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Papers in 2020


107. Cabral A. D., Rafiei N., de Araujo E. D., Radu T. B., Toutah K., Milstein J., Kraskouskaya D., Gunning P.T., Sensitive detection of Broad-Spectrum Bacteria with small fluorescent excimer chemosensors. ACS Sensors 2020.


106. Hassan M.M., Ganda G., Nawar N., Israelian J., Manaswiyoungkul P., Raouf Y.S., Armstrong D., Sedighi A., Olasunkanmi O.O., Erdogan F., Cabral A.D., Angeles F., Altintas R., de Araujo E.D., Gunning P.T. Development of conformationally constrained L-shaped scaffolds for selective HDAC8 targeting. (2020) Journal of Medicinal Chemistry.


105. de Araujo E.D., Keserű G.M., Gunning P.T., Moriggl R. Targeting STAT3 and STAT5 in Cancer. Cancers 2020.

104. Gawel J. M., Shouksmith A. E., Raouf Y. S., Nawar N., Toutah K., Bukhari S., Manaswiyoungkul P., Olaoye O. O., Israelian J., Radu T. B., Cabral A. D., Sina D., Sedighi A., de Araujo E. D., Gunning P.T. “PTG-0861: A Novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukemia.” (2020) European Journal of Medicinal Chemistry 201:112411

103. Hadzijusufovic E., Keller A., Berger D., Greiner G., Wingelhofer B., Witzeneder N., Ivanov D., Pecnard E., Nivarthi H., Schur F.K.M., Filik Y., Kornauth C., Neubauer H.A., Mullauer L., Tin G., Park J., de Araujo E.D., Gunning P.T., Hoermann G., Gouilleux F., Kralovics R., Moriggl R., Valent P. STAT5B is expressed in CD34+/CD38- stem cells and serves as a potential molecular target in Ph-negative myeloproliferative neoplasms. (2020) Cancers. Accepted IF = 6.102


102. Abdeldayem, A., Raouf, Y. S., Constantinescu, S., Moriggl, R., Gunning, P. T. “Advances in Covalent Kinase Inhibitors.” ChemSocRev. 2020 Accepted CS-REV-10-2019-000720 IF = 40.443


101. Manaswiyoungkul P., Erdogan F., Olaoye O. O., de Araujo E. D., Gunning P. T. “The Development and Optimization of STAT5B High-Throughput Fluorescence Polarization Assay for DNA-Binding Domain-Targeting Inhibitors.” J. Pharm Biomed Anal 2020, In press IF = 3.169


100. Shouksmith A. E., Gawel J. M., Nawar N., Sina D., Raouf Y. S., Bukhari S., He L., Johns A. E., Manaswiyoungkul P., Olaoye O. O., Cabral A. D., Sedighi A., de Araujo E. D., Gunning P.T. Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. ACS Med Chem Lett. 2020, 11:56-64. IF = 3.746.


99. Maurer B., Nivarthi H., Wingelhofer B., Pham H. T. T., Grausenburger R., Schlederer M., Prchal-Murphy M., Chen D., Winkler S., Merkel O., Schiefer A-I., Kornauth C., Suske T., Hofbauer M., Hochgatterer B., Hoermann G., Hoelbl-Kovacic A., Cumaraswamy A. A., Eder G., Kitzwögerer M., Chott A., Pospíšilova S., Kubicek S., Valent P., Kolbe T., Grebien T., Kenner L., Gunning P. T., Kralovics R., Herling M., Müller M., Rülicke T., Sexl V., Moriggl  R. “High activation of STAT5A drives Peripheral T-Cell Lymphoma and Leukemia” Haematologica 2020, 105, 435-447. IF = 7.57.


Papers in 2019


98. Geletu M., Hoskin V., Niit M., Adan H., Gunning P. T., Raptis L. “Differentiation of mouse breast epithelial HC11 and EPH4 cells" 2019, JoVE, JoVE60147


97. Manaswiyoungkul P., de Araujo E. D., and Gunning P.T. “Targeting Prenylation Inhibition through the Mevalonate Pathway.” RSC Med Chem. 2019, 11, 51-71.


96. de Araujo E.D., Orlova A., Neubauer H.A., Bajusz D., Seo H-S., Dhe-Paganon S., Keserű G.M., Moriggl R., Gunning P.T. Structural Implications of STAT3 and STAT5 SH2 Domain Mutations. 2019 Cancers. 11, 1757-1778. IF = 6.102


95. Orlova A., Wagner C., de Araujo E. D., Bajusz D., Neubauer H. A., Herling M., Gunning P. T., Keserű G. M., Gunning P. T. Direct targeting options of STAT3 and STAT5 in cancer. 2019 Cancers. 11, 1930-1946. IF = 6.102


94. Nitt, M., Geletu M., Taha Z., Arulanandam R., Cass J., Hoskin V., Elliot B., Gunning P. T., Raptis L. “Regulation of Differentiation of HC11 Mouse Breast Epithelial Cells by the Signal Transducer and Activator of Transcription-3” Anticancer Research. 2019, 39, 2749-2756. IF = 1.935.


