Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Glenn Sivits"'
Autor:
Elizabeth A. Killion, Michelle Chen, James R. Falsey, Glenn Sivits, Todd Hager, Larissa Atangan, Joan Helmering, Jae Lee, Hongyan Li, Bin Wu, Yuan Cheng, Murielle M. Véniant, David J. Lloyd
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-17 (2020)
Both agonism and antagonism of the glucose-dependent insulinotropic polypeptide receptor (GIPR) lead to weight loss in combination with glucagon-like peptide-1 receptor agonists in preclinical models. Here the authors show that this may be explained
Externí odkaz:
https://doaj.org/article/35bda07550384ea78b2522ff1a815550
Autor:
Todd Hager, Jae Lee, Hongyan Li, David Lloyd, James R. Falsey, Elizabeth A. Killion, Bin Wu, Larissa Atangan, Yuan Cheng, Michelle Chen, Murielle M. Véniant, Joan Helmering, Glenn Sivits
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-17 (2020)
Nature Communications
Nature Communications
Antagonism or agonism of the glucose-dependent insulinotropic polypeptide (GIP) receptor (GIPR) prevents weight gain and leads to dramatic weight loss in combination with glucagon-like peptide-1 receptor agonists in preclinical models. Based on the g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e345ea930fa8a2a065b4ce5c63e709e9
http://link.springer.com/article/10.1038/s41467-020-18751-8
http://link.springer.com/article/10.1038/s41467-020-18751-8
Autor:
Brandon C. P. Clavette, Xiaoshan Min, Joanne Lin, Elizabeth A. Killion, Robert J.M. Kurzeja, David Lloyd, Liying Deng, Zhulun Wang, Clarence Hale, Christopher Murawsky, Stone D.-H. Shi, Murielle M. Véniant, Jinghong Wang, James B. Rottman, Christina Abbott, Todd Hager, Lu Shu Chen, Junming Yie, Ian Foltz, Qing Chen, Stephen A. Thibault, Darren L. Bates, Renee Komorowski, Larissa Atangan, Glenn Sivits, Tina Meng
Publikováno v:
Science Translational Medicine. 10
Glucose-dependent insulinotropic polypeptide (GIP) receptor (GIPR) has been identified in multiple genome-wide association studies (GWAS) as a contributor to obesity, and GIPR knockout mice are protected against diet-induced obesity (DIO). On the bas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4219a5cd6927493203264b2541e2f88b
https://doi.org/10.1126/scitranslmed.aat3392
https://doi.org/10.1126/scitranslmed.aat3392
Autor:
Michael D. Bartberger, Michael Croghan, Carolyn Moyer, David Lloyd, Rod Cupples, Seifu Tadesse, Nobuko Nishimura, Ke Kong, Gwyneth Van, Christopher H. Fotsch, Randall W. Hungate, David J. St. Jean, Kevin Yang, Kate Ashton, Mark H. Norman, Samer Chmait, Longbin Liu, Lewis D. Pennington, Fang-Tsao Hong, Matthew P. Bourbeau, Clarence Hale, Jiandong Zhang, Aaron C. Siegmund, Jie Chen, Christopher M. Tegley, Steven R. Jordan, Kristin L. Andrews, Klaus Michelsen, Guomin Yao, Glenn Sivits, Andreas Reichelt, Joan Helmering
Publikováno v:
Journal of Medicinal Chemistry. 58:9663-9679
The HTS-based discovery and structure-guided optimization of a novel series of GKRP-selective GK-GKRP disrupters are revealed. Diarylmethanesulfonamide hit 6 (hGK-hGKRP IC50 = 1.2 μM) was optimized to lead compound 32 (AMG-0696; hGK-hGKRP IC50 = 0.0
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c946578bf834df571e0f47d51f90f41
https://doi.org/10.1021/acs.jmedchem.5b01367
https://doi.org/10.1021/acs.jmedchem.5b01367
Autor:
Kevin Yang, Rod Cupples, Gwyneth Van, Nobuko Nishimura, Longbin Liu, David J. St. Jean, Clarence Hale, Glenn Sivits, Jie Chen, Nuria A. Tamayo, Steven R. Jordan, Fang-Tsao Hong, Mark H. Norman, Michael D. Bartberger, Yunxin Bo, Christopher H. Fotsch, Samer Chmait, Seifu Tadesse, David Lloyd
Publikováno v:
Journal of Medicinal Chemistry. 58:4462-4482
The glucokinase-glucokinase regulatory protein (GK-GKRP) complex plays an important role in controlling glucose homeostasis in the liver. We have recently disclosed a series of arylpiperazines as in vitro and in vivo disruptors of the GK-GKRP complex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0067ff276fb22038ac064d47a32d35c8
