Featured publications

Kinome profiling and cancer cell pathway identification studies:

In collaboration with GSK, NIH-NCI and Structural Genomic Consortium

Elkins JM, Fedele V, Szklarz M, Azeez KRA, Salah E, Mikolajczyk J et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016; 34 (1): 95–103. Google Scholar

Kinome profiling and Mechanism of action studies:

The study was performed for and in collaboration with Principia Biopharma

Bradshaw J. M.McFarland J. M.Paavilainen V. O., et al. Prolonged and Tunable Residence Time Using Reversible Covalent Kinase Inhibitors. Nat. Chem. Biol. 2015, 11 (7), 525531Google Scholar

Enzyme kinetics studies:

The study was performed for Pharmacyclics

Chen J, Kinoshita T, Sukbuntherng J, et al. Ibrutinib Inhibits ERBB Receptor Tyrosine Kinases and HER2-Amplified Breast Cancer Cell Growth. Endocr Relat Cancer 2016; 15: 689-708. Google Scholar


*published by customers and/or co-authored by Nanosyn

  1. Haak AJ, Ligresti G, Abbey R, Romanov S, Chung TD, Tschumperlin DJ. Image-Based Screening for Epigenetic Modifiers of Myofibroblast Activation. The FASEB Journal. 2017 Apr 1;31(1 Supplement):1060-3. Link
  2. Venetsanakos E, Brameld KA, Phan VT, Verner E, Owens TD, Xing Y, Tam D, LaStant J, Leung K, Karr DE, Hill RJ. The irreversible covalent fibroblast growth factor receptor inhibitor PRN1371 exhibits sustained inhibition of FGFR after drug clearance. Molecular Cancer Therapeutics. 2017 Jan 1:molcanther-0309. Link
  3. He X, Da Ros S, Nelson J, Zhu XF, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S, Jia Y. Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases. ACS Medicinal Chemistry Letters. 2017 Sep 27. Link
  4. Bollong MJ, Pietilä M, Pearson AD, Sarkar TR, Ahmad I, Soundararajan R, Lyssiotis CA, Mani SA, Schultz PG, Lairson LL. A vimentin binding small molecule leads to mitotic disruption in mesenchymal cancers. Proceedings of the National Academy of Sciences. 2017 Oct 30:201716009. Link
  5. Bisi JE, Sorrentino JA, Jordan JL, Darr DD, Roberts PJ, Tavares FX, Strum JC. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Jun 27;8(26):42343. Link
  6. Wang M, Kommidi H, Tosi U, Guo H, Zhou Z, Schweitzer ME, Wu LY, Singh R, Hou S, Law B, Ting R. A murine model for quantitative, real-time evaluation of convection-enhanced delivery (RT-CED) using an 18 [F]-positron emitting, fluorescent derivative of dasatinib. Molecular Cancer Therapeutics. 2017 Jan 1:molcanther-0423. Link
  7. Novotny CJ, Pollari S, Park JH, Lemmon MA, Shen W, Shokat KM. Overcoming resistance to HER2 inhibitors through state-specific kinase binding. Nature chemical biology. 2016 Nov 1;12(11):923-30. Link
  8. Mitton B, Chae HD, Hsu K, Dutta R, Aldana-Masangkay G, Ferrari R, Davis K, Tiu BC, Kaul A, Lacayo N, Dahl G. Small molecule inhibition of cAMP response element binding protein in human acute myeloid leukemia cells. Leukemia. 2016 Dec 1;30(12):2302-11. Link
  9. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC. Preclinical characterization of G1T28: A novel CDK4/6 inhibitor for reduction of chemotherapy-induced myelosuppression. Molecular cancer therapeutics. 2016 May 1;15(5):783-93. Link
  10. Sorrentino J, Bisi J, Roberts P, Strum J. G1T38, a novel, oral, potent and selective CDK 4/6 inhibitor for the treatment of Rb competent tumors. InProceedings of the 107th Annual Meeting of the American Association for Cancer Research 2016 Jul 1 (pp. 16-20). Link
  11. Borkin D, Pollock J, Kempinska K, Purohit T, Li X, Wen B, Zhao T, Miao H, Shukla S, He M, Sun D. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein–Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). Journal of medicinal chemistry. 2016 Jan 25;59(3):892-913. Link
