Search Results - "Partridge, Anthony W."

Structural Basis of Integrin Activation by Talin by Wegener, Kate L., Partridge, Anthony W., Han, Jaewon, Pickford, Andrew R., Liddington, Robert C., Ginsberg, Mark H., Campbell, Iain D.

“…Regulation of integrin affinity (activation) is essential for metazoan development and for many pathological processes. Binding of the talin…”
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Stereoisomerism of stapled peptide inhibitors of the p53-Mdm2 interaction: an assessment of synthetic strategies and activity profiles by Yuen, Tsz Ying, Brown, Christopher J, Xue, Yuezhen, Tan, Yaw Sing, Ferrer Gago, Fernando J, Lee, Xue Er, Neo, Jin Yong, Thean, Dawn, Kaan, Hung Yi Kristal, Partridge, Anthony W, Verma, Chandra S, Lane, David P, Johannes, Charles W

“…All-hydrocarbon, i , i+7 stapled peptide inhibitors of the p53-Mdm2 interaction have emerged as promising new leads for cancer therapy. Typical chemical…”
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Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists by 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.

“…Although stapled α-helical peptides can address challenging targets, their advancement is impeded by poor understandings for making them cell permeable while…”
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Exquisitely Specific anti-KRAS Biodegraders Inform on the Cellular Prevalence of Nucleotide-Loaded States by Lim, Shuhui, Khoo, Regina, Juang, Yu-Chi, Gopal, Pooja, Zhang, Huibin, Yeo, Constance, Peh, Khong Ming, Teo, Jinkai, Ng, Simon, Henry, Brian, Partridge, Anthony W

“…Mutations to RAS proteins (H-, N-, and K-RAS) are among the most common oncogenic drivers, and tumors harboring these lesions are some of the most difficult to…”
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Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties by 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

“…Stapled α-helical peptides represent an emerging superclass of macrocyclic molecules with drug-like properties, including high-affinity target binding,…”
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STUB1 is an intracellular checkpoint for interferon gamma sensing by Ng, Simon, Lim, Shuhui, Sim, Adrian Chong Nyi, Mangadu, Ruban, Lau, Ally, Zhang, Chunsheng, Martinez, Sarah Bollinger, Chandramohan, Arun, Lim, U-Ming, Ho, Samantha Shu Wen, Chang, Shih Chieh, Gopal, Pooja, Hong, Lewis Z., Schwaid, Adam, Fernandis, Aaron Zefrin, Loboda, Andrey, Li, Cai, Phan, Uyen, Henry, Brian, Partridge, Anthony W.

“…Immune checkpoint blockade (ICB) leads to durable and complete tumour regression in some patients but in others gives temporary, partial or no response…”
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Stearoyl-CoA desaturase inhibition blocks formation of hepatitis C virus-induced specialized membranes by Lyn, Rodney K., Singaravelu, Ragunath, Kargman, Stacia, O'Hara, Shifawn, Chan, Helen, Oballa, Renata, Huang, Zheng, Jones, Daniel M., Ridsdale, Andrew, Russell, Rodney S., Partridge, Anthony W., Pezacki, John Paul

“…Hepatitis C virus (HCV) replication is dependent on the formation of specialized membrane structures; however, the host factor requirements for the formation…”
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mRNAid, an open-source platform for therapeutic mRNA design and optimization strategies by Vostrosablin, Nikita, Lim, Shuhui, Gopal, Pooja, Brazdilova, Kveta, Parajuli, Sushmita, Wei, Xiaona, Gromek, Anna, Prihoda, David, Spale, Martin, Muzdalo, Anja, Greig, Jamie, Yeo, Constance, Wardyn, Joanna, Mejzlik, Petr, Henry, Brian, Partridge, Anthony W, Bitton, Danny A

“…Abstract Recent COVID-19 vaccines unleashed the potential of mRNA-based therapeutics. A common bottleneck across mRNA-based therapeutic approaches is the rapid…”
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De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits by Ng, Simon, Juang, Yu-Chi, Chandramohan, Arun, Kaan, Hung Yi Kristal, Sadruddin, Ahmad, Yuen, Tsz Ying, Ferrer-Gago, Fernando J, Lee, Xue’Er Cheryl, Liew, Xi, Johannes, Charles W, Brown, Christopher J, Kannan, Srinivasaraghavan, Aronica, Pietro G, Berglund, Nils A, Verma, Chandra S, Liu, Lijuan, Stoeck, Alexander, Sawyer, Tomi K, Partridge, Anthony W, Lane, David P

“…Nonspecific promiscuous compounds can mislead researchers and waste significant resources. This phenomenon, though well-documented for small molecules, has not…”
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MDM2/MDMX inhibition by Sulanemadlin synergizes with anti-Programmed Death 1 immunotherapy in wild-type p53 tumors by Ingelshed, Katrine, Melssen, Marit M., Kannan, Pavitra, Chandramohan, Arun, Partridge, Anthony W., Jiang, Long, Wermeling, Fredrik, Lane, David P., Nestor, Marika, Spiegelberg, Diana

