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Items: 1 to 50 of 94

1.

An Anti-CLL-1 Antibody-Drug Conjugate for the Treatment of Acute Myeloid Leukemia.

Zheng B, Yu SF, Del Rosario G, Leong SR, Lee GY, Vij R, Chiu CPC, Liang WC, Wu Y, Chalouni C, Sadowsky J, Clark VM, Hendricks A, Poon KA, Chu YW, Pillow TH, Schutten MM, Flygare JA, Polson AG.

Clin Cancer Res. 2018 Jun 29. pii: clincanres.0333.2018. doi: 10.1158/1078-0432.CCR-18-0333. [Epub ahead of print]

PMID:
29959143
2.

Reactive-site-centric chemoproteomics identifies a distinct class of deubiquitinase enzymes.

Hewings DS, Heideker J, Ma TP, AhYoung AP, El Oualid F, Amore A, Costakes GT, Kirchhofer D, Brasher B, Pillow T, Popovych N, Maurer T, Schwerdtfeger C, Forrest WF, Yu K, Flygare J, Bogyo M, Wertz IE.

Nat Commun. 2018 Mar 21;9(1):1162. doi: 10.1038/s41467-018-03511-6.

3.

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

Wei B, Gunzner-Toste J, Yao H, Wang T, Wang J, Xu Z, Chen J, Wai J, Nonomiya J, Tsai SP, Chuh J, Kozak KR, Liu Y, Yu SF, Lau J, Li G, Phillips GD, Leipold D, Kamath A, Su D, Xu K, Eigenbrot C, Steinbacher S, Ohri R, Raab H, Staben LR, Zhao G, Flygare JA, Pillow TH, Verma V, Masterson LA, Howard PW, Safina B.

J Med Chem. 2018 Feb 8;61(3):989-1000. doi: 10.1021/acs.jmedchem.7b01430. Epub 2017 Dec 21.

PMID:
29227683
4.

Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers.

Gregson SJ, Masterson LA, Wei B, Pillow TH, Spencer SD, Kang GD, Yu SF, Raab H, Lau J, Li G, Lewis Phillips GD, Gunzner-Toste J, Safina BS, Ohri R, Darwish M, Kozak KR, Dela Cruz-Chuh J, Polson A, Flygare JA, Howard PW.

J Med Chem. 2017 Dec 14;60(23):9490-9507. doi: 10.1021/acs.jmedchem.7b00736. Epub 2017 Nov 16.

PMID:
29112410
5.

Introducing People-Centered Language to SLEEP.

Buysse DJ, Parthasarathy S, Flygare J.

Sleep. 2017 Apr 1;40(4). doi: 10.1093/sleep/zsx038. No abstract available.

PMID:
28475800
6.

Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates.

Pillow TH, Sadowsky JD, Zhang D, Yu SF, Del Rosario G, Xu K, He J, Bhakta S, Ohri R, Kozak KR, Ha E, Junutula JR, Flygare JA.

Chem Sci. 2017 Jan 1;8(1):366-370. doi: 10.1039/c6sc01831a. Epub 2016 Aug 22.

7.

Lentiviral Vectors with Cellular Promoters Correct Anemia and Lethal Bone Marrow Failure in a Mouse Model for Diamond-Blackfan Anemia.

Debnath S, Jaako P, Siva K, Rothe M, Chen J, Dahl M, Gaspar HB, Flygare J, Schambach A, Karlsson S.

Mol Ther. 2017 Aug 2;25(8):1805-1814. doi: 10.1016/j.ymthe.2017.04.002. Epub 2017 Apr 20.

8.

Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody-Drug Conjugates with Self-Immolative Disulfide Linkers.

Pillow TH, Schutten M, Yu SF, Ohri R, Sadowsky J, Poon KA, Solis W, Zhong F, Del Rosario G, Go MAT, Lau J, Yee S, He J, Liu L, Ng C, Xu K, Leipold DD, Kamath AV, Zhang D, Masterson L, Gregson SJ, Howard PW, Fang F, Chen J, Gunzner-Toste J, Kozak KK, Spencer S, Polakis P, Polson AG, Flygare JA, Junutula JR.

