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Items: 1 to 50 of 75

1.

Structural and functional consequences of the STAT5BN642H driver mutation.

de Araujo ED, Erdogan F, Neubauer HA, Meneksedag-Erol D, Manaswiyoungkul P, Eram MS, Seo HS, Qadree AK, Israelian J, Orlova A, Suske T, Pham HTT, Boersma A, Tangermann S, Kenner L, Rülicke T, Dong A, Ravichandran M, Brown PJ, Audette GF, Rauscher S, Dhe-Paganon S, Moriggl R, Gunning PT.

Nat Commun. 2019 Jun 7;10(1):2517. doi: 10.1038/s41467-019-10422-7.

2.

High activation of STAT5A drives peripheral T-cell lymphoma and leukemia.

Maurer B, Nivarthi H, Wingelhofer B, Pham HTT, Schlederer M, Suske T, Grausenburger R, Schiefer AI, Prchal-Murphy M, Chen D, Winkler S, Merkel O, Kornauth C, Hofbauer M, Hochgatterer B, Hoermann G, Hoelbl-Kovacic A, Prochazkova J, Lobello C, Cumaraswamy AA, Latzka J, Kitzwögerer M, Chott A, Janikova A, Pospíšilova Š, Loizou JI, Kubicek S, Valent P, Kolbe T, Grebien F, Kenner L, Gunning PT, Kralovics R, Herling M, Müller M, Rülicke T, Sexl V, Moriggl R.

Haematologica. 2019 May 23. pii: haematol.2019.216986. doi: 10.3324/haematol.2019.216986. [Epub ahead of print]

3.

Effect of caveolin-1 on Stat3-ptyr705 levels in breast and lung carcinoma cells.

Geletu M, Taha Z, Arulanandam R, Mohan R, Assi HH, Castro MG, Nabi IR, Gunning PT, Raptis L.

Biochem Cell Biol. 2019 Oct;97(5):638-646. doi: 10.1139/bcb-2018-0367. Epub 2019 Apr 15.

4.

Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer.

Shouksmith AE, Shah F, Grimard ML, Gawel JM, Raouf YS, Geletu M, Berger-Becvar A, de Araujo ED, Luchman HA, Heaton WL, Bakhshinyan D, Adile AA, Venugopal C, O'Hare T, Deininger MW, Singh SK, Konieczny SF, Weiss S, Fishel ML, Gunning PT.

J Med Chem. 2019 Mar 14;62(5):2651-2665. doi: 10.1021/acs.jmedchem.8b01957. Epub 2019 Mar 6.

PMID:
30776234
5.

PI3k and Stat3: Oncogenes that are Required for Gap Junctional, Intercellular Communication.

Geletu M, Taha Z, Gunning PT, Raptis L.

Cancers (Basel). 2019 Feb 1;11(2). pii: E167. doi: 10.3390/cancers11020167. Review.

6.

The ERBB-STAT3 Axis Drives Tasmanian Devil Facial Tumor Disease.

Kosack L, Wingelhofer B, Popa A, Orlova A, Agerer B, Vilagos B, Majek P, Parapatics K, Lercher A, Ringler A, Klughammer J, Smyth M, Khamina K, Baazim H, de Araujo ED, Rosa DA, Park J, Tin G, Ahmar S, Gunning PT, Bock C, Siddle HV, Woods GM, Kubicek S, Murchison EP, Bennett KL, Moriggl R, Bergthaler A.

Cancer Cell. 2019 Jan 14;35(1):125-139.e9. doi: 10.1016/j.ccell.2018.11.018.

7.

A functional in vitro assay for screening inhibitors of STAT5B phosphorylation.

de Araujo ED, Manaswiyoungkul P, Erdogan F, Qadree AK, Sina D, Tin G, Toutah K, Yuen K, Gunning PT.

J Pharm Biomed Anal. 2019 Jan 5;162:60-65. doi: 10.1016/j.jpba.2018.08.036. Epub 2018 Aug 18.

PMID:
30223143
8.

