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  • Phenotypic screen for oxygen consumption rate identifies an anti-cancer naphthoquinone that induces mitochondrial oxidative stress 

    Byrne, Frances L.; Olzomer, Ellen M.; Marriott, Gabriella R.; Quek, Lake-Ee; Katen, Alice; Su, Jacky; Nelson, Marin E.; Hart-Smith, Gene; Larance, Mark; Sebesfi, Veronica F.; Cuff, Jeff; Martyn, Gabriella E.; Childress, Elizabeth; Alexopoulos, Stephanie J.; Poon, Ivan K.; Faux, Maree C.; Burgess, Antony W.; Reid, Glen; McCarroll, Joshua A.; Santos, Webster L.; Quinlan, Kate G. R.; Turner, Nigel; Fazakerley, Daniel J.; Kumar, Naresh; Hoehn, Kyle L. (2020-01)
    A hallmark of cancer cells is their ability to reprogram nutrient metabolism. Thus, disruption to this phenotype is a potential avenue for anti-cancer therapy. Herein we used a phenotypic chemical library screening approach ...
  • Flavin oxidation in flavin dependent N-monooxygenase 

    Sobrado, Pablo; Robinson, Reeder; Klancher, Catherine; Rodriguez, Pedro (2019-01-02)
  • Peripheral loss of EphA4 ameliorates TBI-induced neuroinflammation and tissue damage 

    Kowalski, Elizabeth A.; Chen, Jiang; Hazy, Amanda; Fritsch, Lauren E.; Gudenschwager-Basso, Erwin K.; Chen, Michael; Wang, Xia; Qian, Yun; Zhou, Mingjun; Byerly, Matthew; Pickrell, Alicia M.; Matson, John B.; Allen, Irving C.; Theus, Michelle H. (2019-11-11)
    Abstract Background The continuum of pro- and anti-inflammatory response elicited by traumatic brain injury (TBI) is suggested to play a key role in the outcome of TBI; however, ...
  • Mobilization studies in mice deficient in sphingosine kinase 2 support a crucial role of the plasma level of sphingosine-1-phosphate in the egress of hematopoietic stem progenitor cells 

    Adamiak, Mateusz; Chelvarajan, Lakshman; Lynch, Kevin R.; Santos, Webster L.; Abdel-Latif, Ahmed; Ratajczak, Mariusz Z. (2017-09-12)
    Sphingosine-1-phosphate (S1P) is a bioactive lipid involved in cell signaling and, if released from cells, also plays a crucial role in regulating the trafficking of lympho-hematopoietic cells, including primitive hematopoietic ...
  • Saccharomyces cerevisiae as a platform for assessing sphingolipid lipid kinase inhibitors 

    Kharel, Yugesh; Agah, Sayeh; Huang, Tao; Mendelson, Anna J.; Eletu, Oluwafunmilayo T.; Barkey-Bircannl, Peter; Gesualdil, James; Smith, Jeffrey S.; Santos, Webster L.; Lynch, Kevin R. (PLOS, 2018-04-19)
    Successful medicinal chemistry campaigns to discover and optimize sphingosine kinase inhibitors require a robust assay for screening chemical libraries and for determining rank order potencies. Existing assays for these ...
  • Inhibiting neurotransmitter reuptake 

    Virginia Tech Intellectual Properties, Inc.; Mayo Foundation for Medical Edication and Research; Carlier, Paul R.; Richelson, Elliott; Fauq, Abdul H.; Monceaux, Christopher J. (United States Patent and Trademark Office, 2018-04-17)
    This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter ...
  • Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond 

