High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875
Srivastava, Ankita, Yano, Jason, Hirozane, Yoshihiko, Kefala, Georgia, Gruswitz, Franz, Snell, Gyorgy, Lane, Weston, Ivetac, Anthony, Aertgeerts, Kathleen, Nguyen, Jasmine, Jennings, Andy, Okada, Kengo
Published in Nature (London) (04.09.2014)
Published in Nature (London) (04.09.2014)
Get full text
Journal Article
Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein
Aertgeerts, Kathleen, Skene, Robert, Yano, Jason, Sang, Bi-Ching, Zou, Hua, Snell, Gyorgy, Jennings, Andy, Iwamoto, Keiji, Habuka, Noriyuki, Hirokawa, Aki, Ishikawa, Tomoyasu, Tanaka, Toshimasa, Miki, Hiroshi, Ohta, Yoshikazu, Sogabe, Satoshi
Published in The Journal of biological chemistry (27.05.2011)
Published in The Journal of biological chemistry (27.05.2011)
Get full text
Journal Article
Design and Synthesis of Novel Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors Bearing a Pyrrolo[3,2-d]pyrimidine Scaffold
Ishikawa, Tomoyasu, Seto, Masaki, Banno, Hiroshi, Kawakita, Youichi, Oorui, Mami, Taniguchi, Takahiko, Ohta, Yoshikazu, Tamura, Toshiya, Nakayama, Akiko, Miki, Hiroshi, Kamiguchi, Hidenori, Tanaka, Toshimasa, Habuka, Noriyuki, Sogabe, Satoshi, Yano, Jason, Aertgeerts, Kathleen, Kamiyama, Keiji
Published in Journal of medicinal chemistry (08.12.2011)
Published in Journal of medicinal chemistry (08.12.2011)
Get full text
Journal Article
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders
Gomez, Laurent, Massari, Mark Eben, Vickers, Troy, Freestone, Graeme, Vernier, William, Ly, Kiev, Xu, Rui, McCarrick, Margaret, Marrone, Tami, Metz, Markus, Yan, Yingzhou G, Yoder, Zachary W, Lemus, Robert, Broadbent, Nicola J, Barido, Richard, Warren, Noelle, Schmelzer, Kara, Neul, David, Lee, Dong, Andersen, Carsten B, Sebring, Kristen, Aertgeerts, Kathleen, Zhou, Xianbo, Tabatabaei, Ali, Peters, Marco, Breitenbucher, J. Guy
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
Get full text
Journal Article
Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV
Zhang, Zhiyuan, Wallace, Michael B, Feng, Jun, Stafford, Jeffrey A, Skene, Robert J, Shi, Lihong, Lee, Bumsup, Aertgeerts, Kathleen, Jennings, Andy, Xu, Rongda, Kassel, Daniel B, Kaldor, Stephen W, Navre, Marc, Webb, David R, Gwaltney, Stephen L
Published in Journal of medicinal chemistry (27.01.2011)
Published in Journal of medicinal chemistry (27.01.2011)
Get full text
Journal Article
The Low Density Lipoprotein Receptor-related Protein Is a Motogenic Receptor for Plasminogen Activator Inhibitor-1
Degryse, Bernard, Neels, Jaap G, Czekay, Ralf-Peter, Aertgeerts, Kathleen, Kamikubo, Yu-Ichi, Loskutoff, David J
Published in The Journal of biological chemistry (21.05.2004)
Published in The Journal of biological chemistry (21.05.2004)
Get full text
Journal Article
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554
Maezaki, Hironobu, Banno, Yoshihiro, Miyamoto, Yasufumi, Moritou, Yuusuke, Asakawa, Tomoko, Kataoka, Osamu, Takeuchi, Koji, Suzuki, Nobuhiro, Ikedo, Koji, Kosaka, Takuo, Sasaki, Masako, Tsubotani, Shigetoshi, Tani, Akiyoshi, Funami, Miyuki, Yamamoto, Yoshio, Tawada, Michiko, Aertgeerts, Kathleen, Yano, Jason, Oi, Satoru
Published in Bioorganic & medicinal chemistry (01.08.2011)
Published in Bioorganic & medicinal chemistry (01.08.2011)
Get full text
Journal Article
Dataset on Galanin Receptor 3 mutants that improve recombinant receptor expression and stability in an agonist and antagonist bound form
Ho, Thao T., Nguyen, Jasmine T., Liu, Juping, Stanczak, Pawel, Thompson, Aaron A., Yan, Yingzhuo G., Chen, Jasmine, Allerston, Charles K., Dillard, Charles L., Xu, Hao, Shoger, Nicholas J., Cameron, Jill S., Massari, Mark E., Aertgeerts, Kathleen
Published in Data in brief (01.06.2017)
Published in Data in brief (01.06.2017)
Get full text
Journal Article
N‐linked glycosylation of dipeptidyl peptidase IV (CD26): Effects on enzyme activity, homodimer formation, and adenosine deaminase binding
Aertgeerts, Kathleen, Ye, Sheng, Shi, Lihong, Prasad, Sridhar G., Witmer, Darbi, Chi, Ellen, Sang, Bi‐Ching, Wijnands, Robert A., Webb, David R., Swanson, Ronald V.