Implications of STAT3 and STAT5 signaling on gene regulation and chromatin remodeling in hematopoietic cancer.

Wingelhofer B, Neubauer HA, Valent P, Han X, Constantinescu SN, Gunning PT, Müller M, Moriggl R.

Leukemia. 2018 Aug;32(8):1713-1726. doi: 10.1038/s41375-018-0117-x. Epub 2018 Mar 27. Review.

9.

Pharmacologic inhibition of STAT5 in acute myeloid leukemia.

Wingelhofer B, Maurer B, Heyes EC, Cumaraswamy AA, Berger-Becvar A, de Araujo ED, Orlova A, Freund P, Ruge F, Park J, Tin G, Ahmar S, Lardeau CH, Sadovnik I, Bajusz D, Keserű GM, Grebien F, Kubicek S, Valent P, Gunning PT, Moriggl R.

Leukemia. 2018 May;32(5):1135-1146. doi: 10.1038/s41375-017-0005-9. Epub 2018 Feb 2.

10.

Reciprocal regulation of the Cadherin-11/Stat3 axis by caveolin-1 in mouse fibroblasts and lung carcinoma cells.

Geletu M, Mohan R, Arulanandam R, Berger-Becvar A, Nabi IR, Gunning PT, Raptis L.

Biochim Biophys Acta Mol Cell Res. 2018 May;1865(5):794-802. doi: 10.1016/j.bbamcr.2018.02.004. Epub 2018 Feb 16.

11.

Emerging therapeutic targets in myeloproliferative neoplasms and peripheral T-cell leukemia and lymphomas.

Orlova A, Wingelhofer B, Neubauer HA, Maurer B, Berger-Becvar A, Keserű GM, Gunning PT, Valent P, Moriggl R.

Expert Opin Ther Targets. 2018 Jan;22(1):45-57. doi: 10.1080/14728222.2018.1406924. Epub 2017 Nov 24. Review.

12.

ProxyPhos sensors for the detection of negatively charged membranes.

Murcar-Evans BI, Cabral AD, Toutah K, de Araujo ED, Lai A, Macdonald PM, Berger-Becvar A, Kraskouskaya D, Gunning PT.

Analyst. 2017 Nov 20;142(23):4511-4521. doi: 10.1039/c7an00568g.

PMID:
29098228
13.

Structure-activity relationship study of ProxyPhos chemosensors for the detection of proximal phosphorylation and other phosphate species.

Cabral AD, Murcar-Evans BI, Toutah K, Bancerz M, Rosa D, Yuen K, Radu TB, Ali M, Penkul A, Kraskouskaya D, Gunning PT.

Analyst. 2017 Oct 9;142(20):3922-3933. doi: 10.1039/c7an00722a.

PMID:
28930308
14.

MicroRNA-337-3p controls hepatobiliary gene expression and transcriptional dynamics during hepatic cell differentiation.

Demarez C, Gérard C, Cordi S, Poncy A, Achouri Y, Dauguet N, Rosa DA, Gunning PT, Manfroid I, Lemaigre FP.

Hepatology. 2018 Jan;67(1):313-327. doi: 10.1002/hep.29475. Epub 2017 Nov 16.

PMID:
28833283
15.

High-throughput thermofluor-based assays for inhibitor screening of STAT SH2 domains.

de Araujo ED, Manaswiyoungkul P, Israelian J, Park J, Yuen K, Farhangi S, Berger-Becvar A, Abu-Jazar L, Gunning PT.

J Pharm Biomed Anal. 2017 Sep 5;143:159-167. doi: 10.1016/j.jpba.2017.04.052. Epub 2017 May 1.

PMID:
28600954
16.

Combined targeting of STAT3 and STAT5: a novel approach to overcome drug resistance in chronic myeloid leukemia.

Gleixner KV, Schneeweiss M, Eisenwort G, Berger D, Herrmann H, Blatt K, Greiner G, Byrgazov K, Hoermann G, Konopleva M, Waliul I, Cumaraswamy AA, Gunning PT, Maeda H, Moriggl R, Deininger M, Lion T, Andreeff M, Valent P.

