Search Results - "PETROS, Andrew M"

Structural biology of the Bcl-2 family of proteins by Petros, Andrew M., Olejniczak, Edward T., Fesik, Stephen W.

“…The proteins of the Bcl-2 family are important regulators of programmed cell death. Structural studies of Bcl-2 family members have provided many important…”
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Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein by Petros, Andrew M., Swann, Steven L., Song, Danying, Swinger, Kerren, Park, Chang, Zhang, Haichao, Wendt, Michael D., Kunzer, Aaron R., Souers, Andrew J., Sun, Chaohong

“…Apoptosis is regulated by the BCL-2 family of proteins, which is comprised of both pro-death and pro-survival members. Evasion of apoptosis is a hallmark of…”
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Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a by Sweis, Ramzi F, Pliushchev, Marina, Brown, Peter J, Guo, Jun, Li, Fengling, Maag, David, Petros, Andrew M, Soni, Nirupama B, Tse, Chris, Vedadi, Masoud, Michaelides, Michael R, Chiang, Gary G, Pappano, William N

“…G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity…”
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Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site by Goedken, Eric R., Argiriadi, Maria A., Dietrich, Justin D., Petros, Andrew M., Krishnan, Navasona, Panchal, Sanjay C., Qiu, Wei, Wu, Haihong, Zhu, Haizhong, Adams, Ashley M., Bodelle, Pierre M., Goguen, Lucas, Richardson, Paul L., Slivka, Peter F., Srikumaran, Myron, Upadhyay, Anup K., Wu, Bainan, Judge, Russell A., Vasudevan, Anil, Gopalakrishnan, Sujatha M., Cox, Philip B., Stoll, Vincent S., Sun, Chaohong

“…Anti-IL17A therapies have proven effective for numerous inflammatory diseases including psoriasis, axial spondylitis and psoriatic arthritis. Modulating and/or…”
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Structure of the N-Terminal RNA-Binding Domain of the SARS CoV Nucleocapsid Protein by Huang, Qiulong, Yu, Liping, Petros, Andrew M, Gunasekera, Angelo, Liu, Zhihong, Xu, Nan, Hajduk, Philip, Mack, Jamey, Fesik, Stephen W, Olejniczak, Edward T

“…The severe acute respiratory syndrome (SARS) virus belongs to the Coronaviridea family of viruses. Its virion encodes several proteins including a replicase…”
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Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR by Petros, Andrew M., Huth, Jeffrey R., Oost, Thorsten, Park, Cheol-Min, Ding, Hong, Wang, Xilu, Zhang, Haichao, Nimmer, Paul, Mendoza, Renaldo, Sun, Chaohong, Mack, Jamey, Walter, Karl, Dorwin, Sarah, Gramling, Emily, Ladror, Uri, Rosenberg, Saul H., Elmore, Steven W., Fesik, Stephen W., Hajduk, Philip J.

“…The Bcl-2 family of proteins plays a major role in the regulation of apoptosis, or programmed cell death. Overexpression of the anti-apoptotic members of this…”
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Solution Structure of the Antiapoptotic Protein bcl-2 by Petros, Andrew M., Medek, Ales, Nettesheim, David G., Kim, Daniel H., Yoon, Ho Sup, Swift, Kerry, Matayoshi, Edmund D., Oltersdorf, Tilman, Fesik, Stephen W.

“…The structures of two isoforms of Bcl-2 that differ by two amino acids have been determined by NMR spectroscopy. Because wild-type Bcl-2 behaved poorly in…”
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Defining the p53 DNA‐binding domain/Bcl‐xL‐binding interface using NMR by Petros, Andrew M, Gunasekera, Angelo, Xu, Nan, Olejniczak, Edward T, Fesik, Stephen W

“…p53 exerts its tumor suppressor activity through both transcription‐dependent and transcription‐independent processes. Although the transcription‐dependent…”
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Solution Structure of a Bcl-2 Homolog from Kaposi Sarcoma Virus by Huang, Qiulong, Petros, Andrew M., Virgin, Herbert W., Fesik, Stephen W., Olejniczak, Edward T.

“…Kaposi sarcoma-associated herpes virus (KSHV) contains a gene that has functional and sequence homology to the apoptotic Bcl-2 family of proteins [Sarid, R.,…”
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A surface groove essential for viral Bcl-2 function during chronic infection in vivo by Loh, Joy, Huang, Qiulong, Petros, Andrew M, Nettesheim, David, van Dyk, Linda F, Labrada, Lucia, Speck, Samuel H, Levine, Beth, Olejniczak, Edward T, Virgin, 4th, Herbert W

“…Antiapoptotic Bcl-2 family proteins inhibit apoptosis in cultured cells by binding BH3 domains of proapoptotic Bcl-2 family members via a hydrophobic BH3…”
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Insights into the Conformation and Self-Association of a Concentrated Monoclonal Antibody using Isothermal Chemical Denaturation and Nuclear Magnetic Resonance by Xu, Jianwen, Namanja, Andrew, Chan, Siew Leong, Son, Chelsea, Petros, Andrew M, Sun, Chaohong, Radziejewski, Czeslaw, Ihnat, Peter M

“…The purpose of this investigation was to highlight the utility of nuclear magnetic resonance (NMR) as a multi-attribute method for the characterization of…”
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Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity by Bruncko, Milan, Wang, Le, Sheppard, George S, Phillips, Darren C, Tahir, Stephen K, Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J, Jin, Sha, Judge, Russell A, Kovar, Peter J, Madar, David, Nimmer, Paul, Park, Chang, Petros, Andrew M, Rosenberg, Saul H, Smith, Morey L, Song, Xiaohong, Sun, Chaohong, Tao, Zhi-Fu, Wang, Xilu, Xiao, Yu, Zhang, Haichao, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J

“…Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the progression and survival of multiple tumor types. Herein we report a…”
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Efficiently driving protein-based fragment screening and lead discovery using two-dimensional NMR by Peng, Chen, Namanja, Andrew T., Munoz, Eva, Wu, Haihong, Frederick, Thomas E., Maestre-Martinez, Mitcheell, Iglesias Fernandez, Isaac, Sun, Qi, Cobas, Carlos, Sun, Chaohong, Petros, Andrew M.

