Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Simon J. Shaw"'
Autor:
Ana M. Cruz, Katie M. Partridge, Yasaman Malekizadeh, Julia M. Vlachaki Walker, Paul G. Weightman Potter, Katherine R. Pye, Simon J. Shaw, Kate L. J. Ellacott, Craig Beall
Publikováno v:
Frontiers in Endocrinology, Vol 12 (2021)
AimWe evaluated the efficacy of a novel brain permeable “metformin-like” AMP-activated protein kinase activator, R481, in regulating glucose homeostasis.Materials and MethodsWe used glucose sensing hypothalamic GT1-7 neuronal cells and pancreatic
Externí odkaz:
https://doaj.org/article/f44879889ae04371b5abf856270d301a
Autor:
Simon J. Shaw, Dane A. Goff, David C. Carroll, Rajinder Singh, David J. Sweeny, Gary Park, Yonchu Jenkins, Vadim Markovtsov, Tian-Qiang Sun, Sarkiz D. Issakani, Yasumichi Hitoshi, Donald G. Payan
Publikováno v:
Bioorganicmedicinal chemistry. 71
Using an in-cell AMPK activation assay, we have developed structure-activity relationships around a hit pyridine dicarboxamide 5 that resulted in 40 (R419). A particular focus was to retain the on-target potency while also improving microsomal stabil
Autor:
Yan Yan, Joseph S. Brunzelle, Y. Li, X.E. Zhou, Patrick R. Griffin, Karsten Melcher, Y. Hitoshi, H.E. Xu, Simon J. Shaw, Scott J. Novick
Publikováno v:
Journal of Biological Chemistry. 294:953-967
AMP-activated protein kinase (AMPK) is an attractive therapeutic target for managing metabolic diseases. A class of pharmacological activators, including Merck 991, binds the AMPK ADaM site, which forms the interaction surface between the kinase doma
Autor:
Bruce E. Kemp, Emily A. Day, Logan K Townsend, David C. Wright, Gregory R. Steinberg, Hesham Shamshoum, Alyssa J. Weber, Christopher G. R. Perry, Simon J. Shaw
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 intake. GDF15 expression and secretion are thought to be regulated by a cellular integrated s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c446c4d28df1f838cdac7d24f5e24da7
https://acuresearchbank.acu.edu.au/item/8w43z/ampk-mediates-energetic-stress-induced-liver-gdf15
https://acuresearchbank.acu.edu.au/item/8w43z/ampk-mediates-energetic-stress-induced-liver-gdf15
Autor:
Wei Li, John McLaughlin, Donald G. Payan, Rajinder Singh, Nan Lin, Simon J. Shaw, Kristen A. Baltgalvis, Todd Kinsella, Dane Goff
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2617-2621
A structure-activity relationship has been developed around the meridianin scaffold for inhibition of Dyrk1a. The compounds have been focussed on the inhibition of kinase Dyrk1a, as a means to retain the transcription factor NFAT in the nucleus. NFAT
Publikováno v:
Tetrahedron Letters. 66:152764
A Noyori reduction of racemic 1-Boc-3-fluoropiperidin-4-one has been achieved under dynamic kinetic resolution conditions that results in a single cis enantiomer being obtained with both diastereo- and enantioselectivity > 90%. This medicinal chemist
Autor:
David C. Carroll, Xiulan Zhou, John McLaughlin, Julie Sheung, Rajinder Singh, Sarkiz D. Issakani, Simon J. Shaw, Lyuben Tsvetkov, Arvinder Sran, Donald G. Payan, Jianing Huang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5199-5202
Structure-activity relationships have been developed around 5-bromo-8-toluylsulfonamidoquinoline 1 a hit compound in an assay for the interaction of the E3 ligase Skp2 with Cks1, part of the SCF ligase complex. Disruption of this protein-protein inte
Publikováno v:
The Journal of Organic Chemistry. 78:8892-8897
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. An enantioselective fluorination is employed, taking advantage of the methodology reported
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:7651-7658
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. The compounds were developed for potency without showing antibacterial activity and inhibition o
Autor:
Yong Li, Yuan Xu, Jessica Simmons, Zong-Qiang Tian, Ziyang Zhong, Leandro Vetcher, Leonard Katz, Simon J. Shaw, Chau Q. Tran, David C. Myles, Zhan Wang
Publikováno v:
ChemMedChem. 3:963-969
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 can be alkylated through reductive amination without loss of potency. However, if it is conve