Haematologica. 2017 Sep;102(9):1519-1529. doi: 10.3324/haematol.2016.163436. Epub 2017 Jun 8.

17.

Characterization and application studies of ProxyPhos, a chemosensor for the detection of proximally phosphorylated peptides and proteins in aqueous solutions.

Kraskouskaya D, Cabral AD, Fong R, Bancerz M, Toutah K, Rosa D, Gardiner JE, de Araujo ED, Duodu E, Armstrong D, Fekl U, Gunning PT.

Analyst. 2017 Jun 26;142(13):2451-2459. doi: 10.1039/c6an02537d.

PMID:
28574079
18.

Combined STAT3 and BCR-ABL1 inhibition induces synthetic lethality in therapy-resistant chronic myeloid leukemia.

Eiring AM, Page BDG, Kraft IL, Mason CC, Vellore NA, Resetca D, Zabriskie MS, Zhang TY, Khorashad JS, Engar AJ, Reynolds KR, Anderson DJ, Senina A, Pomicter AD, Arpin CC, Ahmad S, Heaton WL, Tantravahi SK, Todic A, Colaguori R, Moriggl R, Wilson DJ, Baron R, O'Hare T, Gunning PT, Deininger MW.

Leukemia. 2017 May;31(5):1253-1254. doi: 10.1038/leu.2017.14. No abstract available.

PMID:
28465516
19.

Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site.

Paiva SL, da Silva SR, de Araujo ED, Gunning PT.

J Med Chem. 2018 Jan 25;61(2):405-421. doi: 10.1021/acs.jmedchem.6b01346. Epub 2017 Feb 28. Review.

PMID:
28076680
20.

CD133+ brain tumor-initiating cells are dependent on STAT3 signaling to drive medulloblastoma recurrence.

Garg N, Bakhshinyan D, Venugopal C, Mahendram S, Rosa DA, Vijayakumar T, Manoranjan B, Hallett R, McFarlane N, Delaney KH, Kwiecien JM, Arpin CC, Lai PS, Gómez-Biagi RF, Ali AM, de Araujo ED, Ajani OA, Hassell JA, Gunning PT, Singh SK.

Oncogene. 2017 Feb 2;36(5):606-617. doi: 10.1038/onc.2016.235. Epub 2016 Oct 24.

21.

Strategies for over-expression and purification of recombinant full length STAT5B in Escherichia coli.

de Araujo ED, Geletu M, Gunning PT.

Protein Expr Purif. 2017 Jan;129:1-8. doi: 10.1016/j.pep.2016.08.017. Epub 2016 Aug 31.

PMID:
27590918
22.

A selective inhibitor of the UFM1-activating enzyme, UBA5.

da Silva SR, Paiva SL, Bancerz M, Geletu M, Lewis AM, Chen J, Cai Y, Lukkarila JL, Li H, Gunning PT.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4542-4547. doi: 10.1016/j.bmcl.2015.10.015. Epub 2015 Oct 8.

PMID:
27520940
23.

Chronic Inhibition of STAT3/STAT5 in Treatment-Resistant Human Breast Cancer Cell Subtypes: Convergence on the ROS/SUMO Pathway and Its Effects on xCT Expression and System xc- Activity.

Linher-Melville K, Nashed MG, Ungard RG, Haftchenary S, Rosa DA, Gunning PT, Singh G.

PLoS One. 2016 Aug 11;11(8):e0161202. doi: 10.1371/journal.pone.0161202. eCollection 2016.

24.

Understanding Protein-Protein Interactions: Essential Players in (Patho)physiology (Part 2).

Wilson AJ, Gunning PT.

ChemMedChem. 2016 Apr 19;11(8):732-3. doi: 10.1002/cmdc.201600158. Epub 2016 Apr 9.

PMID:
27061459
25.

Disarming an Electrophilic Warhead: Retaining Potency in Tyrosine Kinase Inhibitor (TKI)-Resistant CML Lines While Circumventing Pharmacokinetic Liabilities.

