Synthesis of 3,4,5-Trisubstituted-1,2,4-triazoles von Moulin, Aline, Bibian, Mathieu, Blayo, Anne-Laure, El Habnouni, Sarah, Martinez, Jean, Fehrentz, Jean-Alain

Volltext

A structural mechanism for directing corepressor-selective inverse agonism of PPARγ von Brust, Richard, Shang, Jinsai, Fuhrmann, Jakob, Mosure, Sarah A., Bass, Jared, Cano, Andrew, Heidari, Zahra, Chrisman, Ian M., Nemetchek, Michelle D., Blayo, Anne-Laure, Griffin, Patrick R., Kamenecka, Theodore M., Hughes, Travis S., Kojetin, Douglas J.

Volltext

Defining a conformational ensemble that directs activation of PPARγ von Chrisman, Ian M., Nemetchek, Michelle D., de Vera, Ian Mitchelle S., Shang, Jinsai, Heidari, Zahra, Long, Yanan, Reyes-Caballero, Hermes, Galindo-Murillo, Rodrigo, Cheatham, Thomas E., Blayo, Anne-Laure, Shin, Youseung, Fuhrmann, Jakob, Griffin, Patrick R., Kamenecka, Theodore M., Kojetin, Douglas J., Hughes, Travis S.

Volltext

Definition of functionally and structurally distinct repressive states in the nuclear receptor PPARγ von Heidari, Zahra, Chrisman, Ian M., Nemetchek, Michelle D., Novick, Scott J., Blayo, Anne-Laure, Patton, Trey, Mendes, Desiree E., Diaz, Philippe, Kamenecka, Theodore M., Griffin, Patrick R., Hughes, Travis S.

Volltext

PPARγ in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix von Frkic, Rebecca L., Marshall, Andrew C., Blayo, Anne-Laure, Pukala, Tara L., Kamenecka, Theodore M., Griffin, Patrick R., Bruning, John B.

Volltext

Synthesis of Various Chiral 1,2,4-Triazole-Containing α-Amino Acids from Aspartic or Glutamic Acids von Blayo, Anne-Laure, Brunel, Frédéric, Martinez, Jean, Fehrentz, Jean-Alain

Volltext

New Enantioselective Synthesis of Monofluorinated Pyridines Designed for the Preparation of Chemical Libraries von Blayo, Anne-Laure, Le Meur, Stéphanie, Grée, Danielle, Grée, René

Volltext

Chemical Crosslinking Mass Spectrometry Reveals the Conformational Landscape of the Activation Helix of PPARγ; a Model for Ligand-Dependent Antagonism von Zheng, Jie, Corzo, Cesar, Chang, Mi Ra, Shang, Jinsai, Lam, Vinh Q., Brust, Richard, Blayo, Anne-Laure, Bruning, John B., Kamenecka, Theodore M., Kojetin, Douglas J., Griffin, Patrick R.

Volltext

Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold von Haj Salah, Khoubaib Ben, Maingot, Mathieu, Blayo, Anne-Laure, M’Kadmi, Céline, Damian, Marjorie, Mary, Sophie, Cantel, Sonia, Neasta, Jérémie, Oiry, Catherine, Péraldi-Roux, Sylvie, Fernandez, Gimena, Romero, Guadalupe García, Perello, Mario, Marie, Jacky, Banères, Jean-Louis, Fehrentz, Jean-Alain, Denoyelle, Séverine

Volltext

PPARγ Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles von Frkic, Rebecca L., Pederick, Jordan L., Horsfall, Aimee J., Jovcevski, Blagojce, Crame, Elise E., Kowalczyk, Wioleta, Pukala, Tara L., Chang, Mi Ra, Zheng, Jie, Blayo, Anne-Laure, Abell, Andrew D., Kamenecka, Theodore M., Harbort, Joshua S., Harmer, Jeffrey R., Griffin, Patrick R, Bruning, John B.