“…Immunotherapy has revolutionized cancer treatment but its efficacy depends on a robust immune response in the tumor. Silencing of the tumor suppressor p53 is…”
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A high-throughput microfluidic mechanoporation platform to enable intracellular delivery of cyclic peptides in cell-based assays by Kasper, Stephen H, Otten, Stephanie, Squadroni, Brian, Orr-Terry, Cionna, Kuang, Yi, Mussallem, Lily, Ge, Lan, Yan, Lin, Kannan, Srinivasaraghavan, Verma, Chandra S, Brown, Christopher J, Johannes, Charles W, Lane, David P, Chandramohan, Arun, Partridge, Anthony W, Roberts, Lee R, Josien, Hubert, Therien, Alex G, Hett, Erik C, Howell, Bonnie J, Peier, Andrea, Ai, Xi, Cassaday, Jason

“…Cyclic peptides are poised to target historically difficult to drug intracellular protein-protein interactions, however, their general cell impermeability…”
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bioPROTACs as versatile modulators of intracellular therapeutic targets including proliferating cell nuclear antigen (PCNA) by Lim, Shuhui, Khoo, Regina, Peh, Khong Ming, Teo, Jinkai, Chang, Shih Chieh, Ng, Simon, Beilhartz, Greg L., Melnyk, Roman A., Johannes, Charles W., Brown, Christopher J., Lane, David P., Henry, Brian, Partridge, Anthony W.

“…Targeted degradation approaches such as proteolysis targeting chimeras (PROTACs) offer new ways to address disease through tackling challenging targets and…”
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Protein Polymerization as a Novel Targeted Protein Degradation Mechanism by Berger, Raphaëlle, Partridge, Anthony W

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The Dual Interactions of p53 with MDM2 and p300: Implications for the Design of MDM2 Inhibitors by Kannan, Srinivasaraghavan, Partridge, Anthony W, Lane, David P, Verma, Chandra S

“…Proteins that limit the activity of the tumour suppressor protein p53 are increasingly being targeted for inhibition in a variety of cancers. In addition to…”
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Molecular Mechanism of P53 Peptide Permeation through Lipid Membranes from Solid-State NMR Spectroscopy and Molecular Dynamics Simulations by Li, Mingyue, Li, Jianguo, Lu, Xingyu, Schroder, Ryan, Chandramohan, Arun, Wuelfing, W. Peter, Templeton, Allen C., Xu, Wei, Gindy, Marian, Kesisoglou, Filippos, Ling, Jing, Sawyer, Tomi, Verma, Chandra S., Partridge, Anthony W., Su, Yongchao

“…Macrocyclic peptides show promise in targeting high-value therapeutically relevant binding sites due to their high affinity and specificity. However, their…”
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Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay by Mortison, Jonathan D, Cornella-Taracido, Ivan, Venkatchalam, Gireedhar, Partridge, Anthony W, Siriwardana, Nirodhini, Bushell, Simon M

“…Determination of target engagement for candidate drug molecules in the native cellular environment is a significant challenge for drug discovery programs. The…”
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Discovery and Structure-Based Design of Macrocyclic Peptides Targeting STUB1 by Ng, Simon, Brueckner, Alexander C., Bahmanjah, Soheila, Deng, Qiaolin, Johnston, Jennifer M., Ge, Lan, Duggal, Ruchia, Habulihaz, Bahanu, Barlock, Benjamin, Ha, Sookhee, Sadruddin, Ahmad, Yeo, Constance, Strickland, Corey, Peier, Andrea, Henry, Brian, Sherer, Edward C., Partridge, Anthony W.

“…Recent evidence suggests that deletion of STUB1a pivotal negative regulator of interferon-γ sensingmay potentially clear malignant cells. However, current…”
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Macrocyclic α helical peptide therapeutic modality: A perspective of learnings and challenges by 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.

“…[Display omitted] Macrocyclic α-helical peptides have emerged as a compelling new therapeutic modality to tackle targets confined to the intracellular…”
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Polar residue tagging of transmembrane peptides by Melnyk, Roman A., Partridge, Anthony W., Yip, Jeannie, Wu, Yanqiu, Goto, Natalie K., Deber, Charles M.

“…Studies that focus on packing interactions between transmembrane (TM) helices in membrane proteins would greatly benefit from the ability to investigate their…”
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Liposome Click Membrane Permeability Assay for Identifying Permeable Peptides by 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

“…Purpose To develop a novel, target agnostic liposome click membrane permeability assay (LCMPA) using liposome encapsulating copper free click reagent dibenzo…”
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