Ali AM, Gómez-Biagi RF, Rosa DA, Lai PS, Heaton WL, Park JS, Eiring AM, Vellore NA, de Araujo ED, Ball DP, Shouksmith AE, Patel AB, Deininger MW, O'Hare T, Gunning PT.

ChemMedChem. 2016 Apr 19;11(8):850-61. doi: 10.1002/cmdc.201600021. Epub 2016 Mar 30.

26.

Understanding Protein-Protein Interactions: Essential Players in (Patho)physiology (Part 1).

Wilson AJ, Gunning PT.

Chembiochem. 2016 Apr 15;17(8):644-5. doi: 10.1002/cbic.201600166. Epub 2016 Mar 30.

PMID:
27027879
27.

STAT3 inhibitor has potent antitumor activity in B-lineage acute lymphoblastic leukemia cells overexpressing the high mobility group A1 (HMGA1)-STAT3 pathway.

Belton A, Xian L, Huso T, Koo M, Luo LZ, Turkson J, Page BD, Gunning PT, Liu G, Huso DL, Resar LM.

Leuk Lymphoma. 2016 Nov;57(11):2681-4. doi: 10.3109/10428194.2016.1153089. Epub 2016 Mar 8. No abstract available.

28.

Signal transducer and activator of transcription 3 (STAT3) inhibitor, S3I-201, acts as a potent and non-selective alkylating agent.

Ball DP, Lewis AM, Williams D, Resetca D, Wilson DJ, Gunning PT.

Oncotarget. 2016 Apr 12;7(15):20669-79. doi: 10.18632/oncotarget.7838.

29.

Applying Small Molecule Signal Transducer and Activator of Transcription-3 (STAT3) Protein Inhibitors as Pancreatic Cancer Therapeutics.

Arpin CC, Mac S, Jiang Y, Cheng H, Grimard M, Page BD, Kamocka MM, Haftchenary S, Su H, Ball DP, Rosa DA, Lai PS, Gómez-Biagi RF, Ali AM, Rana R, Hanenberg H, Kerman K, McElyea KC, Sandusky GE, Gunning PT, Fishel ML.

Mol Cancer Ther. 2016 May;15(5):794-805. doi: 10.1158/1535-7163.MCT-15-0003. Epub 2016 Feb 12.

30.

STAT5 Is a Key Regulator in NK Cells and Acts as a Molecular Switch from Tumor Surveillance to Tumor Promotion.

Gotthardt D, Putz EM, Grundschober E, Prchal-Murphy M, Straka E, Kudweis P, Heller G, Bago-Horvath Z, Witalisz-Siepracka A, Cumaraswamy AA, Gunning PT, Strobl B, Müller M, Moriggl R, Stockmann C, Sexl V.

Cancer Discov. 2016 Apr;6(4):414-29. doi: 10.1158/2159-8290.CD-15-0732. Epub 2016 Feb 12.

31.

A tool for the selective sequestration of ATP and PPi to aid in-solution phosphopeptide detection assays.

Duodu E, Kraskouskaya D, Gómez-Biagi RF, Gunning PT.

Analyst. 2016 Feb 7;141(3):820-2. doi: 10.1039/c5an01414j. Epub 2015 Dec 8.

PMID:
26643551
32.

Identification of Bidentate Salicylic Acid Inhibitors of PTP1B.

Haftchenary S, Jouk AO, Aubry I, Lewis AM, Landry M, Ball DP, Shouksmith AE, Collins CV, Tremblay ML, Gunning PT.

ACS Med Chem Lett. 2015 Jul 22;6(9):982-6. doi: 10.1021/acsmedchemlett.5b00171. eCollection 2015 Sep 10.

33.

A STAT inhibitor patent review: progress since 2011.

Lai PS, Rosa DA, Magdy Ali A, Gómez-Biagi RF, Ball DP, Shouksmith AE, Gunning PT.

