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RESEARCH AND DEVELOPMENT AT MILLENNIUM
Research and Development Engine
PUBLICATIONS 2004
Sasseville VG, Lane JH, Kadambi VJ, Bouchard P, Lee FW, Balani SK, Miwa GT, Smith PF, Alden CL. 2004 Testing paradigm for prediction of development-limiting barriers and human drug toxicity. Chem Biol Interactions 150(1):9-25.
Veiby OP, Read MA. 2004 Chemoresistance: impact of nuclear factor (NF)-kappaB inhibition by small interfering RNA. Commentary re J. Guo et al., Enhanced chemosensitivity to irinotecan by RNA interference-mediated down-regulation of the NF-kappaB p65 subunit. Clin Cancer Res 2004;10:3333-3341. Clinical Cancer Research. 10(10):3262-4.
Kuhn E, Wu J, Karl J, Liao H, Zolg W, Guild B. 2004 Quantification of C-reactive protein in the serum of patients with rheumatoid arthritis using multiple reaction monitoring mass spectrometry and 13C-labeled peptide standards. Proteomics. 4(4):1175-86.
Henry MD, Wen S, Silva MD, Chandra S, Milton M, Worland PJ. 2004 A prostate-specific membrane antigen-targeted monoclonal antibody-chemotherapeutic conjugate designed for the treatment of prostate cancer. Cancer Research. 64(21):7995-8001.
Pradines J, Rudolph-Owen L, Hunter J, Leroy P, Cary M, Coopersmith R, Dancik V, Eltsefon Y, Farutin V, Leroy C, Rees J, Rose D, Rowley S, Ruttenberg A, Wieghardt P, Sander C, Reich C. 2004 Detection of activity centers in cellular pathways using transcript profiling. Journal of Pharmaceutical Statistics. 14(3):701-21.
Sappal DS, McClendon AK, Fleming JA, Thoroddsen V, Connolly K, Reimer C, Blackman RK, Bulawa CE, Osheroff N, Charlton P, Rudolph-Owen LA. 2004 Biological characterization of MLN944: a potent DNA binding agent. Molecular Cancer Therapeutics. 3(1):47-58.
Fang L, Yan Y, Komuves LG, Yonkovich S, Sullivan CM, Stringer B, Galbraith S, Lokker NA, Hwang SS, Nurden P, Phillips DR, Giese NA. 2004 PDGF C is a selective alpha platelet-derived growth factor receptor agonist that is highly expressed in platelet alpha granules and vascular smooth muscle. Arteriosclerosis, Thrombosis and Vascular Biology. 24(4):787-92.
Towler P, Staker B, Prasad SG, Menon S, Tang J, Parsons T, Ryan D, Fisher M, Williams D, Dales NA, Patane MA, Pantoliano MW. 2004 ACE2 X-ray structures reveal a large hinge-bending motion important for inhibitor binding and catalysis. Journal of Biological Chemistry. 279(17):17996-8007.
Ross JS, Schenkein DP, Pietrusko R, Rolfe M, Linette GP, Stec J, Stagliano NE, Ginsburg GS, Symmans WF, Pusztai L, Hortobagyi GN. 2004 Targeted therapies for cancer 2004. American Journal of Clinical Pathology.122 (4):598-609.
Schmidt-Supprian M, Tian J, Grant EP, Pasparakis M, Maehr R, Ovaa H, Ploegh HL, Coyle AJ, Rajewsky K. 2004 Differential dependence of CD4+CD25+ regulatory and natural killer-like T cells on signals leading to NF-kappaB activation. Proceedings of the National Academy of Sciences. 101(13):4566-71.
Schmidt-Supprian M, Tian J, Ji H, Terhorst C, Bhan AK, Grant EP, Pasparakis M, Casola S, Coyle AJ, Rajewsky K. 2004 I kappa B kinase 2 deficiency in T cells leads to defects in priming, B cell help, germinal center reactions, and homeostatic expansion. Journal of Immunology 173(3):1612-9.
Coyle AJ, Gutierrez-Ramos JC. 2004 The role of ICOS and other costimulatory molecules in allergy and asthma. Springer Seminars in Immunopathology. 25(3-4):349-59.
Heath JA, Mehrotra MM, Chi S, Yu JC, Hutchaleelaha A, Hollenbach SJ, Giese NA, Scarborough RM, Pandey A. 2004 Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor. Bioorganic Medicinal Chemistry Letters. 14(19):4867-72.
Clark JJ, Cools J, Curley DP, Yu JC, Lokker NA, Giese NA, Gilliland DG. 2004 Variable sensitivity of FLT3 activation loop mutations to the small molecule tyrosine kinase inhibitor MLN518. Blood. 104(9):2867-72.
Blackman RK, Amidon BS. 2004 Microarray approach for cloned library quality assessment and the comprehensive identification of positives from library screens. Biotechniques. 37(4):536, 538, 540.
Scarborough RM. 2003 Protease-activated receptor-2 antagonists and agonists. Curr Med Chem Cardiovasc Hematol Agents. (1):73-82.
Bembenek ME, Roy R, Li P, Chee L, Jain S, Parsons T. A homogeneous scintillation proximity format for monitoring the activity of recombinant human long-chain-fatty-acyl-CoA synthetase 5. Assay and Drug Development Technologies.  2(3):300-7.