  12. Zhang H, Sun S, Wu L, Pchitskaya E, Zakharova O, Tacer KF, Bezprozvanny I. Store-operated calcium channel complex in postsynaptic spines: a new therapeutic target for Alzheimer’s disease treatment. Journal of Neuroscience. 2016 Nov 23;36(47):11837-50. Link
  13. Federspiel JD, Codreanu SG, Goyal S, Albertolle ME, Lowe E, Teague J, Wong H, Guengerich FP, Liebler DC. Specificity of protein covalent modification by the electrophilic proteasome inhibitor carfilzomib in human cells. Molecular & Cellular Proteomics. 2016 Oct 1;15(10):3233-42. Link
  14. Smith GA, Uchida K, Weiss A, Taunton J. Essential biphasic role for JAK3 catalytic activity in IL-2 receptor signaling. Nature chemical biology. 2016 May 1;12(5):373-9. Link
  15. Yu S, Pearson AD, Lim RK, Rodgers DT, Li S, Parker HB, Weglarz M, Hampton EN, Bollong MJ, Shen J, Zambaldo C. Targeted Delivery of an Anti-inflammatory PDE4 Inhibitor to Immune Cells via an Antibody–drug Conjugate. Molecular Therapy. 2016 Oct 12. Link
  16. Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A, Owens TD. Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694. Journal of Biological Chemistry. 2015 Mar 6;290(10):5960-78. Link
  17. Bisi JE, White HS, Sorrentino JA, Roberts PJ, Strum JC. Pre-clinical characterization of G1T28-1, a novel CDK 4/6 inhibitor for protection of bone marrow from cytotoxic chemotherapies. InCancer Research 2015 Aug 1 (Vol. 75). 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH. Link
  18. de Groot J, Thomas C, Piao Y, Nguyen N, Drewry D, Zuercher B, Verhaak R, Stephan C, Sulman EP, Lang F, Yung A. High-throughput Screening Of Glioma Stem Cell Lines For Drug Structure-And Genotype-correlated Sensitivity To A Panel Of Tyrosine Kinase Inhibitors. Neuro-oncology. 2014 Jul 1;16(suppl_3):iii32-. Link
  19. London N, Miller RM, Krishnan S, Uchida K, Irwin JJ, Eidam O, Gibold L, Cimermančič P, Bonnet R, Shoichet BK, Taunton J. Covalent docking of large libraries for the discovery of chemical probes. Nature chemical biology. 2014 Dec 1;10(12):1066-72. Link
  20. Spicer TP, Jiang J, Taylor AB, Choi JY, Hart PJ, Roush WR, Fields GB, Hodder PS, Minond D. Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. Journal of medicinal chemistry. 2014 Nov 11;57(22):9598-611. Link
  21. Wecksler AT, Hwang SH, Wettersten HI, Gilda JE, Patton A, Leon LJ, Carraway III KL, Gomes AV, Baar K, Weiss RH, Hammock BD. Novel Sorafenib-Based Structural Analogues: In Vitro Anticancer Evaluation of t-MTUCB and t-AUCMB. Anti-cancer drugs. 2014 Apr;25(4):433. Link
  22. Kong Q, Chang LC, Takahashi K, Liu Q, Schulte DA, Lai L, Ibabao B, Lin Y, Stouffer N, Mukhopadhyay CD, Xing X. Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotection. The Journal of clinical investigation. 2014 Mar 3;124(3):1255. Link
  23. Lauffer BE, Mintzer R, Fong R, Mukund S, Tam C, Zilberleyb I, Flicke B, Ritscher A, Fedorowicz G, Vallero R, Ortwine DF. Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. Journal of Biological Chemistry. 2013 Sep 13;288(37):26926-43. Link
  24. Hanson JE, La H, Plise E, Chen YH, Ding X, Hanania T, Sabath EV, Alexandrov V, Brunner D, Leahy E, Steiner P. SAHA enhances synaptic function and plasticity in vitro but has limited brain availability in vivo and does not impact cognition. PLoS One. 2013 Jul 26;8(7):e69964. Link
  25. Kozyrev A, Ethirajan M, Chen P, Ohkubo K, Robinson BC, Barkigia KM, Fukuzumi S, Kadish KM, Pandey RK. Synthesis, photophysical and electrochemistry of near-IR absorbing bacteriochlorins related to bacteriochlorophyll a. The Journal of organic chemistry. 2012 Oct 31;77(22):10260-71. Link
  26. Hill RJ, Bisconte A, Bradshaw JM, Brameld K, Kim EO, Li X, Owens T, Verner E, Goldstein DM, Biopharma P. Discovery of a highly potent, selective, reversible covalent inhibitor of JAK3. Arthritis Rheum. 2012;64(Suppl 10):2326. Link
