Search Results - "Cee, J"

A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation by Wurz, Ryan P, Dellamaggiore, Ken, Dou, Hannah, Javier, Noelle, Lo, Mei-Chu, McCarter, John D, Mohl, Dane, Sastri, Christine, Lipford, J. Russell, Cee, Victor J

“…Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target protein binder and an ubiquitin ligase binder connected by a linker. By…”
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Systematic Study of the Glutathione Reactivity of N‑Phenylacrylamides: 2. Effects of Acrylamide Substitution by Birkholz, Adam, Kopecky, David J, Volak, Laurie P, Bartberger, Michael D, Chen, Yuping, Tegley, Christopher M, Arvedson, Tara, McCarter, John D, Fotsch, Christopher, Cee, Victor J

“…A comprehensive understanding of structure–reactivity relationships is critical to the design and optimization of cysteine-targeted covalent inhibitors…”
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Cortistatin A is a High-Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11 by Cee, Victor J., Chen, David Y.-K., Lee, Matthew R., Nicolaou, K. C.

“…Antiproliferative alkaloid: Cortistatin A is a high‐affinity ligand for a small set of protein kinases including Rho‐associated, coiled‐coil‐containing protein…”
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ID 397 – EMG and clinical outcome of Leechavenvong’s transfer, preliminary results by Brusakova, S, Humhej, I, Cee, J, Sames, M

“…Purpose The aim of the study is to analyse the results of Leechavenvong’s transfer – long head triceps branch of radial nerve to axillary nerve neurotization…”
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Application of Complex Aldol Reactions to the Total Synthesis of Phorboxazole B by Evans, David A, Fitch, Duke M, Smith, Thomas E, Cee, Victor J

“…The synthesis of phorboxazole B has been accomplished in 27 linear steps and an overall yield of 12.6%. The absolute stereochemistry of the C4−C12, C33−C38,…”
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Resurrecting the Cornforth Model for Carbonyl Addition: Studies on the Origin of 1,2-Asymmetric Induction in Enolate Additions to Heteroatom-Substituted Aldehydes by Evans, David A., Siska, Sarah J., Cee, Victor J.

“…Further experimental support for the Cornforth model is obtained from a systematic study of aldol reactions between methyl‐substituted E and Z enolates and…”
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Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones by Nguyen, Hanh Nho, Cee, Victor J, Deak, Holly L, Du, Bingfan, Faber, Kathleen Panter, Gunaydin, Hakan, Hodous, Brian L, Hollis, Steven L, Krolikowski, Paul H, Olivieri, Philip R, Patel, Vinod F, Romero, Karina, Schenkel, Laurie B, Geuns-Meyer, Stephanie D

“…Herein we describe a general three-step synthesis of 4-substituted chlorophthalazines in good overall yields. In the key step, N,N-dimethylaminophthalimide…”
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Targeted Degradation of MDM2 as a New Approach to Improve the Efficacy of MDM2-p53 Inhibitors by Wurz, Ryan P, Cee, Victor J

“…MDM2 is a key oncogenic protein that serves as a negative regulator of the tumor suppressor p53. While a number of inhibitors of the MDM2-p53 interaction have…”
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The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity by Canon, Jude, Rex, Karen, Saiki, Anne Y., Mohr, Christopher, Cooke, Keegan, Bagal, Dhanashri, Gaida, Kevin, Holt, Tyler, Knutson, Charles G., Koppada, Neelima, Lanman, Brian A., Werner, Jonathan, Rapaport, Aaron S., San Miguel, Tisha, Ortiz, Roberto, Osgood, Tao, Sun, Ji-Rong, Zhu, Xiaochun, McCarter, John D., Volak, Laurie P., Houk, Brett E., Fakih, Marwan G., O’Neil, Bert H., Price, Timothy J., Falchook, Gerald S., Desai, Jayesh, Kuo, James, Govindan, Ramaswamy, Hong, David S., Ouyang, Wenjun, Henary, Haby, Arvedson, Tara, Cee, Victor J., Lipford, J. Russell

“…KRAS is the most frequently mutated oncogene in cancer and encodes a key signalling protein in tumours 1 , 2 . The KRAS(G12C) mutant has a cysteine residue…”
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Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor by Hodous, Brian L, Geuns-Meyer, Stephanie D, Hughes, Paul E, Albrecht, Brian K, Bellon, Steve, Bready, James, Caenepeel, Sean, Cee, Victor J, Chaffee, Stuart C, Coxon, Angela, Emery, Maurice, Fretland, Jenne, Gallant, Paul, Gu, Yan, Hoffman, Doug, Johnson, Rebecca E, Kendall, Richard, Kim, Joseph L, Long, Alexander M, Morrison, Michael, Olivieri, Philip R, Patel, Vinod F, Polverino, Anthony, Rose, Paul, Tempest, Paul, Wang, Ling, Whittington, Douglas A, Zhao, Huilin

“…Inhibition of angiogenesis is a promising and clinically validated approach for limiting tumor growth and survival. The receptor tyrosine kinase Tie-2 is…”
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Theoretical Investigation of Enolborane Addition to α-Heteroatom-Substituted Aldehydes. Relevance of the Cornforth and Polar Felkin−Anh Models for Asymmetric Induction by Cee, Victor J, Cramer, Christopher J, Evans, David A

“…The addition of enolborane nucleophiles to chiral α-heteroatom-substituted aldehydes (CH3CH(X)CHO, X = F, Cl, OMe, SMe, NMe2, and PMe2) was investigated using…”
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Quinolinone-based agonists of S1P1: Use of a N-scan SAR strategy to optimize in vitro and in vivo activity by Pennington, Lewis D., Croghan, Michael D., Sham, Kelvin K.C., Pickrell, Alexander J., Harrington, Paul E., Frohn, Michael J., Lanman, Brian A., Reed, Anthony B., Lee, Matthew R., Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G., Arnett, Heather A., Fotsch, Christopher, Tasker, Andrew S., Wong, Min, Cee, Victor J.

