Search Results - "Koehn, Frank"

The antibody-drug conjugate: an enabling modality for natural product-based cancer therapeutics by Gerber, Hans-Peter, Koehn, Frank E, Abraham, Robert T

“…The Antibody Drug Conjugate (ADC) is a therapeutic modality consisting of a monoclonal antibody attached to a cytotoxic, small-molecule payload. The antibody…”
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Spliceostatin hemiketal biosynthesis in Burkholderia spp. is catalyzed by an iron/α-ketoglutarate-dependent dioxygenase by Eustáquio, Alessandra S., Janso, Jeffrey E., Ratnayake, Anokha S., O'Donnell, Christopher J., Koehn, Frank E.

“…Spliceostatins are potent spliceosome inhibitors biosynthesized by a hybrid nonribosomal peptide synthetase-polyketide synthase (NRPS-PKS) system of the…”
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Diversity oriented biosynthesis via accelerated evolution of modular gene clusters by Wlodek, Aleksandra, Kendrew, Steve G., Coates, Nigel J., Hold, Adam, Pogwizd, Joanna, Rudder, Steven, Sheehan, Lesley S., Higginbotham, Sarah J., Stanley-Smith, Anna E., Warneck, Tony, Nur-E-Alam, Mohammad, Radzom, Markus, Martin, Christine J., Overvoorde, Lois, Samborskyy, Markiyan, Alt, Silke, Heine, Daniel, Carter, Guy T., Graziani, Edmund I., Koehn, Frank E., McDonald, Leonard, Alanine, Alexander, Rodríguez Sarmiento, Rosa María, Chao, Suzan Keen, Ratni, Hasane, Steward, Lucinda, Norville, Isobel H., Sarkar-Tyson, Mitali, Moss, Steven J., Leadlay, Peter F., Wilkinson, Barrie, Gregory, Matthew A.

“…Erythromycin, avermectin and rapamycin are clinically useful polyketide natural products produced on modular polyketide synthase multienzymes by an…”
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New Strategies and Methods in the Discovery of Natural Product Anti-Infective Agents: The Mannopeptimycins by Koehn, Frank E

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Discovery of the lomaiviticin biosynthetic gene cluster in Salinispora pacifica by Janso, Jeffrey E., Haltli, Brad A., Eustáquio, Alessandra S., Kulowski, Kerry, Waldman, Abraham J., Zha, Li, Nakamura, Hitomi, Bernan, Valerie S., He, Haiyin, Carter, Guy T., Koehn, Frank E., Balskus, Emily P.

“…The lomaiviticins are a family of cytotoxic marine natural products that have captured the attention of both synthetic and biological chemists due to their…”
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Cytotoxic Spliceostatins from Burkholderia sp. and Their Semisynthetic Analogues by He, Haiyin, Ratnayake, Anokha S, Janso, Jeffrey E, He, Min, Yang, Hui Y, Loganzo, Frank, Shor, Boris, O’Donnell, Christopher J, Koehn, Frank E

“…The spliceostatin class of natural products was reported to be potent cytotoxic agents via inhibition of the spliceosome, a key protein complex in the…”
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Biosynthesis of the immunosuppressants FK506, FK520, and rapamycin involves a previously undescribed family of enzymes acting on chorismate by Andexer, Jennifer N, Kendrew, Steven G, Nur-e-Alam, Mohammad, Lazos, Orestis, Foster, Teresa A, Zimmermann, Anna-Sophie, Warneck, Tony D, Suthar, Dipen, Coates, Nigel J, Koehn, Frank E, Skotnicki, Jerauld S, Carter, Guy T, Gregory, Matthew A, Martin, Christine J, Moss, Steven J, Leadlay, Peter F, Wilkinson, Barrie

“…The macrocyclic polyketides FK506, FK520, and rapamycin are potent immunosuppressants that prevent T-cell proliferation through initial binding to the…”
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Natural Product Bis-Intercalator Depsipeptides as a New Class of Payloads for Antibody–Drug Conjugates by Ratnayake, Anokha S, Chang, Li-ping, Tumey, L. Nathan, Loganzo, Frank, Chemler, Joseph A, Wagenaar, Melissa, Musto, Sylvia, Li, Fengping, Janso, Jeffrey E, Ballard, T. Eric, Rago, Brian, Steele, Greg L, Ding, WeiDong, Feng, Xidong, Hosselet, Christine, Buklan, Vlad, Lucas, Judy, Koehn, Frank E, O’Donnell, Christopher J, Graziani, Edmund I

“…A potent class of DNA-damaging agents, natural product bis-intercalator depsipeptides (NPBIDs), was evaluated as ultrapotent payloads for use in antibody–drug…”
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Borrelidin B: Isolation, Biological Activity, and Implications for Nitrile Biosynthesis by Schulze, Christopher J, Bray, Walter M, Loganzo, Frank, Lam, My-Hanh, Szal, Teresa, Villalobos, Anabella, Koehn, Frank E, Linington, Roger G

“…Borrelidin (1) is a nitrile-containing bacterially derived polyketide that is a potent inhibitor of bacterial and eukaryotic threonyl-tRNA synthetases. We now…”
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Discovery and Assembly-Line Biosynthesis of the Lymphostin Pyrroloquinoline Alkaloid Family of mTOR Inhibitors in Salinispora Bacteria by Miyanaga, Akimasa, Janso, Jeffrey E, McDonald, Leonard, He, Min, Liu, Hongbo, Barbieri, Laurel, Eustáquio, Alessandra S, Fielding, Elisha N, Carter, Guy T, Jensen, Paul R, Feng, Xidong, Leighton, Margaret, Koehn, Frank E, Moore, Bradley S

“…The pyrroloquinoline alkaloid family of natural products, which includes the immunosuppressant lymphostin, has long been postulated to arise from tryptophan…”
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Biosynthetic engineering and fermentation media development leads to gram-scale production of spliceostatin natural products in Burkholderia sp by Eustáquio, Alessandra S., Chang, Li-Ping, Steele, Greg L., O׳Donnell, Christopher J., Koehn, Frank E.