93. Geletu, M., Taha, Z., Arulanandam, R., Mohan, R., Assi, H. H., Castro, M. G., Nabi, I. R., Gunning, P. T., Raptis, L. “Effect of Caveolin-1 upon Stat3-pTyr705 levels in breast and lung carcinoma cells.” Biochem Cell Biol. 2019, 97, 638-646. IF = 2.250.


92. de Araujo E. D., Erdogan F., Neubauer H. A., Meneksedag-Erol D., Manaswiyoungkul P., Eram M. S., Seo H-S., Qadree A. K., Israelian J., Orlova A., Suske T., Pham H. T. T., Boersma A., Tangermann S., Kenner L., Rülicke T., Dong A., Ravichandran M., Brown P. J., Audette G. F., Rauscher S., Dhe-Paganon S., Moriggl R.,  and Gunning P.T.* “Structural and Functional Consequences of the STAT5BN642H Driver Mutation.” Nature Commun. 2019, 10, 1-15. IF = 11.880.


91. Linher-Melville K., Sharma M., Nakhla P., Kum E., Ungard R., Park J., Rosa D.A., Gunning P.T., Singh G. “Inhibiting STAT3 in a murine model of human breast cancer-induced bone pain delays the onset of nociception.” Molecular Pain 2019, 15, 1-16. IF = 3.774.


90. de Araujo E. D., Manaswiyoungkul P., Erdogan F., Qadree A. K., Sina D., Tin G., Toutah K., Yuen K., Gunning P. T. “A functional in vitro assay for screening inhibitors of STAT5B phosphorylation” J. Pharm Biomed Anal 2019, 162, 60-65. IF = 3.169.


89. Geletu M., Taha Z., Gunning P. T., Raptis L. “PI3k and Stat3: Oncogenes that are Required for Gap Junctional, Intercellular Communication.” Cancers 2019, 11, 167. IF = 6.102.


88. 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 E. D., Rosa D. A., Park J., Tin G., Ahmar S., Gunning P. T., Bock C, Siddle H.V., Woods G. M., Kubicek S., Murchison E. P., Bennett K. L., Moriggl R., Bergthaler A.* “The ERBB-STAT3 axis drives Tasmanian devil facial tumor disease.” Cancer Cell 2019, 35, 125-139. IF = 22.844.


87. Shouksmith, A. E., Grimard, M. L., Geletu, M., de Araujo, E. D., Berger-Becvar, A., Heaton, W. L., Gaweł, J. L., Bakhshinyan, D., Adile, A. A., Venugopal, C., Johns, A. E., Al-Qaysi, O., Lewis, A. M., O’Hare, T., Deininger, M., Singh, S. K., Luchman, A., Weiss, S., Fishel, M. L.,* and Gunning, P. T.* “Identification and characterization of AES-135, a potent HDAC inhibitor that prolongs survival in an orthotopic mouse model of pancreatic cancer. J. Med. Chem. 2019, 62, 2651-2665. IF = 3.746.


2018 (6 published)

86. Demarez, C., Gérard, C., Cordi, S., Poncy, A., Achouri, Y., Dauguet, N., Rosa, D. R., Gunning, P. T., Manfroid, I., Lemaigre, F. P. “MiR-337-3p balances hepatobiliary gene expression and controls the transcriptional dynamics during hepatic cell differentiation” Hepatology 2018, 67, 313-327. IF = 11.05.


85. Wingelhofer B., Neubauer H. A., Valent P., Han X., Constantinescu S.N., Gunning P.T., Müller M., and Moriggl R. ‘Implications of JAK-STAT signaling on gene regulation and chromatin remodeling in cancer.’ Leukemia 2018, 32, 1713-1726. IF = 11.702.


84. Geletu, M., Mohan, R., Arulanandam, R., Berger, A., Nabi I., Gunning P. T. and Raptis, L. “Reciprocal regulation of the Cadherin-11/Stat3 axis by caveolin-1 in mouse fibroblasts and lung carcinoma cells.” BBA Molecular Cell Research 2018, 5, 1865. IF = 4.521.


83. Wingelhofer B., Maurer B., Heyes E. C., Cumaraswamy A. A., Berger A., de Araujo E. D., Orlova A., Freund P., Ruge F., Park F., Tin G., Ahmar S., Lardeau C. H., Sadovnik I., Bajusz D., Keserű G. M., Grebien F., Kubicek S., Valent P., Gunning P.T.,* and Moriggl R.* “Pharmacologic inhibition of STAT5 in acute myeloid leukemia.”
Leukemia 2018, 32, 1135. IF = 11.702.


82. Orlova A., Wingelhofer B., Neubauer H. A., Maurer B., Berger A., Keserű G. M., Gunning P. T., Valent P., and Moriggl R.* “Emerging therapeutic targets in myeloproliferative neoplasms and peripheral T cell leukemias and lymphomas.” Ex. Opin. Ther. Targets. 2018, 22, 45-57. IF = 4.598


2017 (10 Papers)

81. Murcar-Evans, B. I., Cabral, A. D., French, S., Toutah, K., De Araujo, E. D., Lai, A., Macdonald, P. M., Brown, E. D., Kraskouskaya, D., and Gunning, P. T.* “ProxyPhos sensors for the detection and quantification of negatively charged membranes.” Analyst. 2017, 142, 4511-4521. IF = 4.107.


