Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction

Autor: Paul A. Barsanti, Joshua Taygerly, Kathleen Boyle, Kyle R. Simonetta, Stephanie L. Yung, Szerenke Kiss von Soly, Chris Padovani, Frank Kayser, Neil Bence, Anjanabha Saha, Stephen E. Basham, John Kuriyan, Mark Gallop, Thomas Cummins, Yan Lou, Michael Rape, Mario G. Cardozo

Publikováno v: Nature Communications, Vol 10, Iss 1, Pp 1-12 (2019)
Nature Communications
Nature communications, vol 10, iss 1
Simonetta, Kyle R; Taygerly, Joshua; Boyle, Kathleen; Basham, Stephen E; Padovani, Chris; Lou, Yan; et al.(2019). Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction.. Nature communications, 10(1), 1402. doi: 10.1038/s41467-019-09358-9. UC Berkeley: Retrieved from: http://www.escholarship.org/uc/item/26s7m3b9

Protein–protein interactions (PPIs) governing the recognition of substrates by E3 ubiquitin ligases are critical to cellular function. There is significant therapeutic potential in the development of small molecules that modulate these interactions

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d19fdea334a0af8bb97cc6bfba60718
https://doaj.org/article/1987a6eabdf140cbaf14746bd1ee3135

A Potent and Highly Selective VPAC2 Agonist Enhances Glucose-Induced Insulin Release and Glucose Disposal

Autor: Stephanie L. Yung, Xianbu Peng, Yin Liang, Hongxing Chen, Fernando Dela Cruz, Ling Yang, Clark Pan, Jian Zhu, James N. Livingston, Thomas H. Claus, Sarah Hamren, Manami Tsutsumi, Yaxin Li

Publikováno v: Diabetes. 51:1453-1460

Pituitary adenylate cyclase—activating peptide (PACAP) and vasoactive intestinal peptide (VIP) activate two shared receptors, VPAC1 and VPAC2. Activation of VPAC1 has been implicated in elevating glucose output, whereas activation of VPAC2 may be i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b9e714eb2b8a748916a7d5971e7b4080
https://doi.org/10.2337/diabetes.51.5.1453

Generation of highly selective VPAC2 receptor agonists by high throughput mutagenesis of vasoactive intestinal peptide and pituitary adenylate cyclase-activating peptide

Autor: Margit MacDougall, Stephanie L. Yung, Clark Pan, Tracey Todd, Margaret Caudle, Sarah Hamren, Manami Tsutsumi, Shanafelt Armen B, Lynn Lemoine, Fernando Dela Cruz, Steve Roczniak, Jian Zhu, James W. Bloom

Publikováno v: The Journal of biological chemistry. 278(12)

Pituitary adenylate cyclase-activating peptide (PACAP) has a specific receptor PAC1 and shares two receptors VPAC1 and VPAC2 with vasoactive intestinal peptide (VIP). VPAC2 activation enhances glucose-induced insulin release while VPAC1 activation el

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e217f6c467f048d52651a53b8f11b40c
https://pubmed.ncbi.nlm.nih.gov/12525492

AMPK activation through mitochondrial regulation results in increased substrate oxidation and improved metabolic parameters in models of diabetes.

Autor: Yonchu Jenkins, Tian-Qiang Sun, Vadim Markovtsov, Marc Foretz, Wei Li, Henry Nguyen, Yingwu Li, Alison Pan, Gerald Uy, Lisa Gross, Kristen Baltgalvis, Stephanie L Yung, Tarikere Gururaja, Taisei Kinoshita, Alexander Owyang, Ira J Smith, Kelly McCaughey, Kathy White, Guillermo Godinez, Raniel Alcantara, Carmen Choy, Hong Ren, Rachel Basile, David J Sweeny, Xiang Xu, Sarkiz D Issakani, David C Carroll, Dane A Goff, Simon J Shaw, Rajinder Singh, Laszlo G Boros, Marc-André Laplante, Bruno Marcotte, Rita Kohen, Benoit Viollet, André Marette, Donald G Payan, Todd M Kinsella, Yasumichi Hitoshi

Publikováno v: PLoS ONE, Vol 8, Iss 12, p e81870 (2013)

Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein kinase (AMPK). Activation of AMPK results in the mobilization of nutrient uptake and cataboli

Externí odkaz: https://doaj.org/article/9f3bbe0f39b0498d932c53dbf27c0985