Search Results - "O'BRYAN, John P"

Pharmacological targeting of RAS: Recent success with direct inhibitors by O’Bryan, John P.

“…RAS inhibitors have been developed that target different aspects of RAS function including (1) membrane association; (2) exchange factor binding; (3) effector…”
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Therapeutic targeting of RAS: New hope for drugging the “undruggable” by Khan, Imran, Rhett, J. Matthew, O'Bryan, John P.

“…RAS is the most frequently mutated oncogene in cancer and a critical driver of oncogenesis. Therapeutic targeting of RAS has been a goal of cancer research for…”
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Direct inhibition of RAS: Quest for the Holy Grail? by Spencer-Smith, Russell, O’Bryan, John P.

“…RAS GTPases (H-, K-, and N-RAS) are the most frequently mutated oncoprotein family in human cancer. However, the relatively smooth surface architecture of RAS…”
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Selective and noncovalent targeting of RAS mutants for inhibition and degradation by Teng, Kai Wen, Tsai, Steven T., Hattori, Takamitsu, Fedele, Carmine, Koide, Akiko, Yang, Chao, Hou, Xuben, Zhang, Yingkai, Neel, Benjamin G., O’Bryan, John P., Koide, Shohei

“…Activating mutants of RAS are commonly found in human cancers, but to date selective targeting of RAS in the clinic has been limited to KRAS(G12C) through…”
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The P-type ATPase transporter ATP7A promotes angiogenesis by limiting autophagic degradation of VEGFR2 by Ash, Dipankar, Sudhahar, Varadarajan, Youn, Seock-Won, Okur, Mustafa Nazir, Das, Archita, O’Bryan, John P., McMenamin, Maggie, Hou, Yali, Kaplan, Jack H., Fukai, Tohru, Ushio-Fukai, Masuko

“…VEGFR2 (KDR/Flk1) signaling in endothelial cells (ECs) plays a central role in angiogenesis. The P-type ATPase transporter ATP7A regulates copper homeostasis,…”
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Inhibition of RAS function through targeting an allosteric regulatory site by Spencer-Smith, Russell, Koide, Akiko, Zhou, Yong, Eguchi, Raphael R, Sha, Fern, Gajwani, Priyanka, Santana, Dianicha, Gupta, Ankit, Jacobs, Miranda, Herrero-Garcia, Erika, Cobbert, Jacqueline, Lavoie, Hugo, Smith, Matthew, Rajakulendran, Thanashan, Dowdell, Evan, Okur, Mustafa Nazir, Dementieva, Irina, Sicheri, Frank, Therrien, Marc, Hancock, John F, Ikura, Mitsuhiko, Koide, Shohei, O'Bryan, John P

“…A monobody was identified that binds to an allosteric lobe at the α4-β6-α5 interface to block H- and K-RAS signaling and transformation by disrupting RAS…”
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Inhibition of RAS: proven and potential vulnerabilities by Zuberi, Mariyam, Khan, Imran, O'Bryan, John P

“…RAS is a membrane localized small GTPase frequently mutated in human cancer. As such, RAS has been a focal target for developing cancer therapeutics since its…”
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Intersectin scaffold proteins and their role in cell signaling and endocytosis by Herrero-Garcia, Erika, O'Bryan, John P.

“…Intersectins (ITSNs) are a family of multi-domain proteins involved in regulation of diverse cellular pathways. These scaffold proteins are well known for…”
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Targeting the "undruggable" RAS with biologics by Whaby, Michael, Khan, Imran, O'Bryan, John P

“…RAS proteins represent critical drivers of tumor development and thus are the focus of intense efforts to pharmacologically inhibit these proteins in human…”
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Mutations in the α4-α5 allosteric lobe of RAS do not significantly impair RAS signaling or self-association by Whaby, Michael, Wallon, Lauren, Mazzei, Megan, Khan, Imran, Teng, Kai Wen, Koide, Shohei, O’Bryan, John P.