“…Fragment-based drug discovery (FBDD) and validation of small molecule binders using NMR spectroscopy is an established and widely used method in the early…”
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Discovery of novel inhibitors of Bcl-xL using multiple high-throughput screening platforms by Qian, Jie, Voorbach, Martin J, Huth, Jeffrey R, Coen, Michael L, Zhang, Haichao, Ng, Shi-Chung, Comess, Kenneth M, Petros, Andrew M, Rosenberg, Saul H, Warrior, Usha, Burns, David J

“…Bcl-xL is a member of the Bcl-2 family of proteins that are implicated to play a vital role in several diseases including cancer. Bcl-xL suppresses apoptosis;…”
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NMR-based fragment screening and lead discovery accelerated by principal component analysis by Namanja, Andrew T., Xu, Jia, Wu, Haihong, Sun, Qi, Upadhyay, Anup K., Sun, Chaohong, Van Doren, Steven R., Petros, Andrew M.

“…Protein-based NMR spectroscopy has proven to be a very robust method for finding fragment leads to protein targets. However, one limitation of protein-based…”
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Structure and ligand recognition of the phosphotyrosine binding domain of Shc by Zhou, Ming-Ming, Ravichandran, Kodimangalam S, Olejniczak, Edward T, Petros, Andrew M, Meadows, Robert P, Sattler, Michael, Harlan, John E, Wade, Warren S, Burakoff, Steven J, Fesik, Stephen W

“…The nuclear magnetic resonance structure of the phosphotyrosine binding (PTB) domain of Shc complexed to a phosphopeptide reveals an alternative means of…”
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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors by Wang, Le, Pratt, John K, Soltwedel, Todd, Sheppard, George S, Fidanze, Steven D, Liu, Dachun, Hasvold, Lisa A, Mantei, Robert A, Holms, James H, McClellan, William J, Wendt, Michael D, Wada, Carol, Frey, Robin, Hansen, T. Matthew, Hubbard, Robert, Park, Chang H, Li, Leiming, Magoc, Terrance J, Albert, Daniel H, Lin, Xiaoyu, Warder, Scott E, Kovar, Peter, Huang, Xiaoli, Wilcox, Denise, Wang, Rongqi, Rajaraman, Ganesh, Petros, Andrew M, Hutchins, Charles W, Panchal, Sanjay C, Sun, Chaohong, Elmore, Steven W, Shen, Yu, Kati, Warren M, McDaniel, Keith F

“…Members of the BET family of bromodomain containing proteins have been identified as potential targets for blocking proliferation in a variety of cancer cell…”
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Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity by Tao, Zhi-Fu, Hasvold, Lisa, Wang, Le, Wang, Xilu, Petros, Andrew M, Park, Chang H, Boghaert, Erwin R, Catron, Nathaniel D, Chen, Jun, Colman, Peter M, Czabotar, Peter E, Deshayes, Kurt, Fairbrother, Wayne J, Flygare, John A, Hymowitz, Sarah G, Jin, Sha, Judge, Russell A, Koehler, Michael F. T, Kovar, Peter J, Lessene, Guillaume, Mitten, Michael J, Ndubaku, Chudi O, Nimmer, Paul, Purkey, Hans E, Oleksijew, Anatol, Phillips, Darren C, Sleebs, Brad E, Smith, Brian J, Smith, Morey L, Tahir, Stephen K, Watson, Keith G, Xiao, Yu, Xue, John, Zhang, Haichao, Zobel, Kerry, Rosenberg, Saul H, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J

“…A-1155463, a highly potent and selective BCL-XL inhibitor, was discovered through nuclear magnetic resonance (NMR) fragment screening and structure-based…”
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Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design by Dietrich, Justin D, Longenecker, Kenton L, Wilson, Noel S, Goess, Christian, Panchal, Sanjay C, Swann, Steven L, Petros, Andrew M, Hobson, Adrian D, Ihle, David, Song, Danying, Richardson, Paul, Comess, Kenneth M, Cox, Philip B, Dombrowski, Amanda, Sarris, Kathy, Donnelly-Roberts, Diana L, Duignan, David B, Gomtsyan, Arthur, Jung, Paul, Krueger, A Chris, Mathieu, Suzanne, McClure, Andrea, Stoll, Vincent S, Wetter, Jill, Mankovich, John A, Hajduk, Philip J, Vasudevan, Anil, Stoffel, Robert H, Sun, Chaohong

“…Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and…”
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Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer by Petros, Andrew M, Korepanova, Alla, Jakob, Clarissa G, Qiu, Wei, Panchal, Sanjay C, Wang, Jie, Dietrich, Justin D, Brewer, Jason T, Pohlki, Frauke, Kling, Andreas, Wilcox, Kyle, Lakics, Viktor, Bahnassawy, Lamiaa, Reinhardt, Peter, Partha, Sarathy Karunan, Bodelle, Pierre M, Lake, Marc, Charych, Erik I, Stoll, Vincent S, Sun, Chaohong, Mohler, Eric G

“…Apolipoprotein E is a 299-residue lipid carrier protein produced in both the liver and the brain. The protein has three major isoforms denoted apoE2, apoE3,…”
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