FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity

Autor: Vivette D. D'Agati, Gabriel Garcia, Enrico Gratton, Luciano Adorini, Suman Ranjit, Komuraiah Myakala, Michal Herman-Edelstein, Moshe Levi, David J. Orlicky, Yingqiong Peng, Mark Pruzanski, Jonathan Levi, Kristopher W. Krausz, Liru Qiu, Frank J. Gonzalez, Xiaoxin X. Wang, Amanda Field, Scott Lucia, Jeffrey B. Kopp, Dong Wang, Alexander Dvornikov, Yuhuan Luo, Avi Z. Rosenberg, Cen Xie, Tao Jiang, Ashley Hill, Kammi J. Henriksen, Evgenia Dobrinskikh

Publikováno v: Journal of the American Society of Nephrology. 29:118-137

Bile acids are ligands for the nuclear hormone receptor farnesoid X receptor (FXR) and the G protein–coupled receptor TGR5. We have shown that FXR and TGR5 have renoprotective roles in diabetes- and obesity-related kidney disease. Here, we determin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82e84829995ee34f946c2f3eebc0f6a2
https://doi.org/10.1681/asn.2017020222

US immigration order strikes against biotech

Autor: Robert Langer, John M. Maraganore, David P. Schenkein, Neil Warma, Chris Adams, Chip Clark, Mark Levin, William Rastetter, Bruce A Leicher, Nancy A Thornberry, Robert I Blum, Jonathan G Rosin, Kleanthis G Xanthopoulos, Timothy D. Harris, Jeff L Cleland, Robert Forrester, Nancy Simonian, Peter Barrett, Stephen Bloch, William J Rieflin, Brian M Gallagher, Lewis Rusty Williams, Doug Doerfler, Richard Ulevitch, David R. Liu, Andrew Levin, P. Grint, Nick J Simon, Pablo J Cagnoni, Daphne Zohar, Kush M Parmar, Guy Macdonald, Corey M McCann, Stelios Papadopoulos, Michael D Clayman, Diego Miralles, Paula Cobb, John Diekman, Jeremy M Levin, Amir Nashat, Samuel G Waksal, Rachel King, Sandford Sandy Zweifach, Gail J Maderis, Ankit Mahadevia, Heather Franklin, Cary G Pfeffer, Steven K Brauer, Akshay Vaishnaw, Clay B. Siegall, Howard Furst, Jonathan S Leff, William J Rutter, Dennis J. Purcell, Mary T Szela, J C Gutierrez-Ramos, Sean A McCarthy, Elizabeth Lr Donley, Yaron Werber, Doug E Williams, Christoph Westphal, Paul Sekhri, W Eddie Martucci, Jeb Keiper, John E Osborn, Simba Gill, Bassil Dahiyat, Steven H Holtzman, Annalisa Jenkins, Saurabh Saha, Matthew J. During, Camille Samuels, Mara G Aspinall, Chad Robins, Jason P Rhodes, Herve Hoppenot, Jeff Kaplan, Michael A Narachi, Amit Rakhit, Julia C Owens, Steve M Paul, Martin Varsavsky, Mark G. Currie, Rajeev Shah, Rob Perez, H. Stewart Parker, Jeff Stein, Leonard Patrick Gage, Perry Karsen, Joel F Martin, Bob More, Matthew Perry, James G McArthur, Gregory J Flesher, Martin Tolar, Andrew Schwab, James A Geraghty, Eric L Dobmeier, Brook Byers, Vanessa King, Mason W. Freeman, Larry Miller, Marco Taglietti, Jeff Albers, Neil A Exter, Michael W Bonney, Ron Cohen, Nick Leschly, Bruce L Booth, William J Newell, Peter Kolchinsky, Ryan J Watts, Paul Laikind, Andrew G. Myers, Cedric Francois, Stephen T Isaacs, Scott Koenig, Michel Vounatsos, Tuan Ha-Ngoc, Nicholas Galakatos, George P Vlasuk, Isaac Ciechanover, Jeff Kindler, Brian M. Cali, Matthew R Patterson, Kenneth I Moch, Tom Graney, Martin Babler, Jonathan J Fleming, Mark A Goldsmith, Daniel M Bradbury, John Mendlein, Mike Powell, Nessan Bermingham, Eric Elenko, H. Robert Horvitz, Yujiro Steve Hata, Mark Pruzanski, Faheem Hasnain, Henri A. Termeer, Maxine Gowen, Scott M Rocklage, Anne VanLent, Thomas Shenk, Leslie Henshaw, Jeff Jonker, Nina Kjellson, Deborah Dunsire, Zoe Barry, Ron C Renaud, Alex Martin, Uri Lopatin, George Scangos, Jean Kim, Kartik Ramamoorthi, Michael Rosenblatt, Nagesh K Mahanthappa, Harvey F. Lodish, Paul B Bolno, Wendell Wierenga, Atul Pande, Barry Greene, Alan Levy, Adrian Ad Rawcliffe, Wende S Hutton, C Geoffrey McDonough, Vicki L. Sato, Jean-Francois Formela, David V. Goeddel, Bill Haney, Rich Heyman, James E Audia, Ron Cooper, Nina Tandon, Brett Ahrens, Julian Adams, Peter Hecht, John J Lee, Stuart L. Schreiber, Laurence E Reid, Bernat Olle, Paul Hastings, John A. Scarlett, Michael Su, David Grayzel, Ted W Love, Arnold J. Levine, Gerhard Koenig, Thomas E Hughes, Jens W Eckstein, Wendy Nelson, Vikas Goyal