“…We reveal how a N-scan SAR strategy (systematic substitution of each CH group with a N atom) was employed for quinolinone-based S1P1 agonist 5 to modulate…”
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Systematic Study of the Glutathione (GSH) Reactivity of N‑Arylacrylamides: 1. Effects of Aryl Substitution by Cee, Victor J, Volak, Laurie P, Chen, Yuping, Bartberger, Michael D, Tegley, Chris, Arvedson, Tara, McCarter, John, Tasker, Andrew S, Fotsch, Christopher

“…Success in the design of targeted covalent inhibitors depends in part on a knowledge of the factors influencing electrophile reactivity. In an effort to…”
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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors by Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L. Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J. Russell, Cee, Victor J

“…KRASG12C has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to…”
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Structural Elucidation and Absolute Stereochemistry for Pharma Compounds Using MicroED by de Moraes, Lygia Silva, Burch, Jessica E., Delgadillo, David A., Rodriguez, Isabel Hernandez, Mai, Huanghao, Smith, Austin G., Caille, Seb, Walker, Shawn D., Wurz, Ryan P., Cee, Victor J., Rodriguez, Jose A., Gostovic, Dan, Quasdorf, Kyle, Nelson, Hosea M.

“…Microcrystal electron diffraction (microED) is an emerging technique for rapid crystallographic analysis of small molecule micro- and nanocrystals. In this…”
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Structure-Based Design of a Novel Series of Potent, Selective Inhibitors of the Class I Phosphatidylinositol 3-Kinases by Smith, Adrian L, D’Angelo, Noel D, Bo, Yunxin Y, Booker, Shon K, Cee, Victor J, Herberich, Brad, Hong, Fang-Tsao, Jackson, Claire L. M, Lanman, Brian A, Liu, Longbin, Nishimura, Nobuko, Pettus, Liping H, Reed, Anthony B, Tadesse, Seifu, Tamayo, Nuria A, Wurz, Ryan P, Yang, Kevin, Andrews, Kristin L, Whittington, Douglas A, McCarter, John D, Miguel, Tisha San, Zalameda, Leeanne, Jiang, Jian, Subramanian, Raju, Mullady, Erin L, Caenepeel, Sean, Freeman, Daniel J, Wang, Ling, Zhang, Nancy, Wu, Tian, Hughes, Paul E, Norman, Mark H

“…A highly selective series of inhibitors of the class I phosphatidylinositol 3-kinases (PI3Ks) has been designed and synthesized. Starting from the dual…”
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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors by Hodous, Brian L., Geuns-Meyer, Stephanie D., Hughes, Paul E., Albrecht, Brian K., Bellon, Steve, Caenepeel, Sean, Cee, Victor J., Chaffee, Stuart C., Emery, Maurice, Fretland, Jenne, Gallant, Paul, Gu, Yan, Johnson, Rebecca E., Kim, Joseph L., Long, Alexander M., Morrison, Michael, Olivieri, Philip R., Patel, Vinod F., Polverino, Anthony, Rose, Paul, Wang, Ling, Zhao, Huilin

“…A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or…”
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Imidazolone as an Amide Bioisostere in the Development of β‑1,3‑N‑Acetylglucosaminyltransferase 2 (B3GNT2) Inhibitors by Jackson, Jeffrey J., Siegmund, Aaron C., Bai, Wen-Ju, Reed, Anthony B., Birkholz, Adam B., Campuzano, Iain D. G., Créquer-Grandhomme, Amandine, Hu, Ruozhen, Modak, Rucha V., Sudom, Athena, Javier, Noelle, Sanders, Christiana, Lo, Mei-Chu, Xie, Fang, Cee, Victor J., Manzanillo, Paolo, Allen, John G.

“…B3GNT2 is responsible for elongation of cell surface long-chain polylactosamine, which influences the regulation of the immune response, making it an…”
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Selective Lithiation of 2-Methyloxazoles. Applications to Pivotal Bond Constructions in the Phorboxazole Nucleus by Evans, David A, Cee, Victor J, Smith, Thomas E, Santiago, Keith J

“…The lithiation of 2-methyloxazoles with alkyllithium and hindered lithium amide bases generally results in the competitive formation of a mixture of 5-lithio-…”
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Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines by PAYTON, Marc, BUSH, Tammy L, NHO NGUYEN, Hanh, OLIVIERI, Philip R, ROMERO, Karina, SCHENKEL, Laurie B, BAK, Annette, STANTON, Mary, DUSSAULT, Isabelle, PATEL, Vinod F, GEUNS-MEYER, Stephanie, RADINSKY, Robert, CHUNG, Grace, KENDALL, Richard L, ZIEGLER, Beth, EDEN, Patrick, MCELROY, Patricia, ROSS, Sandra, CEE, Victor J, DEAK, Holly L, HODOUS, Brian L

“…In mammalian cells, the aurora kinases (aurora-A, -B, and -C) play essential roles in regulating cell division. The expression of aurora-A and -B is elevated…”
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