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Recent Submissions

  • The cardiolipin-binding peptide elamipretide mitigates fragmentation of cristae networks following cardiac ischemia reperfusion in rats 

    Allen, Mitchell E.; Pennington, Edward Ross; Perry, Justin B.; Dadoo, Sahil; Makrecka-Kuka, Marina; Dambrova, Maija; Moukdar, Fatiha; Patel, Hetal D.; Han, Xianlin; Kidd, Grahame K.; Benson, Emily K.; Raisch, Tristan B.; Poelzing, Steven; Brown, David A.; Shaikh, Saame Raza (2020-07-17)
    Allen and Pennington et al. show that the cardiolipin-binding peptide elamipretide mitigates disease-induced fragmentation of cristae networks following cardiac ischemia reperfusion in rats. This study suggests that ...
  • Structural, in silico, and functional analysis of a Disabled-2-derived peptide for recognition of sulfatides 

    Song, Wei; Gottschalk, Carter J.; Tang, Tuo-Xian; Biscardi, Andrew; Ellena, Jeffrey F.; Finkielstein, Carla, V; Brown, Anne M.; Capelluto, Daniel G. S. (2020-08-11)
    Disabled-2 (Dab2) is an adaptor protein that regulates the extent of platelet aggregation by two mechanisms. In the first mechanism, Dab2 intracellularly downregulates the integrin alpha (IIb)beta (3) receptor, converting ...
  • Photoacoustic microscopy reveals the hemodynamic basis of sphingosine 1-phosphate-induced neuroprotection against ischemic stroke 

    Cao, Rui; Li, Jun; Kharel, Yugesh; Zhang, Chenchu; Morris, Emily; Santos, Webster L.; Lynch, Kevin R.; Zuo, Zhiyi; Hu, Song (IvySpring, 2018-11-29)
    Rationale: Emerging evidence has suggested that sphingosine 1-phosphate (S1P), a bioactive metabolite of sphingolipids, may play an important role in the pathophysiological processes of cerebral hypoxia and ischemia. ...
  • Mechanism of sphingosine 1-phosphate clearance from blood 

    Kharel, Yugesh; Huang, Tao; Salamon, Anita; Harris, Thurl E.; Santos, Webster L.; Lynch, Kevin R. (Portland Press, 2020-03-06)
    The interplay of sphingosine 1-phosphate (S1P) synthetic and degradative enzymes as well as S1P exporters creates concentration gradients that are a fundamental to S1P biology. Extracellular S1P levels, such as in blood ...
  • Identification of a novel mitochondrial uncoupler that does not depolarize the plasma membrane 

    Kenwood, Brandon M.; Weaver, Janelle L.; Bajwa, Amandeep; Poon, Ivan K.; Byrne, Frances L.; Murrow, Beverley A.; Calderone, Joseph A.; Huang, Liping; Divakaruni, Ajit S.; Tomsig, Jose L.; Okabe, Kohki; Lo, Ryan H.; Coleman, G. Cameron; Columbus, Linda; Yan, Zhen; Saucerman, Jeffrey J.; Smith, Jeffrey S.; Holmes, Jeffrey W.; Lynch, Kevin R.; Ravichandran, Kodi S.; Uchiyama, Seiichi; Santos, Webster L.; Rogers, George W.; Okusa, Mark D.; Bayliss, Douglas A.; Hoehn, Kyle L. (Elsevier, 2013)
    Dysregulation of oxidative phosphorylation is associated with increased mitochondrial reactive oxygen species production and some of the most prevalent human diseases including obesity, cancer, diabetes, neurodegeneration, ...
  • 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 

    Chemistry; Center for Drug Discovery; 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)

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