    Van Voorhis, Wesley C.; Adams, John H.; Adelfio, Roberto; Ahyong, Vida; Akabas, Myles H.; Alano, Pietro; Alday, Aintzane; Resto, Yesmalie Aleman; Alsibaee, Aishah; Alzualde, Ainhoa; Andrews, Katherine T.; Avery, Simon V.; Avery, Vicky M.; Ayong, Lawrence; Baker, Mark; Baker, Stephen; Ben Mamoun, Choukri; Bhatia, Sangeeta; Bickle, Quentin; Bounaadja, Lotfi; Bowling, Tana; Bosch, Juergen; Boucher, Lauren E.; Boyom, Fabrice F.; Brea, Jose; Brennan, Marian; Burton, Audrey; Caffrey, Conor R.; Camarda, Grazia; Carrasquilla, Manuela; Carter, Dee; Cassera, Maria Belen; Cheng, Ken Chih-Chien; Chindaudomsate, Worathad; Chubb, Anthony; Colon, Beatrice L.; Colon-Lopez, Daisy D.; Corbett, Yolanda; Crowther, Gregory J.; Cowan, Noemi; D'Alessandro, Sarah; Le Dang, Na; Delves, Michael; DeRisi, Joseph L.; Du, Alan Y.; Duffy, Sandra; El-Sayed, Shimaa Abd El-Salam; Ferdig, Michael T.; Robledo, Jose A. Fernandez; Fidock, David A.; Florent, Isabelle; Fokou, Patrick V. T.; Galstian, Ani; Javier Gamo, Francisco; Gokool, Suzanne; Gold, Ben; Golub, Todd; Goldgof, Gregory M.; Guha, Rajarshi; Guiguemde, W. Armand; Gural, Nil; Guy, R. Kiplin; Hansen, Michael A. E.; Hanson, Kirsten K.; Hemphill, Andrew; van Huijsduijnen, Rob Hooft; Horii, Takaaki; Horrocks, Paul; Hughes, Tyler B.; Huston, Christopher; Igarashi, Ikuo; Ingram-Sieber, Katrin; Itoe, Maurice A.; Jadhav, Ajit; Jensen, Amornrat Naranuntarat; Jensen, Laran T.; Jiang, Rays H. Y.; Kaiser, Annette; Keiser, Jennifer; Ketas, Thomas; Kicka, Sebastien; Kim, Sunyoung; Kirk, Kiaran; Kumar, Vidya P.; Kyle, Dennis E.; Jose Lafuente, Maria; Landfear, Scott; Lee, Nathan; Lee, Sukjun; Lehane, Adele M.; Li, Fengwu; Little, David; Liu, Liqiong; Llinas, Manuel; Loza, Maria I.; Lubar, Aristea; Lucantoni, Leonardo; Lucet, Isabelle; Maes, Louis; Mancama, Dalu; Mansour, Nuha R.; March, Sandra; McGowan, Sheena; Vera, Iset Medina; Meister, Stephan; Mercer, Luke; Mestres, Jordi; Mfopa, Alvine N.; Misra, Raj N.; Moon, Seunghyun; Moore, John P.; Rodrigues da Costa, Francielly Morais; Mueller, Joachim; Muriana, Arantza; Hewitt, Stephen Nakazawa; Nare, Bakela; Nathan, Carl; Narraidoo, Nathalie; Nawaratna, Sujeevi; Ojo, Kayode K.; Ortiz, Diana; Panic, Gordana; Papadatos, George; Parapini, Silvia; Patra, Kailash; Ngoc Pham; Prats, Sarah; Plouffe, David M.; Poulsen, Sally-Ann; Pradhan, Anupam; Quevedo, Celia; Quinn, Ronald J.; Rice, Christopher A.; Rizk, Mohamed Abdo; Ruecker, Andrea; St Onge, Robert; Ferreira, Rafaela Salgado; Samra, Jasmeet; Robinett, Natalie G.; Schlecht, Ulrich; Schmitt, Marjorie; Villela, Filipe Silva; Silvestrini, Francesco; Sinden, Robert; Smith, Dennis A.; Soldati, Thierry; Spitzmueller, Andreas; Stamm, Serge Maximilian; Sullivan, David J.; Sullivan, William; Suresh, Sundari; Suzuki, Brian M.; Suzuki, Yo; Swamidass, S. Joshua; Taramelli, Donatella; Tchokouaha, Lauve R. Y.; Theron, Anjo; Thomas, David; Tonissen, Kathryn F.; Townson, Simon; Tripathi, Abhai K.; Trofimov, Valentin; Udenze, Kenneth O.; Ullah, Imran; Vallieres, Cindy; Vigil, Edgar; Vinetz, Joseph M.; Phat Voong Vinh; Hoan Vu; Watanabe, Nao-aki; Weatherby, Kate; White, Pamela M.; Wilks, Andrew F.; Winzeler, Elizabeth A.; Wojcik, Edward; Wree, Melanie; Wu, Wesley; Yokoyama, Naoaki; Zollo, Paul H. A.; Abla, Nada; Blasco, Benjamin; Burrows, Jeremy; Laleu, Benoit; Leroy, Didier; Spangenberg, Thomas; Wells, Timothy; Willis, Paul A. (PLOS, 2016-07-28)
    A major cause of the paucity of new starting points for drug discovery is the lack of interaction between academia and industry. Much of the global resource in biology is present in universities, whereas the focus of ...
  • Characterization of the Ornithine Hydroxylation Step in Albachelin Biosynthesis 