https://doi.org/10.1021/jm5018175
https://doi.org/10.1021/jm5018175
Autor:
Kate S, Ashton, Kristin L, Andrews, Marian C, Bryan, Marion C, Bryan, Jie, Chen, Kui, Chen, Michelle, Chen, Samer, Chmait, Michael, Croghan, Rod, Cupples, Christopher, Fotsch, Joan, Helmering, Steve R, Jordan, Robert J M, Kurzeja, Klaus, Michelsen, Lewis D, Pennington, Steve F, Poon, Glenn, Sivits, Gwyneth, Van, Steve L, Vonderfecht, Robert C, Wahl, Jiandong, Zhang, David J, Lloyd, Clarence, Hale, David J, St Jean
Publikováno v:
Journal of Medicinal Chemistry. 57:309-324
Small molecule activators of glucokinase have shown robust efficacy in both preclinical models and humans. However, overactivation of glucokinase (GK) can cause excessive glucose turnover, leading to hypoglycemia. To circumvent this adverse side effe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::688eef24bebd019f68813ef22be87641
https://doi.org/10.1021/jm4016735
https://doi.org/10.1021/jm4016735
Autor:
Murielle M. Véniant, Jin-Long Chen, Clarence Hale, Richard A. Lindberg, Jing Xu, Zhiyou Zhang, Steven Vonderfecht, Glenn Sivits, Randy Ira Hecht, Yue-Sheng Li, Dae Young Jung, Shanaka Stanislaus, Hwi Jin Ko, Jason K. Kim, David Lloyd, Michelle Chen
Publikováno v:
Diabetes
OBJECTIVE—Fibroblast growth factor 21 (FGF21) has emerged as an important metabolic regulator of glucose and lipid metabolism. The aims of the current study are to evaluate the role of FGF21 in energy metabolism and to provide mechanistic insights
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18d223cd5ccdfcc94dd9132dbdfb095d
http://europepmc.org/articles/PMC2606881
http://europepmc.org/articles/PMC2606881
Autor:
Wei Fan, Jae Lee, David Lloyd, Murielle M. Véniant, Carolyn Moyer, Renee Komorowski, Glenn Sivits, Joan Helmering
Publikováno v:
Cell metabolism. 21(5)
Summary "Browning," the appearance and activation of brown-in-white (brite) adipose cells within inguinal white adipose tissue (iWAT), and induction of uncoupling protein 1 (UCP1) correlate with fibroblast growth factor-21 (FGF21)-induced weight loss
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb333b02a1e5b4ddca3aaa8261a6cb02
https://pubmed.ncbi.nlm.nih.gov/26039444
https://pubmed.ncbi.nlm.nih.gov/26039444
Autor:
Mark H. Norman, Nobuko Nishimura, Samer Chmait, Rod Cupples, Kate Ashton, Roxanne Kunz, Joan Helmering, Aaron C. Siegmund, David J. St. Jean, Clarence Hale, David Lloyd, Steven R. Jordan, Glenn Sivits, Michael D. Bartberger, Christopher H. Fotsch, Kevin Yang, Steve F. Poon, Lewis D. Pennington, Longbin Liu, Jie Chen
Publikováno v:
Journal of medicinal chemistry. 57(7)
We have recently reported a novel approach to increase cytosolic glucokinase (GK) levels through the binding of a small molecule to its endogenous inhibitor, glucokinase regulatory protein (GKRP). These initial investigations culminated in the identi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef9e58eb1815a689eef7dd774dd416f8
https://pubmed.ncbi.nlm.nih.gov/24611879
https://pubmed.ncbi.nlm.nih.gov/24611879
Autor:
Joan Helmering, Fang-Tsao Hong, Mark H. Norman, Jiandong Zhang, Klaus Michelsen, Markian Stec, Nobuko Nishimura, Steven R. Jordan, Lewis D. Pennington, Rod Cupples, David J. St. Jean, Darren L. Reid, Clarence Hale, Gwyneth Van, Jie Chen, Seifu Tadesse, Roxanne Kunz, Nuria A. Tamayo, Steve F. Poon, Kevin Yang, Christopher H. Fotsch, Longbin Liu, David Lloyd, Glenn Sivits, Elizabeth J. Galbreath, Michael D. Bartberger, Kate Ashton, Samer Chmait
Publikováno v:
Journal of medicinal chemistry. 57(2)
In the previous report , we described the discovery and optimization of novel small molecule disruptors of the GK-GKRP interaction culminating in the identification of 1 (AMG-1694). Although this analogue possessed excellent in vitro potency and was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4d2a8943c3198375b234ab664a4fed0
https://pubmed.ncbi.nlm.nih.gov/24405213
https://pubmed.ncbi.nlm.nih.gov/24405213