Search Results - "Showalter, Hollis"

Recent Progress in the Discovery and Development of 2-Nitroimidazooxazines and 6-Nitroimidazooxazoles to Treat Tuberculosis and Neglected Tropical Diseases by Showalter, Hollis D

“…Nitroimidazole drugs have a long history as therapeutic agents to treat bacterial and parasitic diseases. The discovery in 1989 of a bicyclic nitroimidazole…”
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Revisiting the role of dihydroorotate dehydrogenase as a therapeutic target for cancer by Madak, Joseph T., Bankhead, Armand, Cuthbertson, Christine R., Showalter, Hollis D., Neamati, Nouri

“…Identified as a hallmark of cancer, metabolic reprogramming allows cancer cells to rapidly proliferate, resist chemotherapies, invade, metastasize, and survive…”
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Lipid storage disorders block lysosomal trafficking by inhibiting a TRP channel and lysosomal calcium release by Shen, Dongbiao, Wang, Xiang, Li, Xinran, Zhang, Xiaoli, Yao, Zepeng, Dibble, Shannon, Dong, Xian-ping, Yu, Ting, Lieberman, Andrew P., Showalter, Hollis D., Xu, Haoxing

“…Lysosomal lipid accumulation, defects in membrane trafficking and altered Ca 2+ homoeostasis are common features in many lysosomal storage diseases. Mucolipin…”
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Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia by Grembecka, Jolanta, He, Shihan, Shi, Aibin, Purohit, Trupta, Muntean, Andrew G, Sorenson, Roderick J, Showalter, Hollis D, Murai, Marcelo J, Belcher, Amalia M, Hartley, Thomas, Hess, Jay L, Cierpicki, Tomasz

“…MLL fusion genes often encode leukemogenic proteins that depend on interaction with menin, a component of the MLL SET1-like histone methyltransferase complex…”
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A concise synthesis of 3-substituted-7-amino-6-carboxyl-8-azachromones by Gan, Xinmin, Showalter, Hollis D.

“…[Display omitted] •Amlexanox is an approved drug currently under clinical evaluation to treat obesity.•A concise synthesis of truncated analogues…”
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Rifamycins – Obstacles and opportunities by Aristoff, Paul A, Garcia, George A, Kirchhoff, Paul D, Hollis Showalter, H.D

“…Summary With nearly one-third of the global population infected by Mycobacterium tuberculosis , TB remains a major cause of death (1.7 million in 2006). TB is…”
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Progress in the Synthesis of Canthine Alkaloids and Ring-Truncated Congeners by Showalter, H. D. Hollis

“…The canthines represent a fairly large subclass of β-carboline alkaloids, with the first members described 75 years ago. Over the last 60 years, many members…”
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Design, Synthesis, and Characterization of Brequinar Conjugates as Probes to Study DHODH Inhibition by Madak, Joseph T., Cuthbertson, Christine R., Chen, Wenmin, Showalter, Hollis D., Neamati, Nouri

“…Brequinar, a potent dihydroorotate dehydrogenase (DHODH) inhibitor, has been evaluated in multiple clinical trials as a potential treatment for cancer. To…”
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Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies by Peterson, Luke F., Sun, Hanshi, Liu, Yihong, Potu, Harish, Kandarpa, Malathi, Ermann, Monika, Courtney, Stephen M., Young, Matthew, Showalter, Hollis D., Sun, Duxin, Jakubowiak, Andrzej, Malek, Sami N., Talpaz, Moshe, Donato, Nicholas J.

“…Usp9x was recently shown to be highly expressed in myeloma patients with short progression-free survival and is proposed to enhance stability of the survival…”
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Antiviral activity of a small molecule deubiquitinase inhibitor occurs via induction of the unfolded protein response by Perry, Jeffrey W, Ahmed, Mohammad, Chang, Kyeong-Ok, Donato, Nicholas J, Showalter, Hollis D, Wobus, Christiane E

“…Ubiquitin (Ub) is a vital regulatory component in various cellular processes, including cellular responses to viral infection. As obligate intracellular…”
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Design, Synthesis, and Biological Evaluation of 4‑Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase by Madak, Joseph T, Cuthbertson, Christine R, Miyata, Yoshinari, Tamura, Shuzo, Petrunak, Elyse M, Stuckey, Jeanne A, Han, Yanyan, He, Miao, Sun, Duxin, Showalter, Hollis D, Neamati, Nouri

“…We pursued a structure-guided approach toward the development of improved dihydroorotate dehydrogenase (DHODH) inhibitors with the goal of forming new…”
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A novel synthesis of substituted 3‐amino and 3‐thio pyrimido[5,4‐e]‐1,2,4‐triazine‐5,7(1H,6H)‐diones by Xu, Hao, Powelson, Ian A., Jin, Yafei, Showalter, Hollis D.

