Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy von Chang, Yong S, Graves, Bradford, Guerlavais, Vincent, Tovar, Christian, Packman, Kathryn, To, Kwong-Him, Olson, Karen A, Kesavan, Kamala, Gangurde, Pranoti, Mukherjee, Aditi, Baker, Theresa, Darlak, Krzysztof, Elkin, Carl, Filipovic, Zoran, Qureshi, Farooq Z, Cai, Hongliang, Berry, Pamela, Feyfant, Eric, Shi, Xiangguo E, Horstick, James, Annis, D Allen, Manning, Anthony M, Fotouhi, Nader, Nash, Huw, Vassilev, Lyubomir T, Sawyer, Tomi K

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Probing theα-Helical Structural Stability of Stapled p53 Peptides: Molecular Dynamics Simulations and Analysis von Guo, Zuojun, Mohanty, Udayan, Noehre, Justin, Sawyer, Tomi K, Sherman, Woody, Krilov, Goran

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Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α‑Helical Peptide in Clinical Development von Guerlavais, Vincent, Sawyer, Tomi K., Carvajal, Luis, Chang, Yong S., Graves, Bradford, Ren, Jian-Guo, Sutton, David, Olson, Karen A., Packman, Kathryn, Darlak, Krzysztof, Elkin, Carl, Feyfant, Eric, Kesavan, Kamala, Gangurde, Pranoti, Vassilev, Lyubomir T., Nash, Huw M., Vukovic, Vojislav, Aivado, Manuel, Annis, D. Allen

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Aqueous remote loading of setmelanotide in poly(lactic-co-glycolic acid) microspheres for long-term obesity treatment von Wang, Shuying, Downing, Griffin, Olsen, Karl F, Sawyer, Tomi K, Cone, Roger D, Schwendeman, Steven P

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Targeting anti-cancer agents to bone using bisphosphonates von Xing, Lianping, Ebetino, Frank H., Boeckman, Robert K., Srinivasan, Venkat, Tao, Jianguo, Sawyer, Tomi K., Li, Jinbo, Yao, Zhenqiang, Boyce, Brendan F.

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Photoredox Ni-catalyzed peptide C(sp)-O cross-coupling: from intermolecular reactions to side chain-to-tail macrocyclization von Lee, Hyelee, Boyer, Nicolas C, Deng, Qiaolin, Kim, Hai-Young, Sawyer, Tomi K, Sciammetta, Nunzio

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Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists von Chandramohan, Arun, Josien, Hubert, Yuen, Tsz Ying, Duggal, Ruchia, Spiegelberg, Diana, Yan, Lin, Juang, Yu-Chi Angela, Ge, Lan, Aronica, Pietro G., Kaan, Hung Yi Kristal, Lim, Yee Hwee, Peier, Andrea, Sherborne, Brad, Hochman, Jerome, Lin, Songnian, Biswas, Kaustav, Nestor, Marika, Verma, Chandra S., Lane, David P., Sawyer, Tomi K., Garbaccio, Robert, Henry, Brian, Kannan, Srinivasaraghavan, Brown, Christopher J., Johannes, Charles W., Partridge, Anthony W.

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Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-I... von Huang, Wei-Sheng, Metcalf, Chester A, Sundaramoorthi, Raji, Wang, Yihan, Zou, Dong, Thomas, R. Mathew, Zhu, Xiaotian, Cai, Lisi, Wen, David, Liu, Shuangying, Romero, Jan, Qi, Jiwei, Chen, Ingrid, Banda, Geetha, Lentini, Scott P, Das, Sasmita, Xu, Qihong, Keats, Jeff, Wang, Frank, Wardwell, Scott, Ning, Yaoyu, Snodgrass, Joseph T, Broudy, Marc I, Russian, Karin, Zhou, Tianjun, Commodore, Lois, Narasimhan, Narayana I, Mohemmad, Qurish K, Iuliucci, John, Rivera, Victor M, Dalgarno, David C, Sawyer, Tomi K, Clackson, Tim, Shakespeare, William C

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Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties von Partridge, Anthony W, Kaan, Hung Yi Kristal, Juang, Yu-Chi, Sadruddin, Ahmad, Lim, Shuhui, Brown, Christopher J, Ng, Simon, Thean, Dawn, Ferrer, Fernando, Johannes, Charles, Yuen, Tsz Ying, Kannan, Srinivasaraghavan, Aronica, Pietro, Tan, Yaw Sing, Pradhan, Mohan R, Verma, Chandra S, Hochman, Jerome, Chen, Shiying, Wan, Hui, Ha, Sookhee, Sherborne, Brad, Lane, David P, Sawyer, Tomi K

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Editor's Note: Identification of Src-Specific Phosphorylation Site on Focal Adhesion Kinase: Dissection of the Role of Src SH2 and Catalytic Functions and Their Consequences for Tu... von Brunton, Valerie G., Avizienyte, Egle, Fincham, Valerie J., Serrels, Bryan, Metcalf, Chester A., Sawyer, Tomi K., Frame, Margaret C.