Published in Protein science (01.01.2004)
Published in Protein science (01.01.2004)
Get full text
Journal Article
Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of C‑7-Substituted 1,3-Benzothiazole Derivatives
Okaniwa, Masanori, Hirose, Masaaki, Arita, Takeo, Yabuki, Masato, Nakamura, Akito, Takagi, Terufumi, Kawamoto, Tomohiro, Uchiyama, Noriko, Sumita, Akihiko, Tsutsumi, Shunichirou, Tottori, Tsuneaki, Inui, Yoshitaka, Sang, Bi-Ching, Yano, Jason, Aertgeerts, Kathleen, Yoshida, Sei, Ishikawa, Tomoyasu
Published in Journal of medicinal chemistry (22.08.2013)
Published in Journal of medicinal chemistry (22.08.2013)
Get full text
Journal Article
Target Engagement of a Phosphodiesterase 2A Inhibitor Affecting Long-Term Memory in the Rat
Gu, Guibao, Scott, Trevor, Yan, Yingzhuo, Warren, Noelle, Zhang, Adia, Tabatabaei, Ali, Xu, Hao, Aertgeerts, Kathleen, Gomez, Laurent, Morse, Andrew, Li, Yu-Wen, Breitenbucher, J Guy, Massari, Eben, Vivian, Jeffrey, Danks, Anne
Published in The Journal of pharmacology and experimental therapeutics (01.09.2019)
Published in The Journal of pharmacology and experimental therapeutics (01.09.2019)
Get full text
Journal Article
Mathematical and Structural Characterization of Strong Nonadditive Structure–Activity Relationship Caused by Protein Conformational Changes
Gomez, Laurent, Xu, Rui, Sinko, William, Selfridge, Brandon, Vernier, William, Ly, Kiev, Truong, Richard, Metz, Markus, Marrone, Tami, Sebring, Kristen, Yan, Yingzhou, Appleton, Brent, Aertgeerts, Kathleen, Massari, Mark Eben, Breitenbucher, J. Guy
Published in Journal of medicinal chemistry (13.09.2018)
Published in Journal of medicinal chemistry (13.09.2018)
Get full text
Journal Article
Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties
Dyck, Brian, Branstetter, Bryan, Gharbaoui, Tawfik, Hudson, Andrew R, Breitenbucher, J. Guy, Gomez, Laurent, Botrous, Iriny, Marrone, Tami, Barido, Richard, Allerston, Charles K, Cedervall, E. Peder, Xu, Rui, Sridhar, Vandana, Barker, Ryan, Aertgeerts, Kathleen, Schmelzer, Kara, Neul, David, Lee, Dong, Massari, Mark Eben, Andersen, Carsten B, Sebring, Kristen, Zhou, Xianbo, Petroski, Robert, Limberis, James, Augustin, Martin, Chun, Lawrence E, Edwards, Thomas E, Peters, Marco, Tabatabaei, Ali
Published in Journal of medicinal chemistry (27.04.2017)
Published in Journal of medicinal chemistry (27.04.2017)
Get full text
Journal Article
Outcome of the First wwPDB/CCDC/D3R Ligand Validation Workshop
Adams, Paul D., Aertgeerts, Kathleen, Bauer, Cary, Bell, Jeffrey A., Berman, Helen M., Bhat, Talapady N., Blaney, Jeff M., Bolton, Evan, Bricogne, Gerard, Brown, David, Burley, Stephen K., Case, David A., Clark, Kirk L., Darden, Tom, Emsley, Paul, Feher, Victoria A., Feng, Zukang, Groom, Colin R., Harris, Seth F., Hendle, Jorg, Holder, Thomas, Joachimiak, Andrzej, Kleywegt, Gerard J., Krojer, Tobias, Marcotrigiano, Joseph, Mark, Alan E., Markley, John L., Miller, Matthew, Minor, Wladek, Montelione, Gaetano T., Murshudov, Garib, Nakagawa, Atsushi, Nakamura, Haruki, Nicholls, Anthony, Nicklaus, Marc, Nolte, Robert T., Padyana, Anil K., Peishoff, Catherine E., Pieniazek, Susan, Read, Randy J., Shao, Chenghua, Sheriff, Steven, Smart, Oliver, Soisson, Stephen, Spurlino, John, Stouch, Terry, Svobodova, Radka, Tempel, Wolfram, Terwilliger, Thomas C., Tronrud, Dale, Velankar, Sameer, Ward, Suzanna C., Warren, Gregory L., Westbrook, John D., Williams, Pamela, Yang, Huanwang, Young, Jasmine
