Search Results - "SHAW, Simon J"

Developing structure–activity relationships from an HTS hit for inhibition of the Cks1–Skp2 protein–protein interaction by Singh, Rajinder, Sran, Arvinder, Carroll, David C., Huang, Jianing, Tsvetkov, Lyuben, Zhou, Xiulan, Sheung, Julie, McLaughlin, John, Issakani, Sarkiz D., Payan, Donald G., Shaw, Simon J.

“…[Display omitted] Structure–activity relationships have been developed around 5-bromo-8-toluylsulfonamidoquinoline 1 a hit compound in an assay for the…”
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Brain Permeable AMP-Activated Protein Kinase Activator R481 Raises Glycaemia by Autonomic Nervous System Activation and Amplifies the Counterregulatory Response to Hypoglycaemia in Rats by Cruz, Ana M, Partridge, Katie M, Malekizadeh, Yasaman, Vlachaki Walker, Julia M, Weightman Potter, Paul G, Pye, Katherine R, Shaw, Simon J, Ellacott, Kate L J, Beall, Craig

“…We evaluated the efficacy of a novel brain permeable "metformin-like" AMP-activated protein kinase activator, R481, in regulating glucose homeostasis. We used…”
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Enantioselective Synthesis of cis-3-Fluoropiperidin-4-ol, a Building Block for Medicinal Chemistry by Shaw, Simon J, Goff, Dane A, Boralsky, Luke A, Irving, Mark, Singh, Rajinder

“…The first enantioselective route to both enantiomers of cis-1-Boc-3-fluoropiperidin-4-ol, a highly prized building block for medicinal chemistry, is reported…”
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Looking Beyond the Surface: Olutasidenib and Ivosidenib for Treatment of mIDH1 Acute Myeloid Leukemia by Watts, Justin M., Shaw, Simon J., Jonas, Brian A.

“…Opinion Statement Mutations in isocitrate dehydrogenase-1 ( IDH1) are recurrent in several malignancies and prevalent in acute myeloid leukemia (AML)…”
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AMPK mediates energetic stress‐induced liver GDF15 by Townsend, Logan K., Weber, Alyssa J., Day, Emily A., Shamshoum, Hesham, Shaw, Simon J., Perry, Christopher G. R., Kemp, Bruce E., Steinberg, Gregory R., Wright, David C.

“…Growth differentiating factor‐15 (GDF15) is an emerging target for the treatment of obesity and metabolic disease partly due to its ability to suppress food…”
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Optimization of Pharmacokinetic and In Vitro Safety Profile of a Series of Pyridine Diamide Indirect AMPK Activators by Shaw, Simon J., Goff, Dane A., Boralsky, Luke A., Singh, Rajinder, Sweeny, David J., Park, Gary, Sun, Tian-Qiang, Jenkins, Yonchu, Markovtsov, Vadim, Issakani, Sarkiz D., Payan, Donald G., Hitoshi, Yasumichi

“…A set of focused analogues have been generated around a lead indirect adenosine monophosphate-activated kinase (AMPK) activator to improve the rat clearance of…”
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Structures of AMP-activated protein kinase bound to novel pharmacological activators in phosphorylated, non-phosphorylated, and nucleotide-free states by Yan, Yan, Zhou, X. Edward, Novick, Scott J., Shaw, Simon J., Li, Yingwu, Brunzelle, Joseph S., Hitoshi, Yasumichi, Griffin, Patrick R., Xu, H. Eric, Melcher, Karsten

“…AMP-activated protein kinase (AMPK) is an attractive therapeutic target for managing metabolic diseases. A class of pharmacological activators, including Merck…”
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Structure activity relationships leading to the identification of the indirect activator of AMPK, R419 by Shaw, Simon J., Goff, Dane A., Carroll, David C., Singh, Rajinder, Sweeny, David J., Park, Gary, Jenkins, Yonchu, Markovtsov, Vadim, Sun, Tian-Qiang, Issakani, Sarkiz D., Hitoshi, Yasumichi, Payan, Donald G.

“…[Display omitted] Using an in-cell AMPK activation assay, we have developed structure–activity relationships around a hit pyridine dicarboxamide 5 that…”
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119-OR: Amplified Glucagon Response to Hypoglycemia following AMP-Activated Protein Kinase (AMPK) Activator R481 Treatment in Healthy Rats by CRUZ, ANA M.L., MALEKIZADEH, YASAMAN, VLACHAKI WALKER, JULIA M., SHAW, SIMON J., ELLACOTT, KATE L., BEALL, CRAIG

“…Episodes of insulin-induced hypoglycemia are frequent in type 1 and advanced type 2 diabetes, but pharmaceutical approaches to prevent these are lacking…”
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Tuning the Reactivity of Nuclear Factor Erythroid 2‑Related Factor 2 (Nrf2) Activators for Optimal in Vivo Efficacy by Markovtsov, Vadim, Duncton, Matthew A. J., Bagos, Art, Yi, Sothy, Braselmann, Sylvia, Bhamidipati, Somasekhar, Darwish, Ihab S., Yu, Jiaxin, Owyang, Alexander M., Fernandez, Beth, Samant, Bhushan, Park, Gary, Masuda, Esteban S., Shaw, Simon J.