80. Gleixner, K. V., Schneeweiss, M., Herrmann, H., Blatt, K., Berger, D., Eisenwort, G., Greiner, G., Byrgazov, K., Hoermann, G., Konopleva, M., Fang, J., Cumaraswamy, A. C., Gunning, P. T., Maeda, H., Moriggl, R., Deininger, M., Lion, T., Andreeff, M., Valent, P. “Combined targeting of STAT3 and STAT5: a novel approach to overcome drug resistance in Ph+ CML.” Haematologica 2017, 102, 1519-1529.  IF = 6.671.


79. Cabral, A. D., Murcar-Evans, B. I., Toutah, K., Bancerz, M., Rosa, D., Yuen, K., Radu, T. B., Ali, M., Penkul, A., Kraskouskaya, D., Gunning, P. T.* “Characterization and application studies of ProxyPhos, a chemosensor for the detection of proximally phosphorylated peptides and proteins in aqueous solutions.” Analyst 2017, 142, 3922-3933. IF = 4.107.


78. Niit, M., Arulanandam, R., Cass, J., Geletu, M., Gunning, P. T., Elliott, B., and Raptis, L. “Regulation of HC11 Mouse Breast Epithelial Cell Differentiation by the E-cadherin/Rac axis.” Exp Cell Res. 2017 361, 112-125. IF = 3.546


77. De Araujo, E. D., Manaswiyoungkul, P., Israelian, J., Yuena, K., Farhangia, S., Berger, A., Abu Jazar, L., Gunning, P. T.* “High-throughput thermofluor-based assays for inhibitor screening of STAT SH2 domains.” J. Pharm. Biomed. Anal. 2017, 143, 159-167. IF = 3.169.


76. Kraskouskaya, D., Cabral, A. D., Fong, R., Bancerz, M., Rosa, D. A., Gardiner, J. E., De Araujo, E. D., Duodu, E., Armstrong, D., Fekl, U., Gunning, P. T.* “Characterization and application studies of ProxyPhos, a chemosensor for the detection of proximally phosphorylated peptides and proteins in aqueous solutions.” Analyst 2017,142, 2451-2459. IF = 4.107.


75. Paiva, S-L, da Silva, S. R., de Araujo, E., Gunning, P. T.* “Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site.” J. Med. Chem. 2017, 61, 405-421.


74. Garg, N., Bakhshinyan, D., Venugopal, C., Rosa, D. A., Vijayakumar, T., Manoranjan, B., Hallett, R., McFarlane, N., Mahendram, S., Delaney, K., Kwiecien, J., Arpin, C. C., Lai, P-S., Gomez-Biagi, R. F., Ali, A. M., Ajani, O. A., Hassell, J., Gunning, P. T., Singh, S. K. “CD133+ brain tumour initiating cells are dependent on STAT3 signaling to drive medulloblastoma recurrence.” Oncogene 2017, 5, 606-617. IF = 6.854.


73. de Araujo, E. D., Geletu, M., Gunning, P. T.* “Strategies for over-expression and purification of recombinant full length STAT5B in Escherichia coli.” Protein Expr. Purif. 2017, 129, 1-9. IF = 1.695.


Papers Published in 2016 (11 papers)

72. Gottardt, D., Maurer, B., Nivarthi, H., Wingelhofer, B., Prchal-Murphy, M., Chen, D., Winkler, S., Merkel, O., Schlederer, M., Prochazkova, J., Schiefer, A-S., Gurnhofer, E., Hofbauer, M., Thi Thanh Pham, H., Hochgatterer, B., Bauer, E., Hoermann, G., Hoelbl-Kovacic, A., Cumaraswamy, A. A., Lewis, A. M., Eder, J., Kitzwoegerer, M., Han, X., Valent, P., Stoiber, D., Kolbe, T., Loizou, J. I., Grebien, F., Kenner, L., Gunning, P. T., Kralovics, R., Sexl, V., Mueller, M., Rülicke, T., Moriggl, R. “STAT5 is a key regulator in NK cells and act as molecular switch from tumor surveillance to tumor promotion.” Cancer Discovery, 2016, 4, 414-429. IF = 19.453.


71. Gunning, P. T.,* Kraskouskaya, D., Park, J., Cabral, A. D., Gomez-Biagi, R. F. ‘Fluorescence-based Chemosensors for the detection of biologically relevant Phosphates in water.’ Book chapter in ‘Comprehensive Supramolecular Chemistry II’ 2016 ISBN: 978-0-12-803199-5


70. Linher-Melville, K., Nashed, M. G., Ungard, R., Gunning, P. T., Singh, G. “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.” PLoSOne. 2016, 11: e0161202. IF = 2.776.