Roubenoff R. 2004 Sarcopenic obesity: the confluence of two epidemics. Obesity Research. 12(6):887-8.
Yang P, Macdonald F. 2004 Solution stability of factor Xa inhibitors as a function of pH. Drug Development and Industrial Pharmacy. 30(9):967-73.
Ross JS, Schenkein DP, Kashala O, Linette GP, Stec J, Symmans WF, Pusztai L, Hortobagyi GN. 2004 Pharmacogenomics. Advances in Anatomic Pathology. 11(4):211-20.
Balani SK, Li P, Nguyen J, Cardoza K, Zeng H, Mu DX, Wu JT, Gan LS, Lee FW. 2004 Effective dosing regimen of 1-aminobenzotriazole for inhibition of antipyrine clearance in Guinea pigs and mice using serial sampling. Drug Metabolism and Distribution. 32(10):1092-5.
Trepicchio WL, Williams GA, Essayan D, Hall ST, Harty LC, Shaw PM, Spear BB, Wang SJ, Watson ML. 2004 Pharmacogenomic data submissions to the FDA: clinical case studies. Pharmacogenomics. 5(5):519-24.
Marsilje TH, Roses JB, Calderwood EF, Stroud SG, Forsyth NE, Blackburn C, Yowe DL, Miao W, Drabic SV, Bohane MD, Scott Daniels J, Li P, Wu L, Patane MA, Claiborne CF. 2004 Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).  Bioorganic and Medicinal Chemistry Letters. 14(14):3721-5.
Adams J, Kauffman M. 2004 Development of the proteasome inhibitor Velcade (Bortezomib). Cancer Investigation. 22(2):304-11.
Sullivan B, Addona TA, Carr SA. 2004 Selective detection of glycopeptides on ion trap mass spectrometers. Annals of Chemistry. 76(11):3112-8.
Ayers M, Symmans WF, Stec J, Damokosh AI, Clark E, Hess K, Lecocke M, Metivier J, Booser D, Ibrahim N, Valero V, Royce M, Arun B, Whitman G, Ross J, Sneige N, Hortobagyi GN, Pusztai L. 2004 Gene expression profiles predict complete pathologic response to neoadjuvant paclitaxel and fluorouracil, doxorubicin, and cyclophosphamide chemotherapy in breast cancer. Journal of Clinical Oncology. 22(12):2284-93.
Perreault M, Istrate N, Wang L, Nichols AJ, Tozzo E, Stricker-Krongrad A. 2004 Resistance to the orexigenic effect of ghrelin in dietary-induced obesity in mice: reversal upon weight loss. International Journal of Obesity.  28(7):879-85.
Gretler DD, Guerciolini R, Williams PJ. 2004 Pharmacokinetic and pharmacodynamic properties of eptifibatide in subjects with normal or impaired renal function. Clinical Therapeutics. 26(3):390-8.
Jia ZJ, Su T, Zuckett JF, Wu Y, Goldman EA, Li W, Zhang P, Clizbe LA, Song Y, Bauer SM, Huang W, Woolfrey J, Sinha U, Arfsten AE, Hutchaleelaha A, Hollenbach SJ, Lambing JL, Scarborough RM, Zhu BY. 2004 N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors. Bioorganic and Medicinal Chemistry Letters. 14(9):2073-8.
Mehrotra MM, Heath JA, Smyth MS, Pandey A, Rose JW, Seroogy JM, Volkots DL, Nannizzi-Alaimo L, Park GL, Lambing JL, Hollenbach SJ, Scarborough RM. 2004 Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists. Journal of Medicinal Chemistry. 47(8):2037-61.
Cherry M, Williams DH. 2004 Recent kinase and kinase inhibitor X-ray structures: mechanisms of inhibition and selectivity insights. Current Opinions in Medicinal Chemistry. 11(6):663-73.
Vos TJ, Caracoti A, Che JL, Dai M, Farrer CA, Forsyth NE, Drabic SV, Horlick RA, Lamppu D, Yowe DL, Balani S, Li P, Zeng H, Joseph IB, Rodriguez LE, Maguire MP, Patane MA, Claiborne CF. 2004 Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. Journal of Medicinal Chemistry. 47(7):1602-4.
Zhang P, Bao L, Zuckett JF, Jia ZJ, Woolfrey J, Arfsten A, Edwards S, Sinha U, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. 2004 Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. Bioorganic and Medicinal Chemistry Letters. 14(4):989-93.
Gu W, Geddes BJ, Zhang C, Foley KP, Stricker-Krongrad A. 2004 The prolactin-releasing peptide receptor (GPR10) regulates body weight homeostasis in mice. Journal of Molecular Neuroscience. 22(1-2):93-103.
Liao H, Wu J, Kuhn E, Chin W, Chang B, Jones MD, O'neil S, Clauser KR, Karl J, Hasler F, Roubenoff R, Zolg W, Guild BC. 2004 Use of mass spectrometry to identify protein biomarkers of disease severity in the synovial fluid and serum of patients with rheumatoid arthritis. Arthritis and Rheumatism 50(12):3792-803.
Teupser D, Pavlides S, Tan M, Gutierrez-Ramos JC, Kolbeck R, Breslow JL. 2004 Major reduction of atherosclerosis in fractalkine (CX3CL1)-deficient mice is at the brachiocephalic artery, not the aortic root. Proceedings of the National Academy of Sciences. Dec 13; [Epub ahead of print]
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