Expert Opin Ther Pat. 2015;25(12):1397-421. doi: 10.1517/13543776.2015.1086749. Epub 2015 Sep 22. Review. Erratum in: Expert Opin Ther Pat. 2015;25(12):1495.

PMID:
26394986
34.

STAT3 pathway regulates lung-derived brain metastasis initiating cell capacity through miR-21 activation.

Singh M, Garg N, Venugopal C, Hallett R, Tokar T, McFarlane N, Mahendram S, Bakhshinyan D, Manoranjan B, Vora P, Qazi M, Arpin CC, Page B, Haftchenary S, Rosa DA, Lai PS, Gómez-Biagi RF, Ali AM, Lewis A, Geletu M, Murty NK, Hassell JA, Jurisica I, Gunning PT, Singh SK.

Oncotarget. 2015 Sep 29;6(29):27461-77. doi: 10.18632/oncotarget.4742.

35.

Selective detection of tyrosine-containing proximally phosphorylated motifs using an antenna-free Tb³⁺ luminescent sensor.

Duodu E, Kraskouskaya D, Campbell J, Graca-Lima G, Gunning PT.

Chem Commun (Camb). 2015 Apr 18;51(30):6675-7. doi: 10.1039/c5cc00679a.

PMID:
25785373
36.

Carcinoembryonic Antigen Cell Adhesion Molecule 1 long isoform modulates malignancy of poorly differentiated colon cancer cells.

Arabzadeh A, Dupaul-Chicoine J, Breton V, Haftchenary S, Yumeen S, Turbide C, Saleh M, McGregor K, Greenwood CM, Akavia UD, Blumberg RS, Gunning PT, Beauchemin N.

Gut. 2016 May;65(5):821-9. doi: 10.1136/gutjnl-2014-308781. Epub 2015 Feb 9.

37.

STAT3 as a mediator of BCR-ABL1-independent resistance in chronic myeloid leukemia.

Eiring AM, Kraft IL, Page BD, O'Hare T, Gunning PT, Deininger MW.

Leuk Suppl. 2014 Dec;3(Suppl 1):S5-6. doi: 10.1038/leusup.2014.3. Epub 2014 Dec 17. No abstract available.

38.

Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein.

Cumaraswamy AA, Lewis AM, Geletu M, Todic A, Diaz DB, Cheng XR, Brown CE, Laister RC, Muench D, Kerman K, Grimes HL, Minden MD, Gunning PT.

ACS Med Chem Lett. 2014 Sep 19;5(11):1202-1206. eCollection 2014 Nov 13.

39.

Changes in signal transducer and activator of transcription 3 (STAT3) dynamics induced by complexation with pharmacological inhibitors of Src homology 2 (SH2) domain dimerization.

Resetca D, Haftchenary S, Gunning PT, Wilson DJ.

J Biol Chem. 2014 Nov 21;289(47):32538-47. doi: 10.1074/jbc.M114.595454. Epub 2014 Oct 6.

40.

Combined STAT3 and BCR-ABL1 inhibition induces synthetic lethality in therapy-resistant chronic myeloid leukemia.

Eiring AM, Page BDG, Kraft IL, Mason CC, Vellore NA, Resetca D, Zabriskie MS, Zhang TY, Khorashad JS, Engar AJ, Reynolds KR, Anderson DJ, Senina A, Pomicter AD, Arpin CC, Ahmad S, Heaton WL, Tantravahi SK, Todic A, Moriggl R, Wilson DJ, Baron R, O'Hare T, Gunning PT, Deininger MW.

Leukemia. 2015 Mar;29(3):586-597. doi: 10.1038/leu.2014.245. Epub 2014 Aug 19. Erratum in: Leukemia. 2017 May;31(5):1253-1254.

41.

Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.

Haftchenary S, Luchman HA, Jouk AO, Veloso AJ, Page BD, Cheng XR, Dawson SS, Grinshtein N, Shahani VM, Kerman K, Kaplan DR, Griffin C, Aman AM, Al-Awar R, Weiss S, Gunning PT.

ACS Med Chem Lett. 2013 Sep 8;4(11):1102-7. doi: 10.1021/ml4003138. eCollection 2013 Nov 14.