Published in Structure (London) (05.04.2016)
Published in Structure (London) (05.04.2016)
Get full text
Journal Article
Discovery of a Tetrahydropyrimidin-2(1H)-one Derivative (TAK-442) as a Potent, Selective, and Orally Active Factor Xa Inhibitor
Fujimoto, Takuya, Imaeda, Yasuhiro, Konishi, Noriko, Hiroe, Katsuhiko, Kawamura, Masaki, Textor, Garret P, Aertgeerts, Kathleen, Kubo, Keiji
Published in Journal of medicinal chemistry (13.05.2010)
Published in Journal of medicinal chemistry (13.05.2010)
Get full text
Journal Article
Design and Synthesis of Novel DFG-Out RAF/Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Inhibitors. 1. Exploration of [5,6]-Fused Bicyclic Scaffolds
Okaniwa, Masanori, Hirose, Masaaki, Imada, Takashi, Ohashi, Tomohiro, Hayashi, Youko, Miyazaki, Tohru, Arita, Takeo, Yabuki, Masato, Kakoi, Kazuyo, Kato, Juran, Takagi, Terufumi, Kawamoto, Tomohiro, Yao, Shuhei, Sumita, Akihiko, Tsutsumi, Shunichirou, Tottori, Tsuneaki, Oki, Hideyuki, Sang, Bi-Ching, Yano, Jason, Aertgeerts, Kathleen, Yoshida, Sei, Ishikawa, Tomoyasu
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
Get full text
Journal Article
Structural and Kinetic Analysis of the Substrate Specificity of Human Fibroblast Activation Protein α
Aertgeerts, Kathleen, Levin, Irena, Shi, Lihong, Snell, Gyorgy P., Jennings, Andy, Prasad, G. Sridhar, Zhang, Yanming, Kraus, Michelle L., Salakian, Shant, Sridhar, Vandana, Wijnands, Robert, Tennant, Mike G.
Published in The Journal of biological chemistry (20.05.2005)
Published in The Journal of biological chemistry (20.05.2005)
Get full text
Journal Article
Discovery of a 3-Pyridylacetic Acid Derivative (TAK-100) as a Potent, Selective and Orally Active Dipeptidyl Peptidase IV (DPP-4) Inhibitor
Miyamoto, Yasufumi, Banno, Yoshihiro, Yamashita, Tohru, Fujimoto, Tatsuhiko, Oi, Satoru, Moritoh, Yusuke, Asakawa, Tomoko, Kataoka, Osamu, Yashiro, Hiroaki, Takeuchi, Koji, Suzuki, Nobuhiro, Ikedo, Koji, Kosaka, Takuo, Tsubotani, Shigetoshi, Tani, Akiyoshi, Sasaki, Masako, Funami, Miyuki, Amano, Michiko, Yamamoto, Yoshio, Aertgeerts, Kathleen, Yano, Jason, Maezaki, Hironobu
Published in Journal of medicinal chemistry (10.02.2011)
Published in Journal of medicinal chemistry (10.02.2011)
Get full text
Journal Article
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: A new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554
Banno, Yoshihiro, Miyamoto, Yasufumi, Sasaki, Mitsuru, Oi, Satoru, Asakawa, Tomoko, Kataoka, Osamu, Takeuchi, Koji, Suzuki, Nobuhiro, Ikedo, Koji, Kosaka, Takuo, Tsubotani, Shigetoshi, Tani, Akiyoshi, Funami, Miyuki, Tawada, Michiko, Yamamoto, Yoshio, Aertgeerts, Kathleen, Yano, Jason, Maezaki, Hironobu
Published in Bioorganic & medicinal chemistry (15.08.2011)
Published in Bioorganic & medicinal chemistry (15.08.2011)
Get full text
Journal Article