    Bufkin, Kendra; Sobrado, Pablo (MDPI, 2017-10-01)
    N-Hydroxylating monooxygenases (NMOs) are involved in siderophore biosynthesis. Siderophores are high affinity iron chelators composed of catechol and hydroxamate functional groups that are synthesized and secreted ...
  • Identification of Aspergillus fumigatus UDP-Galactopyranose Mutase Inhibitors 

    del Campo, Julia S. Martin; Eckshtain-Levi, Meital; Vogelaar, Nancy J.; Sobrado, Pablo (Nature, 2017-09-07)
    Aspergillus fumigatus is an opportunistic human pathogen responsible for deadly, invasive infections in immunocompromised patients. The A. fumigatus cell wall is a complex network of polysaccharides among them galactofuran, ...
  • Fluorescence Polarization Binding Assay for Aspergillus fumigatus Virulence Factor UDP-Galactopyranose Mutase 

    Qi, Jun; Oppenheimer, Michelle; Sobrado, Pablo (Hindawi, 2011-08-21)
    Aspergillus fumigatus is an opportunistic human pathogenic fungus responsible for deadly lung infections in immunocompromised individuals. Galactofuranose (Galf) residues are essential components of the cell wall and play ...
  • A rapid and high content assay that measures cyto-ID-stained autophagic compartments and estimates autophagy flux with potential clinical applications 

    Guo, Sujuan; Liang, Yanping; Murphy, Susan F.; Huang, Angela; Shen, Haihong; Kelly, Deborah F.; Sobrado, Pablo; Sheng, Zhi (Taylor & Francis Inc, 2015-03-01)
    The lack of a rapid and quantitative autophagy assay has substantially hindered the development and implementation of autophagy-targeting therapies for a variety of human diseases. To address this critical issue, we developed ...
  • Antiproliferative triterpenoid saponins from Leptaulus citroides Baill. from the Madagascar rain forest 

    Su, Qingxi; Brodie, Peggy J.; Liu, Yixi; Miller, James S.; Andrianjafy, Naina M.; Antsiferana, Rabodo; Rasamison, Vincent E.; Kingston, David G. I. (Springer, 2016)
    Bioassay-guided fractionation of EtOH extracts obtained from the roots and wood of the Madagascan plant Leptaulus citroides Baill. (Cardiopteridaceae) led to the isolation of ethyl esters of three new triterpenoid saponins ...
  • Nitrogen-Containing Dimeric nor-Multiflorane Triterpene from a Turraea sp. 