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Subthreshold activation of the melanocortin system causes generalized sensitization to anorectic agents in mice von Dahir, Naima S, Gui, Yijun, Wu, Yanan, Sweeney, Patrick R, Rouault, Alix Aj, Williams, Savannah Y, Gimenez, Luis E, Sawyer, Tomi K, Joy, Stephen T, Mapp, Anna K, Cone, Roger D

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The novel peptide LCGM-10 attenuates metabotropic glutamate receptor 5 activity and demonstrates behavioral effects in animal models von Malyshev, Anton V, Pavshintcev, Vsevolod V, Mitkin, Nikita A, Sukhanova, Iuliia A, Gedzun, Vasilina R, Zlobin, Alexander S, Doronin, Igor I, Babkin, Gennady A, Sawyer, Tomi K

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Macrocyclic α helical peptide therapeutic modality: A perspective of learnings and challenges von Sawyer, Tomi K., Partridge, Anthony W., Kaan, Hung Yi Kristal, Juang, Yu-Chi, Lim, Shuhui, Johannes, Charles, Yuen, Tsz Ying, Verma, Chandra, Kannan, Srinivasaraghavan, Aronica, Pietro, Tan, Yaw Sing, Sherborne, Brad, Ha, Sookhee, Hochman, Jerome, Chen, Shiying, Surdi, Laura, Peier, Andrea, Sauvagnat, Berengere, Dandliker, Peter J., Brown, Christopher J., Ng, Simon, Ferrer, Fernando, Lane, David P.

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NanoClick: A High Throughput, Target-Agnostic Peptide Cell Permeability Assay von Peier, Andrea, Ge, Lan, Boyer, Nicolas, Frost, John, Duggal, Ruchia, Biswas, Kaustav, Edmondson, Scott, Hermes, Jeffrey D, Yan, Lin, Zimprich, Chad, Sadruddin, Ahmad, Kristal Kaan, Hung Yi, Chandramohan, Arun, Brown, Christopher J, Thean, Dawn, Lee, Xue Er, Yuen, Tsz Ying, Ferrer-Gago, Fernando J, Johannes, Charles W, Lane, David P, Sherborne, Brad, Corona, Cesear, Robers, Matthew B, Sawyer, Tomi K, Partridge, Anthony W

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Liposome Click Membrane Permeability Assay for Identifying Permeable Peptides von Desai, Tanvi J., Habulihaz, Bahanu, Cannon, Joe R., Chandramohan, Arun, Kaan, Hung Yi Kristal, Sadruddin, Ahmad, Yuen, Tsz Ying, Johannes, Charles, Thean, Dawn, Brown, Chris J., Lane, David P., Partridge, Anthony W., Evers, Raymond, Sawyer, Tomi K., Hochman, Jerome

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Molecular Simulations Identify Binding Poses and Approximate Affinities of Stapled α‑Helical Peptides to MDM2 and MDMX von Morrone, Joseph A, Perez, Alberto, Deng, Qiaolin, Ha, Sookhee N, Holloway, M. Katharine, Sawyer, Tomi K, Sherborne, Bradley S, Brown, Frank K, Dill, Ken A

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Demonstration of a Common DPhe7 to DNal(2′)7 Peptide Ligand Antagonist Switch for Melanocortin‑3 and Melanocortin‑4 Receptors Identifies the Systematic Mischaracterization of the P... von Gimenez, Luis E, Noblin, Terry A, Williams, Savannah Y, Mullick Bagchi, Satarupa, Ji, Ren-Lei, Tao, Ya-Xiong, Jeppesen, Claus B, Conde-Frieboes, Kilian W, Sawyer, Tomi K, Grieco, Paolo, Cone, Roger D

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Demonstration of a Common DPhe 7 to DNal(2') 7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic Mischaracterization of the... von Gimenez, Luis E, Noblin, Terry A, Williams, Savannah Y, Mullick Bagchi, Satarupa, Ji, Ren-Lei, Tao, Ya-Xiong, Jeppesen, Claus B, Conde-Frieboes, Kilian W, Sawyer, Tomi K, Grieco, Paolo, Cone, Roger D

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Macrocyclization of an all- d linear α-helical peptide imparts cellular permeability von Kannan, Srinivasaraghavan, Aronica, Pietro G. A., Ng, Simon, Gek Lian, Dawn Thean, Frosi, Yuri, Chee, Sharon, Shimin, Jiang, Yuen, Tsz Ying, Sadruddin, Ahmad, Kaan, Hung Yi Kristal, Chandramohan, Arun, Wong, Jin Huei, Tan, Yaw Sing, Chang, Zi Wei, Ferrer-Gago, Fernando J., Arumugam, Prakash, Han, Yi, Chen, Shiying, Rénia, Laurent, Brown, Christopher J., Johannes, Charles W., Henry, Brian, Lane, David P., Sawyer, Tomi K., Verma, Chandra S., Partridge, Anthony W.

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Novel chemistry for undruggable targets von Milletti, Francesca, Sawyer, Tomi K

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