“…Mutations in one of the three RAS genes (HRAS, KRAS, and NRAS) are present in nearly 20% of all human cancers. These mutations shift RAS to the GTP-loaded…”
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Inhibition of RAS-driven signaling and tumorigenesis with a pan-RAS monobody targeting the Switch I/II pocket by Wallon, Lauren, Khan, Imran, Teng, Kai Wen, Koide, Akiko, Zuberi, Mariyam, Li, Jianping, Ketavarapu, Gayatri, Traaseth, Nathaniel J, O'Bryan, John P, Koide, Shohei

“…RAS mutants are major therapeutic targets in oncology with few efficacious direct inhibitors available. The identification of a shallow pocket near the Switch…”
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Caveolin-1 stabilizes ATP7A, a copper transporter for extracellular SOD, in vascular tissue to maintain endothelial function by Sudhahar, Varadarajan, Okur, Mustafa Nazir, O'Bryan, John P, Minshall, Richard D, Fulton, David, Ushio-Fukai, Masuko, Fukai, Tohru

“…Caveolin-1 (Cav-1) is a scaffolding protein and a major component of caveolae/lipid rafts. Previous reports have shown that endothelial dysfunction in…”
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Biology, pathology, and therapeutic targeting of RAS by Rhett, J Matthew, Khan, Imran, O'Bryan, John P

“…RAS was identified as a human oncogene in the early 1980s and subsequently found to be mutated in nearly 30% of all human cancers. More importantly, RAS plays…”
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Exploring switch II pocket conformation of KRAS(G12D) with mutant-selective monobody inhibitors by Akkapeddi, Padma, Hattori, Takamitsu, Khan, Imran, Glasser, Eliezra, Koide, Akiko, Ketavarapu, Gayatri, Whaby, Michael, Zuberi, Mariyam, Teng, Kai Wen, Lefler, Julia, Maso, Lorenzo, Bang, Injin, Ostrowski, Michael C, O'Bryan, John P, Koide, Shohei

“…The G12D mutation is among the most common KRAS mutations associated with cancer, in particular, pancreatic cancer. Here, we have developed monobodies, small…”
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Identification of the nucleotide-free state as a therapeutic vulnerability for inhibition of selected oncogenic RAS mutants by Khan, Imran, Koide, Akiko, Zuberi, Mariyam, Ketavarapu, Gayatri, Denbaum, Eric, Teng, Kai Wen, Rhett, J. Matthew, Spencer-Smith, Russell, Hobbs, G. Aaron, Camp, Ernest Ramsay, Koide, Shohei, O'Bryan, John P.

“…RAS guanosine triphosphatases (GTPases) are mutated in nearly 20% of human tumors, making them an attractive therapeutic target. Following our discovery that…”
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Neuroblastoma differentiation in vivo excludes cranial tumors by Treffy, Randall W., Rajan, Sriivatsan G., Jiang, Xinghang, Nacke, Lynne M., Malkana, Usama A., Naiche, L.A., Bergey, Dani E., Santana, Dianicha, Rajagopalan, Vinodh, Kitajewski, Jan K., O’Bryan, John P., Saxena, Ankur

“…Neuroblastoma (NB), the most common cancer in the first year of life, presents almost exclusively in the trunk. To understand why an early-onset cancer would…”
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Intersecting pathways in cell biology by O'Bryan, John P

“…The endocytic pathway is involved in activation and inhibition of cellular signaling. Thus, defining the regulatory mechanisms that link endocytosis and…”
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Secreted frizzled related-protein 2 is prognostic for human pancreatic cancer patient survival and is associated with fibrosis by Siegel, Julie B, Nasarre, Patrick, Hsu, Lillian, Mukherjee, Rupak, Gormley, Meghan, Richardson, Bailey, Khan, Imran, Morningstar, Jordan E, Hilliard, Eleanor, O'Bryan, John P, Helke, Kristi L, Spruill, Laura, Dolloff, Nathan G, Klauber-DeMore, Nancy

“…Pancreatic adenocarcinoma (PDAC) is one of the deadliest cancers, with five-year survival rates of 9%. We hypothesized that secreted frizzled-related protein 2…”
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RAS: Past, Present, and Future

“…Advances in Cancer Research, volume 153 provides a timely review of the biology, biochemistry, and current approaches to therapeutically target the RAS…”
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Emerging roles for intersectin (ITSN) in regulating signaling and disease pathways by Hunter, Michael P, Russo, Angela, O'Bryan, John P

“…Intersectins (ITSNs) represent a family of multi-domain adaptor proteins that regulate endocytosis and cell signaling. ITSN genes are highly conserved and…”
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