  27. Harvey JH, Long DH, England PM, Whistler JL. Tuned-affinity bivalent ligands for the characterization of opioid receptor heteromers. ACS medicinal chemistry letters. 2012 Jul 18;3(8):640-4. Link
  28. He R, Chen Y, Chen Y, Ougolkov AV, Zhang JS, Savoy DN, Billadeau DD, Kozikowski AP. Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents. Journal of medicinal chemistry. 2010 Jan 7;53(3):1347-56. Link
  29. Bezprozvanny I. The rise and fall of Dimebon. Drug news & perspectives. 2010 Oct;23(8):518. Link
  30. Martin MT, Dix DJ, Judson RS, Kavlock RJ, Reif DM, Richard AM, Rotroff DM, Romanov S, Medvedev A, Poltoratskaya N, Gambarian M. Impact of environmental chemicals on key transcription regulators and correlation to toxicity end points within EPA’s ToxCast program. Chemical research in toxicology. 2010 Feb 10;23(3):578-90. Link
  31. Blackwell LJ, Birkos S, Hallam R, Van De Carr G, Arroway J, Suto CM, Janzen WP. High-throughput screening of the cyclic AMP-dependent protein kinase (PKA) using the caliper microfluidic platform. High Throughput Screening: Methods and Protocols, Second Edition. 2009:225-37. Link
  32. Chen Y, He R, Chen Y, D’Annibale MA, Langley B, Kozikowski AP. Studies of Benzamide‐and Thiol‐Based Histone Deacetylase Inhibitors in Models of Oxidative‐Stress‐Induced Neuronal Death: Identification of Some HDAC3‐Selective Inhibitors. ChemMedChem. 2009 May 11;4(5):842-52. Link
  33. Wu J, Li Q, Bezprozvanny I. Evaluation of Dimebon in cellular model of Huntington’s disease. Molecular Neurodegeneration. 2008 Oct 21;3(1):15. Link
  34. Lally BE, Geiger GA, Kridel S, Arcury-Quandt AE, Robbins ME, Kock ND, Wheeler K, Peddi P, Georgakilas A, Kao GD, Koumenis C. Identification and biological evaluation of a novel and potent small molecule radiation sensitizer via an unbiased screen of a chemical library. Cancer research. 2007 Sep 15;67(18):8791-9. Link
  35. Wang H, Han H, Von Hoff DD. Identification of an Agent Selectively Targeting DPC4 (Deleted in Pancreatic Cancer Locus 4)–Deficient Pancreatic Cancer Cells. Cancer research. 2006 Oct 1;66(19):9722-30. Link
  36. Popa-Burke IG, Issakova O, Arroway JD, Bernasconi P, Chen M, Coudurier L, Galasinski S, Jadhav AP, Janzen WP, Lagasca D, Liu D. Streamlined system for purifying and quantifying a diverse library of compounds and the effect of compound concentration measurements on the accurate interpretation of biological assay results. Analytical chemistry. 2004 Dec 15;76(24):7278-87. Link
  37. Wellendorph P, Goodman MW, Burstein ES, Nash NR, Brann MR, Weiner DM. Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H 3 receptor. Neuropharmacology. 2002 Jun 30;42(7):929-40. Link
  38. Ma Y, Stern RJ, Scherman MS, Vissa VD, Yan W, Jones VC, Zhang F, Franzblau SG, Lewis WH, McNeil MR. Drug targeting Mycobacterium tuberculosis cell wall synthesis: genetics of dTDP-rhamnose synthetic enzymes and development of a microtiter plate-based screen for inhibitors of conversion of dTDP-glucose to dTDP-rhamnose. Antimicrobial agents and chemotherapy. 2001 May 1;45(5):1407-16. Link
  39. Mazurov A. Solid phase synthesis of 5, 6, 7, 8-tetrahydro-1H-imidazo [4, 5-g] quinoxalin-6-ones. Tetrahedron Letters. 2000 Jan 1;41(1):7-10. Link
  40. Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG. Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl) propyl)-6-(2, 6-dichloro-3, 5-dimethoxyphenyl)-2-(methylamino) pyrido [2, 3-d] pyrimidin-7 (8 H)-one (PRN1371) for the Treatment of Solid Tumors. Link
  41. Novotny CJ. Discovery and Design of Next Generation Inhibitors to Targeting the HER2/HER3 Heterodimer and K-Ras (Doctoral dissertation, University of California, San Francisco). Link