Search Results - "Do, Mary K. Geck"

Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2 by Poncet-Montange, Guillaume, Zhan, Yanai, Bardenhagen, Jennifer P, Petrocchi, Alessia, Leo, Elisabetta, Shi, Xi, Lee, 4th, Gilbert R, Leonard, Paul G, Geck Do, Mary K, Cardozo, Mario G, Andersen, Jannik N, Palmer, Wylie S, Jones, Philip, Ladbury, John E

“…Preventing histone recognition by bromodomains emerges as an attractive therapeutic approach in cancer. Overexpression of ATAD2 (ATPase family AAA…”
Get more information

PRMT1-dependent regulation of RNA metabolism and DNA damage response sustains pancreatic ductal adenocarcinoma by Giuliani, Virginia, Miller, Meredith A., Liu, Chiu-Yi, Hartono, Stella R., Class, Caleb A., Bristow, Christopher A., Suzuki, Erika, Sanz, Lionel A., Gao, Guang, Gay, Jason P., Feng, Ningping, Rose, Johnathon L., Tomihara, Hideo, Daniele, Joseph R., Peoples, Michael D., Bardenhagen, Jennifer P., Geck Do, Mary K., Chang, Qing E., Vangamudi, Bhavatarini, Vellano, Christopher, Ying, Haoqiang, Deem, Angela K., Do, Kim-Anh, Genovese, Giannicola, Marszalek, Joseph R., Kovacs, Jeffrey J., Kim, Michael, Fleming, Jason B., Guccione, Ernesto, Viale, Andrea, Maitra, Anirban, Emilia Di Francesco, M., Yap, Timothy A., Jones, Philip, Draetta, Giulio, Carugo, Alessandro, Chedin, Frederic, Heffernan, Timothy P.

“…Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer that has remained clinically challenging to manage. Here we employ an RNAi-based in vivo…”
Get full text

Spirocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: From Hit to Lowering of Cerebrospinal Fluid (CSF) Amyloid β in a Higher Species by Hunt, Kevin W, Cook, Adam W, Watts, Ryan J, Clark, Christopher T, Vigers, Guy, Smith, Darin, Metcalf, Andrew T, Gunawardana, Indrani W, Burkard, Michael, Cox, April A, Geck Do, Mary K, Dutcher, Darrin, Thomas, Allen A, Rana, Sumeet, Kallan, Nicholas C, DeLisle, Robert K, Rizzi, James P, Regal, Kelly, Sammond, Douglas, Groneberg, Robert, Siu, Michael, Purkey, Hans, Lyssikatos, Joseph P, Marlow, Allison, Liu, Xingrong, Tang, Tony P

“…A hallmark of Alzheimer’s disease is the brain deposition of amyloid beta (Aβ), a peptide of 36–43 amino acids that is likely a primary driver of…”
Get full text

8‑Tetrahydropyran-2-yl Chromans: Highly Selective Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors by Thomas, Allen A, Hunt, Kevin W, Newhouse, Brad, Watts, Ryan J, Liu, Xingrong, Vigers, Guy, Smith, Darin, Rhodes, Susan P, Brown, Karin D, Otten, Jennifer N, Burkard, Michael, Cox, April A, Geck Do, Mary K, Dutcher, Darrin, Rana, Sumeet, DeLisle, Robert K, Regal, Kelly, Wright, Albion D, Groneberg, Robert, Liao, Jiangpeng, Scearce-Levie, Kimberly, Siu, Michael, Purkey, Hans E, Lyssikatos, Joseph P

“…A series of 2,3,4,4a,10,10a-hexahydropyrano[3,2-b]chromene analogs was developed that demonstrated high selectivity (>2000-fold) for BACE1 vs Cathepsin D…”
Get full text

Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery by Zhan, Yanai, Kost-Alimova, Maria, Shi, Xi, Leo, Elisabetta, Bardenhagen, Jennifer P, Shepard, Hannah E, Appikonda, Srikanth, Vangamudi, Bhavatarini, Zhao, Shuping, Tieu, Trang N, Jiang, Shiming, Heffernan, Timothy P, Marszalek, Joseph R, Toniatti, Carlo, Draetta, Giulio, Tyler, Jessica, Barton, Michelle, Jones, Philip, Palmer, Wylie S, Geck Do, Mary K, Andersen, Jannik N

“…Proteins that 'read' the histone code are central elements in epigenetic control and bromodomains, which bind acetyl-lysine motifs, are increasingly recognized…”
Get full text

Discovery of IPN60090, a Clinical Stage Selective Glutaminase‑1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties by Soth, Michael J, Le, Kang, Di Francesco, Maria Emilia, Hamilton, Matthew M, Liu, Gang, Burke, Jason P, Carroll, Chris L, Kovacs, Jeffrey J, Bardenhagen, Jennifer P, Bristow, Christopher A, Cardozo, Mario, Czako, Barbara, de Stanchina, Elisa, Feng, Ningping, Garvey, Jill R, Gay, Jason P, Do, Mary K. Geck, Greer, Jennifer, Han, Michelle, Harris, Angela, Herrera, Zachary, Huang, Sha, Giuliani, Virginia, Jiang, Yongying, Johnson, Sarah B, Johnson, Troy A, Kang, Zhijun, Leonard, Paul G, Liu, Zhen, McAfoos, Timothy, Miller, Meredith, Morlacchi, Pietro, Mullinax, Robert A, Palmer, Wylie S, Pang, Jihai, Rogers, Norma, Rudin, Charles M, Shepard, Hannah E, Spencer, Nakia D, Theroff, Jay, Wu, Qi, Xu, Alan, Yau, Ju Anne, Draetta, Giulio, Toniatti, Carlo, Heffernan, Timothy P, Jones, Philip