69. Wilson A.* and Gunning P. T.* “Understanding Protein–Protein Interactions: Essential Players in (Patho)physiology.” ChemMedChem 2016, 11, 732-733. IF = 3.016.


68. Ali, A.M., Gómez-Biagi, R. F., Rosa, D. A.,  Lai, P-S., Heaton, W. L., Park, J., Eiring, A. M., Vellore, N. A., de Araujo, E. D., Ball, D. P., Shouksmith, A. E., Patel, A. B., O’Hare, T., Deininger, M. W., Gunning, P. T.* “Disarming an electrophilic warhead: Retaining potency in TKI-resistant CML cell lines, while circumventing pharmacokinetic liabilities.” ChemMedChem 2016, 11, 850–861. IF = 3.016.


67. Belton, A., Koo, M., Huso, D., Huso, T., Xian, L., Turkson, J., Gunning, P. T.*, Resar, L. “STAT3 inhibitor has potent anti-tumor activity in B-lineage acute lymphoblastic leukemia cells overexpressing the High Mobility Group A1 (HMGA1)-STAT3 pathway.” Leukemia and Lymphoma. 2016, 11: 2681-2684. IF = 3.093.


66. Ball, D. P., Lewis, A. M., Williams, D., Resetca, D., Wilson, D. J., Gunning, P. T. “Signal transducer and activator of transcription 3 (STAT3) inhibitor, S3I-201, acts as a potent and non-selective alkylating agent.” Oncotarget. 2016, 7, 20669-20679. IF = 6.63.


65. Arpin, C. C., Mac, S., Cheng, H., Jiang, Y., Page, B. D. G., Kamocka, M. M., Haftchenary, S., Su, H., Ball, D., Rosa, D., Lai, P-S., Gómez-Biagi, R. F., Ali, A. M., Kerman, K., Fishel, M. L., and Gunning, P. T. “Applying Small Molecule Signal Transducer and Activator of Trancription-3 (STAT3) Protein Inhibitors as Pancreatic Cancer Therapeutics.” Mol. Cancer Ther. 2016, 5, 794-805. IF = 6.107.


64. da Silva, S. R., Paiva, S-L., Bancerz, M., Geletu, M., Lewis, A. M., Chen, J., Cai, Y., Lukkarila, J. L., Dhe-Paganon, S., Li, H., Gunning, P. T, ‘A selective inhibitor of the UFM1-activating enzyme, UBA5.’ BMCL 2016, 26, 4542-4547. IF = 2.42


63. Duodu, E., Kraskouskaya, D., Gunning, P. T. “A tool for the selective sequestration of ATP and PPi to aid in-solution phosphopeptide detection assays.” Analyst 2016, 141, 820 – 822. IF = 3.864.


62. Shouksmith, A. E., Gunning, P. T. “Targeting Signal Transducer and Activator of Transcription (STAT) 3 with Small Molecules.” Book chapter in ‘Small Molecule Transcription Factors in Oncology.’ by Royal Society of Chemistry Book, 2016, ISBN: 9781788015271


Papers Published in 2015 (9 papers)

61. Lai, P.L., Rosa, D. A., Ali, A. M., Gomez-Biagi, R. E., Ball, D. P., Shouksmith, A. E., Gunning, P. T. “A STAT inhibitor patent review: progress since 2011.” Ex. Opin. Ther. Pat. 2015, 12, 1397-421. IF = 4.297.


60. Haftchenary, S, Jouk, A. O., Aubry, I., Lewis, A. M., Landry, M., Ball, D. P., Shouksmith, A. E., Collins, C. V., Tremblay, M. L.,* Gunning, P. T.* “Identification of Bidentate Salicylic Acid Inhibitors of PTP1B” ACS Med. Chem. Lett. 2015, 6, 982–986. IF = 3.120.


59. Singh, M., Garg, N., Venugopal, C., Hallett, R., Tokar, T., McFarlane, N., Arpin, C. C., Page, B. D. G., Haftchenary, S., Todic, A., Rosa, D. A., Lai, P-S., Gómez-Biagi, R., Ali, M., Lewis, A., Geletu, M., Mahendram, S., Bakhshinyan, D., Manoranjan, B., Vora, P., Qazi, M., Murty, N. K., Hassell, J. A., Jurisica, I., Gunning, P. T., Singh, S. K. “STAT3 pathway regulates lung-derived brain metastasis initiating cell capacity through miR-21 activation.” Oncotarget 2015, 6, 27461-27477. IF = 6.63.


58. Linher-Melville, K., Haftchenary, S., Gunning, P. T., Singh, G.* “Signal transducer and activator of transcription 3 and 5 regulate system Xc- and redox balance in human breast cancer cells.” Mol. Cell. Biochem. 2015, 405, 205-221. IF = 2.388.


57. Lewis, A. M., Rana, R., Park, J-S., Gomez, R., Shaheen, A., Rosa, D., Gunning, P. T. “Developing inhibitors of STAT proteins: Targeting downstream of the kinases for treating disease.” Book chapter in “Kinomics: Approaches and Applications” by Wiley-VCH 2015, ISBN: 978-3-527-33765-1


56. Zeidan, N., Su, H., Aitken, M., Gunning, P. T., Kerman, K.* “Magnetic bead-based electrochemical detection of interaction between epigallocatechin-3-gallate and STAT proteins.” Anal. Methods, 2015, 7, 3566-3569. IF = 1.938.