    Rasamison, Vincent E.; Rakotondraibe, L. Harinantenaina; Slebodnick, Carla; Brodie, Peggy J.; Ratsimbason, Michael; TenDyke, Karen; Shen, Yongchun; Randrianjanaka, Lucien M.; Kingston, David G. I. (Amer Chemical Soc, 2014-05-16)
    The new triterpene turranoic acid (1) and thenew N-containing nor-triterpene turraenine (2), along with triptocallic acid B (3) and esculentoic acid (4) were isolated from leaves of a Turraea sp. Compounds 1-3 showed weak ...
  • The Quest for a Simple Bioactive Analog of Paclitaxel as a Potential Anticancer Agent 

    Kingston, David G. I.; Snyder, J. P. (Amer Chemical Soc, 2014-08-01)
  • Antiproliferative Compounds from Cleistanthus boivinianus from the Madagascar Dry Forest 

    Liu, Yixi; Young, Kelly; Rakotondraibe, L. Harinantenaina; Brodie, Peggy J.; Wiley, Jessica D.; Cassera, Maria B.; Callmander, Martin W.; Rakotondrajaona, R; Rakotobe, Etienne; Rasamison, Vincent E.; TenDyke, Karen; Shen, Yongchun; Kingston, David G. I. (Amer Chemical Soc, 2015-07-01)
  • Antimalarial 5,6-Dihydro-alpha-pyrones from Cryptocarya rigidifolia: Related Bicyclic Tetrahydro-alpha-Pyrones Are Artifacts 

    Liu, Yixi; Rakotondraibe, L. Harinantenaina; Brodie, Peggy J.; Wiley, Jessica D.; Cassera, Maria B.; Miller, James S.; Ratovoson, F.; Rakotobe, Etienne; Rasamison, Vincent E.; Kingston, David G. I. (Amer Chemical Soc, 2015-06-01)
  • Crystal structure of the MACPF domain of human complement protein C8 alpha in complex with the C8 gamma subunit 

    Slade, Daniel J.; Lovelace, Leslie L.; Chruszcz, Maksymilian; Minor, Wladek; Lebioda, Lukasz; Sodetz, James M. (Academic Press Ltd Elsevier Science Ltd, 2008-05-29)
    Human C8 is one of five complement components (C5b, C6, C7, C8 and C9) that assemble on bacterial membranes to form a pore-like structure referred to as the "membrane attack complex" (MAC). C8 contains three genetically ...
  • Peptidylarginine deiminase 2-catalyzed histone H3 arginine 26 citrullination facilitates estrogen receptor alpha target gene activation 

    Zhang, Xuesen; Bolt, Michael; Guertin, Michael J.; Chen, Wei; Zhang, Sheng; Cherrington, Brian D.; Slade, Daniel J.; Dreyton, Cchristina J.; Subramanian, Venkataraman; Bicker, Kevin L.; Thompson, Paul R.; Mancini, Michael A.; Lis, John T,; Coonrod, Scott A. (2012-08-14)
    Cofactors for estrogen receptor α (ERα) can modulate gene activity by posttranslationally modifying histone tails at target promoters. Here, we found that stimulation of ERα-positive cells with 17β-estradiol (E2) promotes ...
  • Chemical and Biological Methods to Detect Post-Translational Modifications of Arginine 

    Slade, Daniel J.; Subramanian, Venkataraman; Fuhrmann, Jakob; Thompson, Paul R. (2014-02)
    Posttranslational modifications (PTMs) of protein embedded arginines are increasingly being recognized as playing an important role in both prokaryotic and eukaryotic biology, and it is now clear that these PTMs modulate ...
  • Citrulination unravels stem cells 

    Slade, Daniel J.; Subramanian, Venkataraman; Thompson, Paul R. (2014-05)
    Maintenance of the pluripotent stem cell state is regulated by the post-translational modification of histones. The discovery that citrullination of the linker histone H1 is critical to this

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