“…Inhibition of glutaminase-1 (GLS-1) hampers the proliferation of tumor cells reliant on glutamine. Known glutaminase inhibitors have potential limitations, and…”
Get full text

Ataxia-Telangiectasia Mutated Loss-of-Function Displays Variant and Tissue-Specific Differences across Tumor Types by Pilié, Patrick G, Giuliani, Virginia, Wang, Wei-Lien, McGrail, Daniel J, Bristow, Christopher A, Ngoi, Natalie Y L, Kyewalabye, Keith, Wani, Khalida M, Le, Hung, Campbell, Erick, Sanchez, Nora S, Yang, Dong, Gheeya, Jinesh S, Goswamy, Rohit Vivek, Holla, Vijaykumar, Shaw, Kenna Rael, Meric-Bernstam, Funda, Liu, Chiu-Yi, Ma, XiaoYan, Feng, Ningping, Machado, Annette A, Bardenhagen, Jennifer P, Vellano, Christopher P, Marszalek, Joseph R, Rajendra, Eeson, Piscitello, Desiree, Johnson, Timothy I, Likhatcheva, Maria, Elinati, Elias, Majithiya, Jayesh, Neves, Joana, Grinkevich, Vera, Ranzani, Marco, Luzarraga, Marina Roy, Boursier, Marie, Armstrong, Lucy, Geo, Lerin, Lillo, Giorgia, Tse, Wai Yiu, Lazar, Alexander J, Kopetz, Scott E, Geck Do, Mary K, Lively, Sarah, Johnson, Michael G, Robinson, Helen M R, Smith, Graeme C M, Carroll, Christopher L, Di Francesco, M Emilia, Jones, Philip, Heffernan, Timothy P, Yap, Timothy A

“…Mutations in the ATM gene are common in multiple cancers, but clinical studies of therapies targeting ATM-aberrant cancers have yielded mixed results…”
Get full text

Discovery of 7‑Tetrahydropyran-2-yl Chromans: β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors That Reduce Amyloid β‑Protein (Aβ) in the Central Nervous System by Thomas, Allen A, Hunt, Kevin W, Volgraf, Matthew, Watts, Ryan J, Liu, Xingrong, Vigers, Guy, Smith, Darin, Sammond, Douglas, Tang, Tony P, Rhodes, Susan P, Metcalf, Andrew T, Brown, Karin D, Otten, Jennifer N, Burkard, Michael, Cox, April A, Do, Mary K. Geck, Dutcher, Darrin, Rana, Sumeet, DeLisle, Robert K, Regal, Kelly, Wright, Albion D, Groneberg, Robert, Scearce-Levie, Kimberly, Siu, Michael, Purkey, Hans E, Lyssikatos, Joseph P, Gunawardana, Indrani W

“…In an attempt to increase selectivity vs Cathepsin D (CatD) in our BACE1 program, a series of 1,3,4,4a,10,10a-hexahydropyrano[4,3-b]chromene analogues was…”
Get full text

Abstract 1655: Discovery and development of IACS-010759, a novel inhibitor of Complex I currently in phase I studies to exploit oxidative phosphorylation dependency in acute myeloid leukemia and solid tumors by Francesco, Maria Emilia Di, Marszalek, Joseph R., McAfoos, Timothy, Carroll, Christopher L., Kang, Zhijun, Liu, Gang, Theroff, Jay P., Bardenhager, Jennifer P., Bandi, Madhavi L., Molina, Jennifer R., Gera, Sonal, Protopopova, Marina, Sun, Yuting, Do, Mary K. Geck, Feng, Ningping, Gay, Jason P., Muller, Florian, Konopleva, Marina, Meric-Bernstam, Funda, Toniatti, Carlo, Heffernan, Timothy P., Draetta, Giulio F., Jones, Philip

“…Abstract Over the past few years we and others reported that specific populations of tumor cells including AML, subsets of lymphoma, glioblastoma, triple…”
Get full text

Abstract PR01: IACS-010759 a novel inhibitor of oxidative phosphorylation advancing into first-in-human studies to exploit metabolic vulnerabilities by Jones, Philip, Francesco, M Emilia Di, Molina, Jennifer M., Protopopova, Marina, Bandi, Madhavi, Bardenhagen, Jennifer, Bristow, Christopher A., Carroll, Christopher L., Feng, Ningping, Gay, Jason P., Do, Mary K. Geck, Greer, Jennifer M., Konopleva, Marina, Kang, Zhijun, Liu, Gang, McAfoos, Timothy, Morlacchi, Pietro, Smith, Melinda G., Fnu, Sonal, Theroff, Jay P., Draetta, Giulio, Toniatti, Carlo, Marszalek, Joseph R.

“…Abstract Tumor cells normally depend on both glycolysis and oxidative phosphorylation (OXPHOS) to provide the energy and macromolecule building blocks needed…”
Get full text