“…Dimethyl fumarate 1 is approved for the treatment of multiple sclerosis but is also associated with off-target activation of the niacin receptor. By using a…”
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Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus by Shaw, Simon J., Goff, Dane A., Lin, Nan, Singh, Rajinder, Li, Wei, McLaughlin, John, Baltgalvis, Kristen A., Payan, Donald G., Kinsella, Todd M.

“…[Display omitted] A structure-activity relationship has been developed around the meridianin scaffold for inhibition of Dyrk1a. The compounds have been…”
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Investigating Carboxylic Acid Analogues of Ambruticin through Semi-Synthesis by Xu, Yuan, Wang, Zhan, Tian, Zong-Qiang, Li, Yong, Shaw, Simon J.

“…Systemic fungal infections have increased significantly in recent years and this is important particularly for immunocompromised patients. A series of…”
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The structure activity relationship of discodermolide analogues by Shaw, Simon J

“…The marine polyketide discodermolide is a member of a class of natural products that stabilize microtubules. Many analogues have been synthesized suggesting…”
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Exercise performance and peripheral vascular insufficiency improve with AMPK activation in high-fat diet-fed mice by Baltgalvis, Kristen A, White, Kathy, Li, Wei, Claypool, Mark D, Lang, Wayne, Alcantara, Raniel, Singh, Baljit K, Friera, Annabelle M, McLaughlin, John, Hansen, Derek, McCaughey, Kelly, Nguyen, Henry, Smith, Ira J, Godinez, Guillermo, Shaw, Simon J, Goff, Dane, Singh, Rajinder, Markovtsov, Vadim, Sun, Tian-Qiang, Jenkins, Yonchu, Uy, Gerald, Li, Yingwu, Pan, Alison, Gururaja, Tarikere, Lau, David, Park, Gary, Hitoshi, Yasumichi, Payan, Donald G, Kinsella, Todd M

“…Intermittent claudication is a form of exercise intolerance characterized by muscle pain during walking in patients with peripheral artery disease (PAD)…”
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Investigating Amine Derivatives of Ambruticin VS-5 and VS-4 by Tian, Zong-Qiang, Wang, Zhan, Xu, Yuan, Tran, Chau Q., Myles, David C., Zhong, Ziyang, Simmons, Jessica, Vetcher, Leandro, Katz, Leonard, Li, Yong, Shaw, Simon J.

“…A structure–activity relationship around the amine group of the ambruticin VS series has been developed for antifungal activity. It was shown that the amine…”
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AMPK activation through mitochondrial regulation results in increased substrate oxidation and improved metabolic parameters in models of diabetes by Jenkins, Yonchu, Sun, Tian-Qiang, Markovtsov, Vadim, Foretz, Marc, Li, Wei, Nguyen, Henry, Li, Yingwu, Pan, Alison, Uy, Gerald, Gross, Lisa, Baltgalvis, Kristen, Yung, Stephanie L, Gururaja, Tarikere, Kinoshita, Taisei, Owyang, Alexander, Smith, Ira J, McCaughey, Kelly, White, Kathy, Godinez, Guillermo, Alcantara, Raniel, Choy, Carmen, Ren, Hong, Basile, Rachel, Sweeny, David J, Xu, Xiang, Issakani, Sarkiz D, Carroll, David C, Goff, Dane A, Shaw, Simon J, Singh, Rajinder, Boros, Laszlo G, Laplante, Marc-André, Marcotte, Bruno, Kohen, Rita, Viollet, Benoit, Marette, André, Payan, Donald G, Kinsella, Todd M, Hitoshi, Yasumichi

“…Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein…”
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15-amido erythromycins: synthesis and in vitro activity of a new class of macrolide antibiotics by Shaw, Simon J, Abbanat, Darren, Ashley, Gary W, Bush, Karen, Foleno, Barbara, Macielag, Mark, Zhang, Dan, Myles, David C

“…An array of 15-amido substituted erythromycin A compounds was synthesized using a chemobiosynthesis approach. It was found that while the in vitro…”
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Global metabolite profiling of mice with high-fat diet-induced obesity chronically treated with AMPK activators R118 or metformin reveals tissue-selective alterations in metabolic pathways by Jenkins, Yonchu, Sun, Tian-Qiang, Li, Yingwu, Markovtsov, Vadim, Uy, Gerald, Gross, Lisa, Goff, Dane A, Shaw, Simon J, Boralsky, Luke, Singh, Rajinder, Payan, Donald G, Hitoshi, Yasumichi

“…The novel small molecule R118 and the biguanide metformin, a first-line therapy for type 2 diabetes (T2D), both activate the critical cellular energy sensor…”
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The role of the 4′′-hydroxyl on motilin agonist potency in the 9-dihydroerythromycin series by Liu, Yaoquan, Carreras, Christopher W., Claypool, Mark, Myles, David C., Shaw, Simon J.

“…The role of the erythromycin 4′′-hydroxyl group has been explored on the motilin agonist potential in the 9-dihydroerythromycin series of motilides. The…”
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9-Dihydroerythromycin ethers as motilin agonists—Developing structure–activity relationships for potency and safety by Liu, Yaoquan, Li, Yong, Myles, David C., Claypool, Mark, Carreras, Christopher W., Shaw, Simon J.

“…A series of derivatives of the amine of 9-dihydro-9- O-ethylamino- N-desmethyl- N-isopropyl erythromycin A derivatives were synthesized as motilin agonists…”
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