42.

Dynamic reprogramming of signaling upon met inhibition reveals a mechanism of drug resistance in gastric cancer.

Lai AZ, Cory S, Zhao H, Gigoux M, Monast A, Guiot MC, Huang S, Tofigh A, Thompson C, Naujokas M, Marcus VA, Bertos N, Sehat B, Perera RM, Bell ES, Page BD, Gunning PT, Ferri LE, Hallett M, Park M.

Sci Signal. 2014 Apr 22;7(322):ra38. doi: 10.1126/scisignal.2004839.

PMID:
24757178
43.

Mutations in UBA3 confer resistance to the NEDD8-activating enzyme inhibitor MLN4924 in human leukemic cells.

Xu GW, Toth JI, da Silva SR, Paiva SL, Lukkarila JL, Hurren R, Maclean N, Sukhai MA, Bhattacharjee RN, Goard CA, Medeiros B, Gunning PT, Dhe-Paganon S, Petroski MD, Schimmer AD.

PLoS One. 2014 Apr 1;9(4):e93530. doi: 10.1371/journal.pone.0093530. eCollection 2014. Erratum in: PLoS One. 2014;9(10):e112004. Medeiros, Bruno [added].

44.

Electrochemical detection of the Fc-STAT3 phosphorylation and STAT3-Fc-STAT3 dimerization and inhibition.

Martic S, Rains MK, Haftchenary S, Shahani VM, Kraskouskaya D, Ball DP, Gunning PT, Kraatz HB.

Mol Biosyst. 2014 Mar 4;10(3):576-80. doi: 10.1039/c3mb70493a. Epub 2014 Jan 8.

PMID:
24402062
45.

An excimer-based, turn-on fluorescent sensor for the selective detection of diphosphorylated proteins in aqueous solution and polyacrylamide gels.

Kraskouskaya D, Bancerz M, Soor HS, Gardiner JE, Gunning PT.

J Am Chem Soc. 2014 Jan 29;136(4):1234-7. doi: 10.1021/ja411492k. Epub 2014 Jan 14.

PMID:
24387313
46.

Inhibiting aberrant signal transducer and activator of transcription protein activation with tetrapodal, small molecule Src homology 2 domain binders: promising agents against multiple myeloma.

Page BD, Croucher DC, Li ZH, Haftchenary S, Jimenez-Zepeda VH, Atkinson J, Spagnuolo PA, Wong YL, Colaguori R, Lewis AM, Schimmer AD, Trudel S, Gunning PT.

J Med Chem. 2013 Sep 26;56(18):7190-200. doi: 10.1021/jm3017255. Epub 2013 Sep 13.

PMID:
23968501
47.

A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.

Shahani VM, Ball DP, Ramos AV, Li Z, Spagnuolo PA, Haftchenary S, Schimmer AD, Trudel S, Gunning PT.

Bioorg Med Chem. 2013 Sep 1;21(17):5618-28. doi: 10.1016/j.bmc.2013.04.080. Epub 2013 May 9.

PMID:
23810672
48.

Extolling the benefits of molecular therapeutic lipidation.

Avadisian M, Gunning PT.

Mol Biosyst. 2013 Sep;9(9):2179-88. doi: 10.1039/c3mb70147f. Review.

PMID:
23771042
49.

Progress towards the development of SH2 domain inhibitors.

Kraskouskaya D, Duodu E, Arpin CC, Gunning PT.

Chem Soc Rev. 2013 Apr 21;42(8):3337-70. doi: 10.1039/c3cs35449k. Epub 2013 Feb 11. Review.

PMID:
23396540
50.

Exploring a new frontier in cancer treatment: targeting the ubiquitin and ubiquitin-like activating enzymes.

da Silva SR, Paiva SL, Lukkarila JL, Gunning PT.

J Med Chem. 2013 Mar 28;56(6):2165-77. doi: 10.1021/jm301420b. Epub 2013 Mar 1. Review.

PMID:
23360215

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