55. Arabzadeh, A., Dupaul-Chicoine, J., Breton, V., Haftchenary, S., Yumeen, S., Turbide, C., Saleh, M., McGregor, K., Greenwood, C. M. T., Akavia, U. D., Blumberg, R. S., Gunning, P. T., Beauchemin, N. “Carcinoembryonic Antigen Cell Adhesion Molecule 1 long isoform modulates malignancy of poorly differentiated colon cancer cells.” Gut 2015, 65, 821-829. IF = 13.319.


54. Duodu, E., Kraskouskaya, D., Campbell, J., Graca-Lima, G., Gunning, P. T. “Selective detection of tyrosine-containing proximally phosphorylated motifs using an antenna-free Tb3+ luminescent sensor.” ChemComm 2015, 51, 6675 - 6677. IF = 6.718.


53. Eiring, A. M., Page, B. D. G., Kraft, I. L., Zhang, T. Y., Vellore N. A., Reynolds, K. R., Senina, A., Pomicter, A. D., Khorashad, J. S., Gu, Z., Anderson, D. J., Zabriskie, M. S., Arpin, C. C., Cologouri, R., Ahmad, S., Moriggl, R., Baron, R., O’Hare, T., Gunning, P. T.,* Deininger, M. W.*  “Combined STAT3 and BCR-ABL1 Inhibition Induces Synthetic Lethality in Therapy-Resistant Chronic Myeloid Leukemia.” Leukemia 2015, 29, 586-597. IF = 9.379.


2014 (6 publications in 2014)

52. Resetca, D., Haftchenary, S., Gunning, P. T., Wilson, D. J.* “Changes in Signal Transducer and Activator of Transcription 3 (STAT3) Dynamics Induced by Complexation with Pharmacological Inhibitors of Src Homology 2 (SH2) Domain Dimerization.” J. Biol. Chem. 2014, 289, 32538-32547. IF = 4.600.


51. Cumaraswamy, A.A., Lewis, A. M., Geletu, M., Todic, A., Diaz, D. B., Cheng, X. R., Brown, C. E., Laister, R. C., Muench, D., Kerman, K., Grimes, L. H., Minden, M. D., Gunning, P. T.* “Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein.” ACS Med Chem Lett. 2014, 19, 1202-1206. IF = 3.073.


50. Xu, G. W., Toth, J. I., daSilva, S., Paiva, S. L., Lukkarila, J. L., Hurren, R., MacLean, N., Sukhai, M. A., Bhattacharjee, R., Goard, C. A., Gunning, P. T., Dhe-Paganon, S., Petroski, M. D.,* Schimmer, A. D.* “Mutations in UBA3 Confer Resistance to the NEDD8-Activating Enzyme Inhibitor MLN4924 in Human Leukemic Cells.” PLOSone 2014, 9, (e93530) 1-10. IF = 3.534.


49. Lai, A. Z., Cory, S., Zhao, H., Gigoux, M., Monast, A., Guiot, M. C., Huang, S., Tofigh, A., Thompson, C., Naujokas, M., Marcus, V. A., Bertos, N., Sehat, B., Perera, R. M., Bell, E. S., Page, D. G. B., Gunning, P. T., Ferri, L.E., Hallett, M.L., Park, M.* “Dynamic reprogramming of signaling upon Met inhibition reveals pathways for cell proliferation and negative feedback in gastric cancer.” Science Signaling 2014, 7, (ra38) 1-15. IF = 7.648.


48. Kraskouskaya, D., Bancerz, M., Soor, H. S., Gardiner, J. E., Gunning, P. T.* “An excimer-based, turn-on fluorescent sensor for the selective detection of di-phosphorylated proteins in aqueous solution and polyacrylamide gels.” J. Am. Chem. Soc. 2014, 136, 1234–1237. IF = 11.444.


47. Martic, S., Rains, M. K, Haftchenary, S., Shahani, V. M., Kraskouskaya, D., Ball, D. P., Gunning, P. T., Kraatz, H-B.* “Electrochemical detection of the Fc-STAT3 phosphorylation and STAT3–Fc-STAT3 dimerization and inhibition.” Mol. Bio. Syst. 2014, 10, 576-580. IF = 3.183.



46. Haftchenary, S., Luchman, H. A. Jouk, A. O., Veloso, A. J., Page, B. D. G., Cheng, X. R., Dawson, S. S., Grinshtein, N., Shahani, V. M., Kerman, K., Kaplan, D. R., Griffin, C., Aman, A. M., Al-awar, R., Weiss, S.* Gunning, P. T.* “Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.” ACS Med. Chem. Lett. 2013, 4, 1102-1107. IF = 3.441.