“…Fervenulin is a natural product that has been extensively studied due to its molecular features and breadth of biological activities. Published studies have…”
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Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKK ε and Reveal Mechanisms for Selective Inhibition by Beyett, Tyler S, Gan, Xinmin, Reilly, Shannon M, Chang, Louise, Gomez, Andrew V, Saltiel, Alan R, Showalter, Hollis D, Tesmer, John J G

“…Chronic low-grade inflammation is a hallmark of obesity, which is a risk factor for the development of type 2 diabetes. The drug amlexanox inhibits I B kinase…”
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Chemical derivatives of a small molecule deubiquitinase inhibitor have antiviral activity against several RNA viruses by Gonzalez-Hernandez, Marta J, Pal, Anupama, Gyan, Kofi E, Charbonneau, Marie-Eve, Showalter, Hollis D, Donato, Nicholas J, O'Riordan, Mary, Wobus, Christiane E

“…Most antiviral treatment options target the invading pathogen and unavoidably encounter loss of efficacy as the pathogen mutates to overcome replication…”
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RecO and RecR Are Necessary for RecA Loading in Response to DNA Damage and Replication Fork Stress by Lenhart, Justin S, Brandes, Eileen R, Schroeder, Jeremy W, Sorenson, Roderick J, Showalter, Hollis D, Simmons, Lyle A

“…RecA is central to maintaining genome integrity in bacterial cells. Despite the near-ubiquitous conservation of RecA in eubacteria, the pathways that…”
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Synthesis of azide congeners of preQ1 as potential substrates for tRNA guanine transglycosylase by Brooks, Allen F., Garcia, George A., Showalter, Hollis D.

“…PreQ1 (2) is a precursor of queuine (1) that in eubacteria is incorporated into transfer RNA (tRNA) by tRNA guanine transglycosylase (TGT) before being further…”
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Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity by Beyett, Tyler S., Gan, Xinmin, Reilly, Shannon M., Gomez, Andrew V., Chang, Louise, Tesmer, John J.G., Saltiel, Alan R., Showalter, Hollis D.

“…[Display omitted] The non-canonical IκB kinases TANK-binding kinase 1 (TBK1) and inhibitor of nuclear factor kappa-B kinase ε (IKKε) play a key role in…”
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Direct and Systemic Administration of a CNS-Permeant Tamoxifen Analog Reduces Amphetamine-Induced Dopamine Release and Reinforcing Effects by Carpenter, Colleen, Zestos, Alexander G, Altshuler, Rachel, Sorenson, Roderick J, Guptaroy, Bipasha, Showalter, Hollis D, Kennedy, Robert T, Jutkiewicz, Emily, Gnegy, Margaret E

“…Amphetamines (AMPHs) are globally abused. With no effective treatment for AMPH addiction to date, there is urgent need for the identification of druggable…”
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Altered Domain Structure of the Prion Protein Caused by Cu2+ Binding and Functionally Relevant Mutations: Analysis by Cross-Linking, MS/MS, and NMR by McDonald, Alex J., Leon, Deborah R., Markham, Kathleen A., Wu, Bei, Heckendorf, Christian F., Schilling, Kevin, Showalter, Hollis D., Andrews, Philip C., McComb, Mark E., Pushie, M. Jake, Costello, Catherine E., Millhauser, Glenn L., Harris, David A.

“…The cellular isoform of the prion protein (PrPC) serves as precursor to the infectious isoform (PrPSc), and as a cell-surface receptor, which binds misfolded…”
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Synthesis of CID-cleavable protein crosslinking agents containing quaternary amines for structural mass spectrometry by Hagen, Susan E, Liu, Kun, Jin, Yafei, Piersimoni, Lolita, Andrews, Philip C, Showalter, Hollis D

“…Two novel cyclic quaternary amine crosslinking probes are synthesized for structural mass spectrometry of protein complexes in solution and for analysis of…”
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