Mol Cancer Ther. 2017 May;16(5):871-878. doi: 10.1158/1535-7163.MCT-16-0641. Epub 2017 Feb 21.

9.

Activity-based probes for the ubiquitin conjugation-deconjugation machinery: new chemistries, new tools, and new insights.

Hewings DS, Flygare JA, Bogyo M, Wertz IE.

FEBS J. 2017 May;284(10):1555-1576. doi: 10.1111/febs.14039. Epub 2017 Mar 10. Review.

10.

Activity-based probes for the multicatalytic proteasome.

Hewings DS, Flygare JA, Wertz IE, Bogyo M.

FEBS J. 2017 May;284(10):1540-1554. doi: 10.1111/febs.14016. Epub 2017 Feb 7. Review.

11.

Direct lineage reprogramming: a useful addition to the blood cell research toolbox.

Capellera-Garcia S, Flygare J.

Expert Rev Hematol. 2017 Feb;10(2):107-109. doi: 10.1080/17474086.2017.1272409. Epub 2017 Jan 5. No abstract available.

PMID:
27967256
12.

Listening to the Patient Voice in Narcolepsy: Diagnostic Delay, Disease Burden, and Treatment Efficacy.

Maski K, Steinhart E, Williams D, Scammell T, Flygare J, McCleary K, Gow M.

J Clin Sleep Med. 2017 Mar 15;13(3):419-425. doi: 10.5664/jcsm.6494.

13.

Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody-drug conjugates.

Staben LR, Koenig SG, Lehar SM, Vandlen R, Zhang D, Chuh J, Yu SF, Ng C, Guo J, Liu Y, Fourie-O'Donohue A, Go M, Linghu X, Segraves NL, Wang T, Chen J, Wei B, Phillips GD, Xu K, Kozak KR, Mariathasan S, Flygare JA, Pillow TH.

Nat Chem. 2016 Dec;8(12):1112-1119. doi: 10.1038/nchem.2635. Epub 2016 Oct 17.

PMID:
27874860
14.

Direct Conversion of Fibroblasts to Megakaryocyte Progenitors.

Pulecio J, Alejo-Valle O, Capellera-Garcia S, Vitaloni M, Rio P, Mejía-Ramírez E, Caserta I, Bueren JA, Flygare J, Raya A.

Cell Rep. 2016 Oct 11;17(3):671-683. doi: 10.1016/j.celrep.2016.09.036.

15.

Defining the Minimal Factors Required for Erythropoiesis through Direct Lineage Conversion.

Capellera-Garcia S, Pulecio J, Dhulipala K, Siva K, Rayon-Estrada V, Singbrant S, Sommarin MN, Walkley CR, Soneji S, Karlsson G, Raya Á, Sankaran VG, Flygare J.

Cell Rep. 2016 Jun 14;15(11):2550-62. doi: 10.1016/j.celrep.2016.05.027. Epub 2016 Jun 2.

16.

Targeting LGR5+ cells with an antibody-drug conjugate for the treatment of colon cancer.

Junttila MR, Mao W, Wang X, Wang BE, Pham T, Flygare J, Yu SF, Yee S, Goldenberg D, Fields C, Eastham-Anderson J, Singh M, Vij R, Hongo JA, Firestein R, Schutten M, Flagella K, Polakis P, Polson AG.

Sci Transl Med. 2015 Nov 18;7(314):314ra186. doi: 10.1126/scitranslmed.aac7433.

PMID:
26582901
17.

Novel antibody-antibiotic conjugate eliminates intracellular S. aureus.

Lehar SM, Pillow T, Xu M, Staben L, Kajihara KK, Vandlen R, DePalatis L, Raab H, Hazenbos WL, Morisaki JH, Kim J, Park S, Darwish M, Lee BC, Hernandez H, Loyet KM, Lupardus P, Fong R, Yan D, Chalouni C, Luis E, Khalfin Y, Plise E, Cheong J, Lyssikatos JP, Strandh M, Koefoed K, Andersen PS, Flygare JA, Wah Tan M, Brown EJ, Mariathasan S.