45. Shahani, V. M., Ball, D. P., Ramos, A. V., Li, Z., Spagnuolo, P. A., Haftchenary, S., Schimmer, A. D., Trudel, S., Gunning, P. T.* “A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells.” Bioorg. Med. Chem. 2013, 21, 5618-28. IF = 3.205.


44. Page, B. D. G., Croucher, D., Li, Z. H., Haftchenary, S., Jimenez-Zepeda, V., Atkinson, J., Spagnuolo, P., Wong, Y. L., Colaguori, R., Lewis, A. M., Schimmer, A. D., Trudel, S., Gunning, P. T. “Inhibiting Aberrant Signal Transducer and Activator of Transcription Protein Activation with Tetrapodal, Small Molecule Src Homology 2 Domain Binders: Promising Agents against Multiple Myeloma.” J. Med.Chem. 2013, 56, 7190-7200. IF = 5.480.


43. Haftchenary, S., Ball, D. P., Aubry, I., Landry, M., Shahani, V. M., Fletcher, S., Page, B. D. G., Jouk, A. O., Tremblay, M. L., Gunning, P. T.*  “Identification of a potent salicylic acid-based inhibitor of tyrosine phosphatase PTP1B.” RSC Med. Chem. Comm. 2013, 4, 987-992. IF = 2.495.


42. Avadisian, M. A., Gunning, P. T.* “Extolling the Benefits of Molecular Therapeutic Lipidation.”Mol. Bio. Syst. 2013, 9, 2179-2188. IF = 3.183.


41. da Silva, S. R., Paiva, S-L., Lukkarila, J., Gunning, P. T.* "Exploring a new frontier in cancer treatment: Targeting the ubiquitin and ubiquitin-like activating enzymes." J. Med. Chem. 2013, 56, 2165–2177. IF = 5.480.


40. Camporeale, A., Marino, F., Papageorgiou, A., Carai, P., Fornero, S., Fletcher, S., Page, B. D. G., Gunning, P. T., Chiarle, R., Morello, M., Jenssen, O., Levi, R., Heymans, S., Poli, V. “STAT3 activity is necessary and sufficient for the development of immune-mediated myocarditis in mice and promotes progression to dilated cardiomyopathy.” EMBO Mol. Med. 2013, 5, 1-19. IF = 9.390.


39. Zhang, W., daSilva, S., Pavia, S. L., Lukkarila, J., Schimmer, A. D., Gunning, P. T.* “Targeting the ubiquitin E1 as a novel anti-cancer strategy.” Curr. Pharma. Design 2013, 19, 3201-2209. IF = 3.288.


38. Kraskouskaya, D., Duodu, E., Arpin, C. C., Gunning, P. T.* “Progress towards the development of SH2 domain inhibitors.”  Chem. Soc. Rev., 2013, 42, 3337-3370. IF = 30.425.


37. Kraskouskaya, D., Drewry, J. A., Duodu, E., Burger, S., Eaton, J., Gunning, P. T.* “Exploring the structural determinants of selective phosphopeptide recognition using bivalent metal-coordination complexes.” Med. Chem. Comm. 2013, 4, 289-292. IF = 2.626.



36. Drewry, J. A., Duodu, E., Mazouchi, A., Spaganueulo, P., Burger, S., Gradinaru, C. C., Ayers, P., Schimmer, A. D., Gunning, P. T.* “Phosphopeptide Selective Coordination Complexes as Promising Src Homology 2 Domain Mimetics.” Inorg. Chem, 2012, 51, 8284-8291. IF = 4.593.


35. Cumaraswamy, A., Gunning, P. T.* “Progress towards direct inhibitors of Stat5 protein.” Hormone Mol. Biol. Clin. Invest. 2012, 10, 281-286.


34. Burger, S., Lacasse, M., Verstraelen, T., Drewry, J. A., Gunning, P. T., Ayers, P. W. “Automated Parameterization of AMBER force field terms from vibrational analysis with a focus on functionalizing a dinuclear zinc(II) scaffold.” J. Chem. Theory and Comput. 2012, 8, 554-562. IF = 5.310.


33. Drewry, J. A., Duodu, E., Burger, S.,  Mazouchi, A.,  Ayers, P., Gradinaru, C. C., Gunning, P. T.* “Src Homology 2 Domain Proteomimetics: Developing Phosphopeptide Selective Receptors.” Med. Chem. Commun. 2012, 3, 763-770.  (LLSC, NSERC DG) (front cover article) IF = 2.626.


32. Mitra, R. N., Doshi, M., Zhang, Z., Tyus, J. C., Bengtsson, N., Fletcher, S., Page, B. D. G., Turkson, J., Gesquiere, A. J., Gunning, P. T., Walter G. A., Santra, S. “An activatable multimodal/multifunctional nanoprobe for direct imaging of intracellular drug delivery.” Biomaterials 2012, 33, 1500-1508. IF = 8.312.


31. Zhang, X., Yue, P., Page, B. D. G., Li, T., Zhao, W., Namanja, A. T., Paladino, D., Zhao, J., Chen, Y., Gunning, P. T.,* Turkson, J.* “Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts.” P. N. A. S. 2012, 109, 9623-9628. IF = 9.809.