“…A key challenge in natural products drug discovery is compound supply. Hundreds of grams of purified material are needed to advance a natural product lead…”
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The evolving role of natural products in drug discovery by Koehn, Frank E, Carter, Guy T

“…Natural products and their derivatives have historically been invaluable as a source of therapeutic agents. However, in the past decade, research into natural…”
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Synthesis of rapamycin glycoconjugates via a CuAAC-based approach by Moni, Lisa, Marra, Alberto, Skotnicki, Jerauld S., Koehn, Frank E., Abou-Gharbia, Magid, Dondoni, Alessandro

“…The conversion of the C40 secondary hydroxyl group of rapamycin into the azido group was followed by copper catalyzed cycloaddition of the resulting…”
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Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities by Ruan, Benfang, Pong, Kevin, Jow, Flora, Bowlby, Mark, Crozier, Robert A, Liu, Danni, Liang, Shi, Chen, Yi, Mercado, Mary Lynn, Feng, Xidong, Bennett, Frann, von Schack, David, McDonald, Leonard, Zaleska, Margaret M, Wood, Andrew, Reinhart, Peter H, Magolda, Ronald L, Skotnicki, Jerauld, Pangalos, Menelas N, Koehn, Frank E, Carter, Guy T, Abou-Gharbia, Magid, Graziani, Edmund I

“…Rapamycin is an immunosuppressive immunophilin ligand reported as having neurotrophic activity. We show that modification of rapamycin at the mammalian target…”
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Absolute Configurational Assignments of Secondary Amines by CD-Sensitive Dimeric Zinc Porphyrin Host by Huang, Xuefei, Fujioka, Naoko, Pescitelli, Gennaro, Koehn, Frank E, Williamson, R. Thomas, Nakanishi, Koji, Berova, Nina

“…A general chiroptical protocol for determination of absolute configuration of secondary amines including acyclic and cyclic aliphatic amines, aromatic amines,…”
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Therapeutic potential of natural product signal transduction agents by Koehn, Frank E

“…Modern drug discovery embraces a strategy of targeting cellular signal transduction pathways as a means of finding new therapeutic agents. Historically,…”
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Recombinant strains for the enhanced production of bioengineered rapalogs by Kendrew, Steven G., Petkovic, Hrvoje, Gaisser, Sabine, Ready, Sarah J., Gregory, Matthew A., Coates, Nigel J., Nur-e-Alam, Mohammad, Warneck, Tony, Suthar, Dipen, Foster, Teresa A., McDonald, Leonard, Schlingman, Gerhard, Koehn, Frank E., Skotnicki, Jerauld S., Carter, Guy T., Moss, Steven J., Zhang, Ming-Qiang, Martin, Christine J., Sheridan, Rose M., Wilkinson, Barrie

“…The rapK gene required for biosynthesis of the DHCHC starter acid that initiates rapamycin biosynthesis was deleted from strain BIOT-3410, a derivative of…”
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Reassessing the Structure of Pyranonigrin by Schlingmann, Gerhard, Taniguchi, Tohru, He, Haiyin, Bigelis, Ramunas, Yang, Hui Y, Koehn, Frank E, Carter, Guy T, Berova, Nina

“…Fermentation extracts of the marine fungus Aspergillus niger LL-LV3020 were found to have relevant activity in a number of assays. Chemical screening of the…”
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6-Substituted-4-(3-bromophenylamino)quinazolines as Putative Irreversible Inhibitors of the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor (HER-2) Tyrosine Kinases with Enhanced Antitumor Activity by Tsou, Hwei-Ru, Mamuya, Nellie, Johnson, Bernard D, Reich, Marvin F, Gruber, Brian C, Ye, Fei, Nilakantan, Ramaswamy, Shen, Ru, Discafani, Carolyn, DeBlanc, Ronald, Davis, Rachel, Koehn, Frank E, Greenberger, Lee M, Wang, Yu-Fen, Wissner, Allan

“…A series of new 6-substituted-4-(3-bromophenylamino)quinazoline derivatives that may function as irreversible inhibitors of epidermal growth factor receptor…”
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Amphotericin B, identified from a natural product screen, antagonizes CNS inhibitors to promote axon growth via activation of an Akt pathway in neurons by Gao, Ying, Deng, Kangwen, Cao, Zixuan, Graziani, Edmund I, Gilbert, Adam M, Koehn, Frank E, Wood, Andrew, Doherty, Patrick, Walsh, Frank S

“…J. Neurochem. (2010) 113, 1331-1342. One of the major barriers to successful axon regeneration in the adult CNS is the presence of inhibitory molecules that…”
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