Volltext

Multi-gram scale mercury-free synthesis of optically pure 3,4,5-trisubstituted 1,2,4-triazoles using silver benzoate von Bibian, Mathieu, Blayo, Anne-Laure, Moulin, Aline, Martinez, Jean, Fehrentz, Jean-Alain

Volltext

New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center von Maingot, Mathieu, Blayo, Anne-Laure, Denoyelle, Séverine, M’Kadmi, Céline, Damian, Marjorie, Mary, Sophie, Gagne, Didier, Sanchez, Pierre, Aicher, Babette, Schmidt, Peter, Müller, Gilbert, Teifel, Michael, Günther, Eckhard, Marie, Jacky, Banères, Jean-Louis, Martinez, Jean, Fehrentz, Jean-Alain

Volltext

Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists von Asteian, Alice, Blayo, Anne-Laure, He, Yuanjun, Koenig, Marcel, Shin, Youseung, Kuruvilla, Dana S, Corzo, Cesar A, Cameron, Michael D, Lin, Li, Ruiz, Claudia, Khan, Susan, Kumar, Naresh, Busby, Scott, Marciano, David P, Garcia-Ordonez, Ruben D, Griffin, Patrick R, Kamenecka, Theodore M

Volltext

New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists von Blayo, Anne-Laure, Maingot, Mathieu, Aicher, Babette, M’Kadmi, Céline, Schmidt, Peter, Müller, Gilbert, Teifel, Michael, Günther, Eckhard, Gagne, Didier, Denoyelle, Séverine, Martinez, Jean, Fehrentz, Jean-Alain

Volltext

817 DT095895, a selective EP4 receptor antagonist with monotherapy efficacy in syngeneic mouse model(s) and best-in-class properties von Blayo, Anne-Laure, Deshons, Laurène, Dumont, Alexia, Franchet, Christel, Halter, Célia, Herbin, Ludovic, Hommet, Gaël, Mayer, Stanislas, Bessede, Alban, Nafia, Imane, Sidhoum, Marjorie, Leroy, Xavier, Schann, Stéphan

Volltext

An alternate binding site for PPARγ ligands von Hughes, Travis S., Giri, Pankaj Kumar, de Vera, Ian Mitchelle S., Marciano, David P., Kuruvilla, Dana S., Shin, Youseung, Blayo, Anne-Laure, Kamenecka, Theodore M., Burris, Thomas P., Griffin, Patrick R., Kojetin, Douglas J.

Volltext

Abstract 934: “GPCR-ome” modulation upon PD1 / PDL1 axis blockade von Nafia, Imane, Leroy, Xavier, Cerf, Loic, Guegan, Jean-Philippe, Blayo, Anne-Laure, Italiano, Antoine, Schann, Stephan, Bessede, Alban

Volltext

Abstract 6697: DT095895, a selective EP4 receptor antagonist with monotherapy efficacy in syngeneic mouse model(s) and best-in-class properties von Blayo, Anne-Laure, Deshons, Laurène, Dumont, Alexia, Franchet, Christel, Halter, Célia, Herbin, Ludovic, Hommet, Gaël, Mayer, Stanislas, Bessede, Alban, Nafia, Imane, Sidhoum, Marjorie, Leroy, Xavier, Schann, Stephan

Volltext

Development of non-peptidic inverse agonists of the ghrelin receptor (GHSR) based on the 1,2,4-triazole scaffold von Ben Haj Salah, Khoubaib, Maingot, Mathieu, Blayo, Anne-Laure, M'Kadmi, Céline, Damian, Marjorie, Mary, Sophie, Cantel, Sonia, Neasta, Jérémie, Oiry, Catherine, Péraldi-Roux, Sylvie, Fernandez, Gimena, Romero, Guadalupe García, Perello, Mario, Marie, Jacky, Banères, Jean-Louis, Fehrentz, Jean-Alain, Denoyelle, Séverine

Volltext

814 DT-9081, a selective EP4 receptor antagonist which synergizes with immune checkpoint inhibitors to induce complete responses in syngeneic murine cancer models von Blayo, Anne-Laure, Jouffroy-Zeller, Claire, Lenne, Nathalie, Nafia, Imane, Zerr, Patricia, Schann, Stéphan, Leroy, Xavier

Volltext