30. Page, B. D. G., Khoury, H., Laister, R. C., Fletcher, S., Vellozo, M., Manzoli, A., Yue, P., Turkson, J., Minden, M. D.,* Gunning, P. T.* “Small Molecule STAT5-SH2 Domain Inhibitors Exhibit Potent Anti-leukemia Activity.” J. Med. Chem. 2012, 55, 1047-1055.  IF = 5.480.


29. Cumaraswamy, A., Todic, A., Resetca, D., Minden, M. D., Gunning, P. T.* “Inhibitors of Stat5 protein signalling.” MedChemComm, 2012, 3, 22-27. IF = 2.626.



28. Page, B. D. G., Fletcher, S., Li, Z., Zhang, X., Yue, P., Sharmeen, S., Datti, A., Wrana, J. L., Trudel, S., Schimmer, A. D., Turkson, J., Gunning, P. T.* “Identification of a Non-phosphorylated, Cell Permeable, Small Molecule Ligand for the Stat3 SH2 Domain.” Bioorg. Med. Chem. Lett. 2011, 21, 5605-5609. (front cover article) IF = 2.447.


27. Lukkarila, J., da Silva, S. R., Ali, M., Shahani, V. M., Wei, X., Berman, J., Roughton, A., DhePhaganon, S., Schimmer, A. D., Gunning, P. T.* “Identification of NAE inhibitors exhibiting potent activity in Leukemia cells: Exploring the structural determinants of NAE Specificity.” ACS Med. Chem. Lett. 2011, 2, 577-582. IF = 3.073.


26. Avadisian, M., Fletcher, S., Lui, B., Zhao, W., Yue, P., Badali, D., Xu, W., Schimmer, A. D., Turkson, J., Gradinaru, C. C., Gunning, P. T.* “Artificially Induced Protein–Membrane Anchorage with Cholesterol-Based Recognition Agents as a New Therapeutic Concept.” Angewandte Intl. Ed. 2011, 50, 6248-6253 (front cover article) IF = 13.734.


25. Fletcher, S., Page, B. D. G., Zhang, X., Yue, P., Li, Z-H., Sharmeen, S., Singh,J., Zhao, W., Schimmer, A. D., Trudel, S., Turkson, J.,* Gunning, P. T.* “Antagonism of the Stat3-Stat3 protein dimer with salicylic acid based small molecules.” ChemMedChem. 2011, 6, 1459-1470. IF = 3.046.


24. Shahani, V. M., Yue, P., Fletcher, S., Sharmeen, S., Sukhai, M. A., Luu, D. P., Zhang, X., Sun, H., Zhao, W., Schimmer, A. D., Turkson, J., Gunning, P. T.* “Design, synthesis, and in vitro characterization of novel hybrid peptidomimetic inhibitors of STAT3 protein.” Bioorg. Med. Chem. 2011,19, 1823-1838. (front cover article) IF = 3.205.


23. Shahani, V. M., Yue, P., Haftchenary, S., Zhao, W., Lukkarila, J., Zhang, X., Ball, D., Nona, C., Gunning, P. T.,* Turkson, J.* “Identification of Purine-Scaffold Small-Molecule Inhibitors of Stat3 Activation by QSAR Studies.” ACS. Med. Chem. Lett. 2011, 2, 79-84. Highlighted as a Top 20 most read articles in 2010-2011. IF = 3.073.


22. Page, B. D. G., Ball, D. P., Gunning, P. T.* “Signal transducer and activator of transcription 3 inhibitors: a patent review.” Expert Opin. Ther. Patents 2011, 21, 65-83. IF = 3.441.


21. Drewry, J. A., Gunning, P. T.* "Recent Advances in Biosensory and Medicinal Therapeutic Applications of Zinc(II) and Copper(II) Coordination Complexes." Coord. Chem. Rev., 2011, 255, 459-472. IF = 12.598.


20. Haftchenary, S., Avadisian, M., Gunning, P. T.* “Inhibiting aberrant Stat3 function with molecular therapeutics: a progress report.” Anticancer Drugs 2011, 22, 115-127. IF = 1.891.


19. Fletcher, S. Shahani, V. M., Lough, A. J., Gunning, P. T.* “Concise Access to N9-Mono, N2-Mono and N2, N9 Di-substituted Guanines via Efficient Mitsunobu Reactions.” Tetrahedron 2010, 66, 4621-4632. IF = 2.817.


18. Badali, D., Lui, B., Avadisian, M. A., Fletcher, S., Gunning, P. T., Gradinaru, C. "Development of Stat3 as an accessible target for fluorescence-based inhibition assays." JULS, 2010, 4, 18-22.


17. Zhang, X., Yue, P., Fletcher, S., Zhao, W., Gunning, P. T., Turkson, J. “A novel small-molecule disrupts Stat3 SH2 domain–phosphotyrosine interactions and Stat3-dependent tumor processes.” Biochem. Pharm. 2010, 79, 1398-1409. TOP-25 Hottest articles (ranked #7) IF = 4.772.