Publikováno v: Nature Biotechnology. 35:204-206

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee2d10770c0eb9d17bb770366663a693
https://doi.org/10.1038/nbt.3824

Probing the Binding Site of Bile Acids in TGR5

Autor: Roberto Pellicciari, Johan Auwerx, Nicola Giacchè, Antimo Gioiello, Kristina Schoonjans, Charles Thomas, Cristina Ferrari, Roberto Nuti, Francesca De Franco, Antonio Macchiarulo, Thijs W.H. Pols, Mark Pruzanski

Publikováno v: ACS medicinal chemistry letters

TGR5 is a G-protein-coupled receptor (GPCR) mediating cellular responses to bile acids (BAs). Although some efforts have been devoted to generate homology models of TGR5 and draw structure-activity relationships of BAs, none of these studies has hith

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4cdf9eb9b27922009c13da8f126e7fd
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027510/

Discovery of 6α-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity

Autor: Antonio Macchiarulo, Aldo Roda, Mark Pruzanski, Roccaldo Sardella, Charles Thomas, Antimo Gioiello, Roberto Pellicciari, Johan Auwerx, Elisabetta Pastorini, Benedetto Natalini, Kristina Schoonjans, Emiliano Rosatelli

Publikováno v: Journal of medicinal chemistry

In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) aff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e2a31c893dd9d320fedb2d663fdd282
https://doi.org/10.1021/jm901390p

A Farnesoid X Receptor-Small Heterodimer Partner Regulatory Cascade Modulates Tissue Metalloproteinase Inhibitor-1 and Matrix Metalloprotease Expression in Hepatic Stellate Cells and Promotes Resolution of Liver Fibrosis

Autor: Barbara Renga, Antonio Morelli, Andrea Mencarelli, Stefano Orlandi, Mark Pruzanski, Luisa Riccardi, Elisabetta Antonelli, Giovanni Rizzo, Stefano Fiorucci, Roberto Pellicciari

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 314:584-595

The farnesoid X receptor (FXR) is expressed by and regulates hepatic stellate cells (HSCs). In the present study, we investigated whether 6-ethyl chenodeoxycholic acid (6-ECDCA or INT-747), a semisynthetic derivative of chenodeoxycholic acid (CDCA),

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dd968f22701c6d8007159d703ceddce
https://doi.org/10.1124/jpet.105.084905