Nature. 2015 Nov 19;527(7578):323-8. doi: 10.1038/nature16057. Epub 2015 Nov 4.

PMID:
26536114
18.

FTY720 (Fingolimod) sensitizes hepatocellular carcinoma cells to sorafenib-mediated cytotoxicity.

Ahmed D, de Verdier PJ, Ryk C, Lunqe O, Stål P, Flygare J.

Pharmacol Res Perspect. 2015 Oct;3(5):e00171. doi: 10.1002/prp2.171. Epub 2015 Aug 19.

19.

Glucocorticoids improve erythroid progenitor maintenance and dampen Trp53 response in a mouse model of Diamond-Blackfan anaemia.

Sjögren SE, Siva K, Soneji S, George AJ, Winkler M, Jaako P, Wlodarski M, Karlsson S, Hannan RD, Flygare J.

Br J Haematol. 2015 Nov;171(4):517-29. doi: 10.1111/bjh.13632. Epub 2015 Aug 25.

20.

Influence of rimonabant treatment on peripheral blood mononuclear cells; flow cytometry analysis and gene expression profiling.

Almestrand S, Wang X, Jeppsson-Ahlberg Å, Nordgren M, Flygare J, Christensson B, Rössner S, Sander B.

PeerJ. 2015 Jun 30;3:e1056. doi: 10.7717/peerj.1056. eCollection 2015.

21.

Disruption of the 5S RNP-Mdm2 interaction significantly improves the erythroid defect in a mouse model for Diamond-Blackfan anemia.

Jaako P, Debnath S, Olsson K, Zhang Y, Flygare J, Lindström MS, Bryder D, Karlsson S.

Leukemia. 2015 Nov;29(11):2221-9. doi: 10.1038/leu.2015.128. Epub 2015 May 19.

22.

A Novel Anti-CD22 Anthracycline-Based Antibody-Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs.

Yu SF, Zheng B, Go M, Lau J, Spencer S, Raab H, Soriano R, Jhunjhunwala S, Cohen R, Caruso M, Polakis P, Flygare J, Polson AG.

Clin Cancer Res. 2015 Jul 15;21(14):3298-306. doi: 10.1158/1078-0432.CCR-14-2035. Epub 2015 Apr 3.

23.

Perturbations of the endocannabinoid system in mantle cell lymphoma: correlations to clinical and pathological features.

Wasik AM, Nygren L, Almestrand S, Zong F, Flygare J, Wennerholm SB, Saft L, Andersson P, Kimby E, Wahlin BE, Christensson B, Sander B.

Oncoscience. 2014 Sep 4;1(8):550-7. eCollection 2014.

24.

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.

ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 9.

25.

Gene therapy cures the anemia and lethal bone marrow failure in a mouse model of RPS19-deficient Diamond-Blackfan anemia.

Jaako P, Debnath S, Olsson K, Modlich U, Rothe M, Schambach A, Flygare J, Karlsson S.

Haematologica. 2014 Dec;99(12):1792-8. doi: 10.3324/haematol.2014.111195. Epub 2014 Sep 12.

26.

Site-specific trastuzumab maytansinoid antibody-drug conjugates with improved therapeutic activity through linker and antibody engineering.

Pillow TH, Tien J, Parsons-Reponte KL, Bhakta S, Li H, Staben LR, Li G, Chuh J, Fourie-O'Donohue A, Darwish M, Yip V, Liu L, Leipold DD, Su D, Wu E, Spencer SD, Shen BQ, Xu K, Kozak KR, Raab H, Vandlen R, Lewis Phillips GD, Scheller RH, Polakis P, Sliwkowski MX, Flygare JA, Junutula JR.

J Med Chem. 2014 Oct 9;57(19):7890-9. doi: 10.1021/jm500552c. Epub 2014 Sep 18.

PMID:
25191794
27.

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G.

ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12.

28.

Narcolepsy: let the patient's voice awaken us!

Flygare J, Parthasarathy S.

