Search Results - "WILCOXEN, Keith M"

In vivo anti-tumor activity of the PARP inhibitor niraparib in homologous recombination deficient and proficient ovarian carcinoma by AlHilli, Mariam M, Becker, Marc A, Weroha, S. John, Flatten, Karen S, Hurley, Rachel M, Harrell, Maria I, Oberg, Ann L, Maurer, Matt J, Hawthorne, Kieran M, Hou, Xiaonan, Harrington, Sean C, McKinstry, Sarah, Meng, X. Wei, Wilcoxen, Keith M, Kalli, Kimberly R, Swisher, Elizabeth M, Kaufmann, Scott H, Haluska, Paul

“…Abstract Objective Poly(ADP-ribose) polymerase (PARP) inhibitors have yielded encouraging responses in high-grade serous ovarian carcinomas (HGSOCs), but the…”
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Antibacterial agents based on the cyclic d,l -α-peptide architecture by Ghadiri, M. Reza, Fernandez-Lopez, Sara, Kim, Hui-Sun, Choi, Ellen C, Delgado, Mercedes, Granja, Juan R, Khasanov, Alisher, Kraehenbuehl, Karin, Long, Georgina, Weinberger, Dana A, Wilcoxen, Keith M

“…The rapid emergence of bacterial infections that are resistant to many drugs underscores the need for new therapeutic agents. Here we report that six- and…”
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Antiviral cyclic d, l-α-peptides: Targeting a general biochemical pathway in virus infections by Horne, W. Seth, Wiethoff, Christopher M., Cui, Chunli, Wilcoxen, Keith M., Amorin, Manuel, Ghadiri, M. Reza, Nemerow, Glen R.

“…Using adenovirus as a model non-enveloped virus, we have determined that eight-residue cyclic d, l-α-peptides can specifically prevent the development of low…”
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Recent advances of MEK inhibitors and their clinical progress by Wang, John Yuan, Wilcoxen, Keith M, Nomoto, Kenichi, Wu, Sara

“…The RAS/RAF/MEK/ERK signaling pathway has been a major clinical focus in oncology research in recent years. A clearer association of B-RAF mutations to cancers…”
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Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylamino-pyrazolo[1,5-a] pyrimidine (NBI 30775/r121919) and structure-activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists by CHEN CHEN, WILCOXEN, Keith M, BOZIGIAN, Haig, GRIGORIADIS, Dimitri E, HUANG, Charles Q, XIE, Yun-Feng, MCCARTHY, James R, WEBB, Thomas R, ZHU, Yun-Fei, SAUNDERS, John, LIU, Xin-Jun, CHEN, Ta-Kung

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Biomimetic Catalysis of Intermodular Aminoacyl Transfer by Wilcoxen, Keith M, Leman, Luke J, Weinberger, Dana A, Huang, Zheng-Zheng, Ghadiri, M. Reza

“…Intermodular aminoacyl transfer is the fundamental bond-forming reaction in the biosynthesis of polypeptides by ribosomes and nonribosomal peptide synthetases…”
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Functional and Mechanistic Analyses of Biomimetic Aminoacyl Transfer Reactions in de Novo Designed Coiled Coil Peptides via Rational Active Site Engineering by Leman, Luke J, Weinberger, Dana A, Huang, Zheng-Zheng, Wilcoxen, Keith M, Ghadiri, M. Reza

“…Ribosomes and nonribosomal peptide synthetases (NRPSs) carry out instructed peptide synthesis through a series of directed intermodular aminoacyl transfer…”
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Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility by CHEN CHEN, WILCOXEN, Keith M, HUANG, Charles Q, MCCARTHY, James R, CHEN, Takung, GRIGORIADIS, Dimitri E

“…In our efforts to identify potent CRF(1) antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar…”
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Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists by HUANG, Charles Q, WILCOXEN, Keith M, GRIGORIADIS, Dimitri E, MCCARTHY, James R, CHEN CHEN

“…A series of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines was designed and synthesized as antagonists for the corticotrophin-releasing factor-1 (CRF(1)) receptor…”
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Synthesis and initial structure–Activity relationships of a novel series of imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists by Wilcoxen, Keith M., Zhu, Yun-Fei, Connors, Patrick J., Saunders, John, Gross, Timothy D., Gao, Yinghong, Reinhart, Greg J., Struthers, R.Scott, Chen, Chen

“…SAR studies of 2-arylimidazolo[1,2- a]pyrimid-5-ones 10a– m, which were derived from initial lead 3a, resulted in the discovery of a series of potent…”
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Automated Mass Spectrometric Sequence Determination of Cyclic Peptide Library Members by Redman, James E, Wilcoxen, Keith M, Ghadiri, M. Reza