16. Drewry, J. A., Fletcher, S., Peibin, Y., Marushchak, D., Zhao, W., Sumaiya, S., Zhang, X., Zhang, X., Schimmer, A. D., Gradinaru, C., Turkson, J., Gunning, P. T.* “Coordination Complex SH2 Domain Proteomimetics: An Alternative Approach to Disrupting Oncogenic Protein–Protein Interactions.” Chem. Commun. 2010, 46, 892-894. (front cover) IF = 6.718.


15. Drewry, J. A., Fletcher, S., Hassan, H., Gunning, P. T.* “Novel asymmetrically functionalized bis-dipicolylamine metal complexes: peripheral decoration of a potent anion recognition scaffold.” Org. Biomol. Chem. 2009, 7, 5074–5077. (front cover) IF = 3.487.


14. Fletcher, S., Drewry, J. A., Shahani, V. M., Page, B. D. G., Gunning, P. T.* “Molecular disruption of oncogenic signal transducer and activator of transcription 3 (STAT3) protein.” Biochem. Cell Biol. 2009, 87, 825-833. IF = 2.915.


13. Fletcher, S., Singh, J., Zhang, X., Yue, P., Page, B. D. G., Sharmeen, S., Shahani, V. M., Zhao, W., Schimmer, A. D., Turkson, J., Gunning, P. T.* “Disruption of Transcriptionally Active Stat3 Dimers with Nonphosphorylated, Salicylic Acid-Based Small Molecules: Potent in vitro and Tumor Cell Activities.” ChemBioChem 2009, 10, 1959-1964. (front cover) IF = 3.060.


12. Liu, B., Badali, D., Fletcher, S., Avadisian, M., Gunning, P. T., Gradinaru, C. C.* "Single-Molecule Fluorescence Study of the Inhibition of the Oncogenic Functionality of STAT3." Proc. SPIE, 2009, 7386, 738605-1.


11. Liu, B., Fletcher, S., Avadisian, M., Gunning, P. T., Gradinaru, C. C.* "A photostable, pH-invariant fluorescein derivative for single-molecule microscopy." J. Fluoresc., 2009, 19, 915-920. IF = 1.667.


10. Fletcher, S., Shahani, V., Gunning, P. T.* "Facile and efficient access to 2,6,9-tri-substituted purines through sequential N9, N2 Mitsunobu reactions." Tet. Lett., 2009, 50, 4258-4261. IF = 2.295.


9. Fletcher, S., Turkson, J., Gunning, P. T.* "Molecular approaches towards the inhibition of the Signal Transducer and Activator of Transcription 3 (Stat3) Protein." ChemMedChem, 2008, 3, 1159-1168. IF = 3.046.


8. Fletcher, S., Gunning, P. T.* “Mild, efficient and rapid O-debenzylation of electron-withdrawing, ortho-substituted phenols with trifluoroacetic acid.” Tet. Lett. 2008, 49, 4817-4819. IF = 2.295.


Doctoral and Postdoctoral:

7. Gunning, P. T., Glenn, M., Siddiquee, K. A. Z., Katt, K. P., Masson, E., Sebti, S. M., Turkson, J., Hamilton, A. D. "Targeting protein-protein interactions: suppression of Stat3 dimerization via rationally designed small molecule, non-peptidic SH2 domain binders." ChemBioChem, 2008, 17, 2800-2803. IF = 3.060.


6. Siddiquee, K. A. Z., Gunning, P. T., Glenn, M., Katt, W. P., Zhang, S., Schroeck, C., Sebti, S. M., Jove, R., Hamilton, A. D., Turkson, J. "An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects." ACS Chem. Biol., 2007, 12, 787-798. IF = 5.356.


5. Gunning, P. T., Glenn, M., Turkson, J., Kim, J. S., Katt, W. P., Sebti, S. M., Jove, R., Hamilton, A. D."Isoform selective inhibition of Stat1 or Stat3 homodimerization via peptidomimetic probes: structural recognition of Stat SH2 domains." Bioorg. Med. Chem. Lett., 2007, 17, 1875-1878. IF = 2.447.


4. Fielden, J., Gunning, P. T., Long, D-L., Ellern, A., Nutley, A., Koegerler, P., Cronin, L."Anion control of isomerism, crystal packing and phosphate binding in a mononuclear zinc complex." Polyhedron, 2006, 25, 3474-3480. IF = 2.047.


3. Gunning, P. T., Peacock, R. D., Benniston, A. C. "Artificial zinc hydrolysis enzymes: synthesis of hybrid cyclophane-azamacrocyclic receptors." J. Org. Chem., 2005, 70, 115-123. IF = 4.564.


2. Gunning, P. T.* "Positive ion-pair cooperativity exhibited for the binding of phosphate under physiological conditions." Org. Biomol. Chem., 2005, 3, 3877-3879. IF = 3.487.


1. Gunning, P. T., Peacock, R. D., Benniston, A. C. "Modular ditopic crown-shielded phosphate ion pair receptor." Chem. Comm., 2004, 1, 2226-2227. IF = 6.718.




















Docs & Postdocs
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