Am J Med. 2015 Jan;128(1):10-3. doi: 10.1016/j.amjmed.2014.05.037. Epub 2014 Jun 12. No abstract available.

29.

Secondary stimulation from Bacillus Calmette-Guérin induced macrophages induce nitric oxide independent cell-death in bladder cancer cells.

Thiel T, Ryk C, Chatzakos V, Hallén Grufman K, Bavand-Chobot N, Flygare J, Wiklund NP, de Verdier PJ.

Cancer Lett. 2014 Jun 28;348(1-2):119-25. doi: 10.1016/j.canlet.2014.03.014. Epub 2014 Mar 18.

PMID:
24657658
30.

Inhibiting caspase-6 activation and catalytic activity for neurodegenerative diseases.

Flygare JA, Arkin MR.

Curr Top Med Chem. 2014;14(3):319-25. Review.

PMID:
24283214
31.

Tailoring small molecules for an allosteric site on procaspase-6.

Murray J, Giannetti AM, Steffek M, Gibbons P, Hearn BR, Cohen F, Tam C, Pozniak C, Bravo B, Lewcock J, Jaishankar P, Ly CQ, Zhao X, Tang Y, Chugha P, Arkin MR, Flygare J, Renslo AR.

ChemMedChem. 2014 Jan;9(1):73-7, 2. doi: 10.1002/cmdc.201300424. Epub 2013 Nov 20.

PMID:
24259468
32.

Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist.

Wong H, Gould SE, Budha N, Darbonne WC, Kadel EE 3rd, La H, Alicke B, Halladay JS, Erickson R, Portera C, Tolcher AW, Infante JR, Mamounas M, Flygare JA, Hop CE, Fairbrother WJ.

Drug Metab Dispos. 2013 Dec;41(12):2104-13. doi: 10.1124/dmd.113.053926. Epub 2013 Sep 16.

33.

ZFP36L2 is required for self-renewal of early burst-forming unit erythroid progenitors.

Zhang L, Prak L, Rayon-Estrada V, Thiru P, Flygare J, Lim B, Lodish HF.

Nature. 2013 Jul 4;499(7456):92-6. doi: 10.1038/nature12215. Epub 2013 Jun 9.

34.

Structure-guided design of a selective BCL-X(L) inhibitor.

Lessene G, Czabotar PE, Sleebs BE, Zobel K, Lowes KN, Adams JM, Baell JB, Colman PM, Deshayes K, Fairbrother WJ, Flygare JA, Gibbons P, Kersten WJ, Kulasegaram S, Moss RM, Parisot JP, Smith BJ, Street IP, Yang H, Huang DC, Watson KG.

Nat Chem Biol. 2013 Jun;9(6):390-7. doi: 10.1038/nchembio.1246. Epub 2013 Apr 21.

PMID:
23603658
35.

Fetal hepatic progenitors support long-term expansion of hematopoietic stem cells.

Chou S, Flygare J, Lodish HF.

Exp Hematol. 2013 May;41(5):479-490.e4. doi: 10.1016/j.exphem.2013.02.003. Epub 2013 Feb 13.

36.

Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.

Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M.

Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10.

PMID:
23294830
37.

Antibody-drug conjugates for the treatment of cancer.

Flygare JA, Pillow TH, Aristoff P.

Chem Biol Drug Des. 2013 Jan;81(1):113-21. doi: 10.1111/cbdd.12085. Review.

PMID:
23253133
38.

Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6.

Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, Tang Y, Zhao X, Lewcock JW, Renslo AR, Flygare J, Arkin MR.

PLoS One. 2012;7(12):e50864. doi: 10.1371/journal.pone.0050864. Epub 2012 Dec 5.

39.

Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-α pharmacology.

Erickson RI, Tarrant J, Cain G, Lewin-Koh SC, Dybdal N, Wong H, Blackwood E, West K, Steigerwalt R, Mamounas M, Flygare JA, Amemiya K, Dambach D, Fairbrother WJ, Diaz D.