“…Cyclic peptides have come under scrutiny as potential antimicrobial therapeutic agents. Combinatorial split-and-pool synthesis of cyclic peptides can afford…”
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Design, synthesis and structure–Activity relationships of novel imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists by Gross, Timothy D., Zhu, Yun-Fei, Saunders, John, Wilcoxen, Keith M., Gao, Yinghong, Connors, Patrick J., Guo, Zhiqiang, Struthers, R.Scott, Reinhart, Greg J., Chen, Chen

“…SAR studies of lead GnRH receptor antagonists 2a and 2b reported earlier resulted in the discovery of compound 10b which showed much higher potency ( K i=4.6…”
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Four-Atom-Linked Capped Porphyrins:  Synthesis and Characterization by Johnson, Martin R, Seok, Won K, Ma, Wuping, Slebodnick, Carla, Wilcoxen, Keith M, Ibers, James A

“…Three new capped porphyrins, H2(OC2OPor) (7), H2(OC(CO)NPor) (13), and H2(OC2NPor) (14), to be used as heme model compounds, have been synthesized and…”
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Design of 2,5-Dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and Structure−Activity Relationships of a Series of Potent and Orally Active Corticotropin-Releasing Factor Receptor Antagonists by Chen, Chen, Wilcoxen, Keith M, Huang, Charles Q, Xie, Yun-Feng, McCarthy, James R, Webb, Thomas R, Zhu, Yun-Fei, Saunders, John, Liu, Xin-Jun, Chen, Ta-Kung, Bozigian, Haig, Grigoriadis, Dimitri E

“…We have previously shown that 3-phenylpyrazolo[1,5-a]pyrimidines exemplified by 8 were potent antagonists of the human corticotropin-releasing factor-1…”
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Abstract A258: The PARP inhibitor niraparib demonstrates synergy with chemotherapy in treatment of patient derived Ewing's sarcoma tumorGraft models by Wilcoxen, Keith M., Brooks, David G., Tiruchinapalli, Dhanrajan, Anderson, Nathan, Donaldson, Rodney, Nivens, McIver, Cook, Charlie, Khor, Tin, Lu, Bin, De Oliveira, Elizabeth, Hawley, Erin, Bruckheimer, Elizabeth

“…Abstract Ewing's sarcoma (ES) is the second most common primary tumor of bone in young adults and accounts for 40% of bone tumors in children and adolescents…”
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Abstract 1795: Characterization of a novel series of potent, selective inhibitors of wild type and mutant/fusion anaplastic lymphoma kinase by Wilcoxen, Keith M., Brake, Rachael L., Saffran, Doug, Teffera, Yohannes, Choquette, Deborah, Whittington, Doug, Yu, Violeta, Romero, Karina, Bode, Christiane, Stellwagen, John, Potashman, Michelle, Emkey, Renee, Andrews, Paul, Drew, Allison E., Xu, Man, Szilvassy, Stephen, Al-Assad, Samer, Lewis, Richard T.

“…Abstract Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that has been implicated as a driving oncogene in a number of cancers, including non-small cell…”
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A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease by Douglas, Lisa E J, Reihill, James A, Ho, Melisa W Y, Axten, Jeffrey M, Campobasso, Nino, Schneck, Jessica L, Rendina, Alan R, Wilcoxen, Keith M, Martin, S Lorraine

“…In cystic fibrosis (CF), excessive furin activity plays a critical role in the activation of the epithelial sodium channel (ENaC), dysregulation of which…”
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Antiviral cyclic D,L-α-peptides : Targeting a general biochemical pathway in virus infections: Chemistry & Biology of Natural Products, Tetrahedron Prize for Creativity in Organic Chemistry 2004 K. Nakanishi by HOME, W. Seth, WIETHOFF, Christopher M, CHUNLI CUI, WILCOXEN, Keith M, AMORIN, Manuel, GHADIRI, M. Reza, NEMEROW, Glen R

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Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5- a]pyrimidines as potent CRF 1 receptor antagonists by Huang, Charles Q, Wilcoxen, Keith M, Grigoriadis, Dimitri E, McCarthy, James R, Chen, Chen

“…Graphic A series of 3-(2-pyridyl)pyrazolo[1,5- a]pyrimidines was designed and synthesized as antagonists for the corticotrophin-releasing factor-1 (CRF 1)…”
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correction: Antibacterial agents based on the cyclic d,l-[alpha]-peptide architecture by Fernandez-Lopez, Sara, Hui-Sun, Kim, Choi, Ellen C, Delgado, Mercedes, Granja, Juan R, Khasanov, Alisher, Kraehenbuehl, Karin, Long, Georgina, Weinberger, Dana A, Wilcoxen, Keith M, Ghadiri, M Reza

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