9200. doi: 10.1073/pnas.1810584115. Epub 2018 Sep 12.

7.

Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK1 inhibitor GSK2982772 in healthy volunteers.

Weisel K, Scott NE, Tompson DJ, Votta BJ, Madhavan S, Povey K, Wolstenholme A, Simeoni M, Rudo T, Richards-Peterson L, Sahota T, Wang JG, Lich J, Finger J, Verticelli A, Reilly M, Gough PJ, Harris PA, Bertin J, Wang ML.

Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.365.

8.

Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues.

Finger JN, Brusq JM, Campobasso N, Cook MN, Deutsch J, Haag H, Harris PA, Jenkins EL, Joglekar D, Lich JD, Maguire S, Nagilla R, Rivera EJ, Sun H, Votta BJ, Bertin J, Gough PJ.

Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.377.

9.

Autophagy protein ATG16L1 prevents necroptosis in the intestinal epithelium.

Matsuzawa-Ishimoto Y, Shono Y, Gomez LE, Hubbard-Lucey VM, Cammer M, Neil J, Dewan MZ, Lieberman SR, Lazrak A, Marinis JM, Beal A, Harris PA, Bertin J, Liu C, Ding Y, van den Brink MRM, Cadwell K.

J Exp Med. 2017 Dec 4;214(12):3687-3705. doi: 10.1084/jem.20170558. Epub 2017 Oct 31.

10.

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J.

J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10.

PMID:
28151659
11.

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ.

J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23.

PMID:
26854747
12.

Antioxidant Activity of 3-[N-(Acylhydrazono)ethyl]-4-hydroxy-coumarins.

Kotali A, Nasiopoulou DA, Tsoleridis CA, Harris PA, Kontogiorgis CA, Hadjipavlou-Litina DJ.

Molecules. 2016 Jan 23;21(2):138. doi: 10.3390/molecules21020138.

13.

Recent progress on MAP kinase pathway inhibitors.

Uehling DE, Harris PA.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4047-56. doi: 10.1016/j.bmcl.2015.07.093. Epub 2015 Aug 1. Review.

PMID:
26298497
14.

High throughput screening identifies ATP-competitive inhibitors of the NLRP1 inflammasome.

Harris PA, Duraiswami C, Fisher DT, Fornwald J, Hoffman SJ, Hofmann G, Jiang M, Lehr R, McCormick PM, Nickels L, Schwartz B, Wu Z, Zhang G, Marquis RW, Bertin J, Gough PJ.

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2739-43. doi: 10.1016/j.bmcl.2015.05.032. Epub 2015 May 19.

PMID:
26022841
15.

Herpes simplex virus suppresses necroptosis in human cells.

Guo H, Omoto S, Harris PA, Finger JN, Bertin J, Gough PJ, Kaiser WJ, Mocarski ES.

Cell Host Microbe. 2015 Feb 11;17(2):243-51. doi: 10.1016/j.chom.2015.01.003.

16.

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.

Harris PA, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Finger JN, Hoffman SJ, Kahler KM, Lehr R, Lich JD, Nagilla R, Nolte RT, Ouellette MT, Pao CS, Schaeffer MC, Smallwood A, Sun HH, Swift BA, Totoritis RD, Ward P, Marquis RW, Bertin J, Gough PJ.

ACS Med Chem Lett. 2013 Nov 4;4(12):1238-43. doi: 10.1021/ml400382p. eCollection 2013 Dec 12.

17.

Cutting Edge: RIP1 kinase activity is dispensable for normal development but is a key regulator of inflammation in SHARPIN-deficient mice.

Berger SB, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Cook M, Finger J, Hughes-Earle A, Harris PA, Kaiser WJ, Mocarski ES, Bertin J, Gough PJ.

J Immunol. 2014 Jun 15;192(12):5476-80. doi: 10.4049/jimmunol.1400499. Epub 2014 May 12.

18.

N'-[1-(2,4-Dioxo-3,4-dihydro-2H-1-benzopyran-3-yl-idene)eth-yl]thiophene-2-carbo-hydrazide.

Helliwell M, Nasiopoulou DA, Harris PA, Kotali A, Joule JA.

Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 1;67(Pt 4):o1014. doi: 10.1107/S1600536811010907. Epub 2011 Mar 31.

19.

The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.

Cheung M, Harris PA, Badiang JG, Peckham GE, Chamberlain SD, Alberti MJ, Jung DK, Harris SS, Bramson NH, Epperly AH, Stimpson SA, Peel MR.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5428-30. doi: 10.1016/j.bmcl.2008.09.040. Epub 2008 Sep 12.

PMID:
18818075
20.

Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.

Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter RN 3rd, Johnson JH, Knick VB, Laudeman CP, Luttrell DK, Mook RA, Nolte RT, Rudolph SK, Szewczyk JR, Truesdale AT, Veal JM, Wang L, Stafford JA.

J Med Chem. 2008 Aug 14;51(15):4632-40. doi: 10.1021/jm800566m. Epub 2008 Jul 12.

PMID:
18620382

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