Toxicol Sci. 2013 Jan;131(1):247-58. doi: 10.1093/toxsci/kfs265. Epub 2012 Sep 5.

PMID:
22956632
40.

Dogs are more sensitive to antagonists of inhibitor of apoptosis proteins than rats and humans: a translational toxicokinetic/toxicodynamic analysis.

Wong H, Budha NR, West K, Blackwood E, Ware JA, Yu R, Darbonne WC, Gould SE, Steigerwalt R, Erickson R, Hop CE, LoRusso P, Eckhardt SG, Wagner A, Chan IT, Mamounas M, Flygare JA, Fairbrother WJ.

Toxicol Sci. 2012 Nov;130(1):205-13. doi: 10.1093/toxsci/kfs235. Epub 2012 Jul 28.

PMID:
22843607
41.

Dietary L-leucine improves the anemia in a mouse model for Diamond-Blackfan anemia.

Jaako P, Debnath S, Olsson K, Bryder D, Flygare J, Karlsson S.

Blood. 2012 Sep 13;120(11):2225-8. doi: 10.1182/blood-2012-05-431437. Epub 2012 Jul 12.

42.

Transition-state metal aryl bond stability determines regioselectivity in palladium acetate mediated C-H bond activation of heteroarenes.

Petit A, Flygare J, Miller AT, Winkel G, Ess DH.

Org Lett. 2012 Jul 20;14(14):3680-3. doi: 10.1021/ol301521n. Epub 2012 Jul 10.

PMID:
22780880
43.

Inhibition of sphingosine kinase 1 enhances cytotoxicity, ceramide levels and ROS formation in liver cancer cells treated with selenite.

Chatzakos V, Rundlöf AK, Ahmed D, de Verdier PJ, Flygare J.

Biochem Pharmacol. 2012 Sep 1;84(5):712-21. doi: 10.1016/j.bcp.2012.06.009. Epub 2012 Jun 19.

PMID:
22727936
44.

Progress towards mechanism-based treatment for Diamond-Blackfan anemia.

Sjögren SE, Flygare J.

ScientificWorldJournal. 2012;2012:184362. doi: 10.1100/2012/184362. Epub 2012 Apr 24. Review.

45.

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ.

J Med Chem. 2012 May 10;55(9):4101-13. doi: 10.1021/jm300060k. Epub 2012 Mar 28.

46.

Long noncoding RNA-mediated anti-apoptotic activity in murine erythroid terminal differentiation.

Hu W, Yuan B, Flygare J, Lodish HF.

Genes Dev. 2011 Dec 15;25(24):2573-8. doi: 10.1101/gad.178780.111. Epub 2011 Dec 8.

47.

Effects of redox modulation by inhibition of thioredoxin reductase on radiosensitivity and gene expression.

Selenius M, Hedman M, Brodin D, Gandin V, Rigobello MP, Flygare J, Marzano C, Bindoli A, Brodin O, Björnstedt M, Fernandes AP.

J Cell Mol Med. 2012 Jul;16(7):1593-605. doi: 10.1111/j.1582-4934.2011.01469.x.

48.

From stem cell to red cell: regulation of erythropoiesis at multiple levels by multiple proteins, RNAs, and chromatin modifications.

Hattangadi SM, Wong P, Zhang L, Flygare J, Lodish HF.

Blood. 2011 Dec 8;118(24):6258-68. doi: 10.1182/blood-2011-07-356006. Epub 2011 Oct 12. Review.

49.

Mice with ribosomal protein S19 deficiency develop bone marrow failure and symptoms like patients with Diamond-Blackfan anemia.

Jaako P, Flygare J, Olsson K, Quere R, Ehinger M, Henson A, Ellis S, Schambach A, Baum C, Richter J, Larsson J, Bryder D, Karlsson S.

Blood. 2011 Dec 1;118(23):6087-96. doi: 10.1182/blood-2011-08-371963. Epub 2011 Oct 11.

50.

Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.

Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB.

J Med Chem. 2011 Mar 24;54(6):1914-26. doi: 10.1021/jm101596e. Epub 2011 Mar 2.

PMID:
21366295

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