Efficacy and Pharmacology of the NLRP3 Inflammasome Inhibitor CP-456,773 (CRID3) in Murine Models of Dermal and Pulmonary Inflammation
Primiano, Michael J, Lefker, Bruce A, Bowman, Michael R, Bree, Andrea G, Hubeau, Cedric, Bonin, Paul D, Mangan, Matthew, Dower, Ken, Monks, Brian G, Cushing, Leah, Wang, Stephen, Guzova, Julia, Jiao, Aiping, Lin, Lih-Ling, Latz, Eicke, Hepworth, David, Hall, J Perry
Published in The Journal of immunology (1950) (15.09.2016)
Published in The Journal of immunology (1950) (15.09.2016)
Get full text
Journal Article
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay
Hall, Justin, Brault, Amy, Vincent, Fabien, Weng, Shawn, Wang, Hong, Dumlao, Darren, Aulabaugh, Ann, Aivazian, Dikran, Castro, Dana, Chen, Ming, Culp, Jeffrey, Dower, Ken, Gardner, Joseph, Hawrylik, Steven, Golenbock, Douglas, Hepworth, David, Horn, Mark, Jones, Lyn, Jones, Peter, Latz, Eicke, Li, Jing, Lin, Lih-Ling, Lin, Wen, Lin, David, Lovering, Frank, Niljanskul, Nootaree, Nistler, Ryan, Pierce, Betsy, Plotnikova, Olga, Schmitt, Daniel, Shanker, Suman, Smith, James, Snyder, William, Subashi, Timothy, Trujillo, John, Tyminski, Edyta, Wang, Guoxing, Wong, Jimson, Lefker, Bruce, Dakin, Leslie, Leach, Karen
Published in PloS one (21.09.2017)
Published in PloS one (21.09.2017)
Get full text
Journal Article
Specific quinone reductase 2 inhibitors reduce metabolic burden and reverse Alzheimer's disease phenotype in mice
Gould, Nathaniel L, Scherer, Gila R, Carvalho, Silvia, Shurrush, Khriesto, Kayyal, Haneen, Edry, Efrat, Elkobi, Alina, David, Orit, Foqara, Maria, Thakar, Darshit, Pavesi, Tommaso, Sharma, Vijendra, Walker, Matthew, Maitland, Matthew, Dym, Orly, Albeck, Shira, Peleg, Yoav, Germain, Nicolas, Babaev, Ilana, Sharir, Haleli, Lalzar, Maya, Shklyar, Boris, Hazut, Neta, Khamaisy, Mohammad, Lévesque, Maxime, Lajoie, Gilles, Avoli, Massimo, Amitai, Gabriel, Lefker, Bruce, Subramanyam, Chakrapani, Shilton, Brian, Barr, Haim, Rosenblum, Kobi
Published in The Journal of clinical investigation (01.10.2023)
Published in The Journal of clinical investigation (01.10.2023)
Get full text
Journal Article
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging
Liang, Steven H., Chen, Jinshan Michael, Normandin, Marc D., Chang, Jeanne S., Chang, George C., Taylor, Christine K., Trapa, Patrick, Plummer, Mark S., Para, Kimberly S., Conn, Edward L., Lopresti-Morrow, Lori, Lanyon, Lorraine F., Cook, James M., Richter, Karl E. G., Nolan, Charlie E., Schachter, Joel B., Janat, Fouad, Che, Ye, Shanmugasundaram, Veerabahu, Lefker, Bruce A., Enerson, Bradley E., Livni, Elijahu, Wang, Lu, Guehl, Nicolas J., Patnaik, Debasis, Wagner, Florence F., Perlis, Roy, Holson, Edward B., Haggarty, Stephen J., El Fakhri, Georges, Kurumbail, Ravi G., Vasdev, Neil
Published in Angewandte Chemie (International ed.) (08.08.2016)
Published in Angewandte Chemie (International ed.) (08.08.2016)
Get full text
Journal Article
Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis
Helal, Christopher J, Bundesmann, Mark, Hammond, Susan, Holmstrom, Melissa, Klug-McLeod, Jacquelyn, Lefker, Bruce A, McLeod, Dale, Subramanyam, Chakrapani, Zakaryants, Oleg, Sakata, Sylvie
Published in ACS medicinal chemistry letters (08.08.2019)
Published in ACS medicinal chemistry letters (08.08.2019)
Get full text
Journal Article
Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
Liu, Shenping, Dakin, Leslie A., Xing, Li, Withka, Jane M., Sahasrabudhe, Parag V., Li, Wei, Banker, Mary Ellen, Balbo, Paul, Shanker, Suman, Chrunyk, Boris A., Guo, Zuojun, Chen, Jinshan M., Young, Jennifer A., Bai, Guoyun, Starr, Jeremy T., Wright, Stephen W., Bussenius, Joerg, Tan, Sheng, Gopalsamy, Ariamala, Lefker, Bruce A., Vincent, Fabien, Jones, Lyn H., Xu, Hua, Hoth, Lise R., Geoghegan, Kieran F., Qiu, Xiayang, Bunnage, Mark E., Thorarensen, Atli
Published in Scientific reports (16.08.2016)
Published in Scientific reports (16.08.2016)
Get full text
Journal Article
Toward the assembly and characterization of an encoded library hit confirmation platform: Bead-Assisted Ligand Isolation Mass Spectrometry (BALI-MS)
Ratnayake, Anokha S., Flanagan, Mark E., Foley, Timothy L., Hultgren, Scott L., Bellenger, Justin, Montgomery, Justin I., Lall, Manjinder S., Liu, Bo, Ryder, Tim, Kölmel, Dominik K., Shavnya, Andre, Feng, Xidong, Lefker, Bruce, Byrnes, Laura J., Sahasrabudhe, Parag V., Farley, Kathleen A., Chen, Shi, Wan, Jinqiao
Published in Bioorganic & medicinal chemistry (01.07.2021)
Published in Bioorganic & medicinal chemistry (01.07.2021)
Get full text
Journal Article
Practical synthesis of capromorelin, a growth hormone secretagogue, via a crystallization-induced dynamic resolution
Rose, Colin R., Zawistoski, Michael P., Lefker, Bruce A., Mangano, F. Michael, Wright, Ann S., Carpino, Philip A.
Published in Bioorganic & medicinal chemistry (01.02.2017)
Published in Bioorganic & medicinal chemistry (01.02.2017)
Get full text
Journal Article
Activation of the G-Protein-Coupled Receptor 119: A Conformation-Based Hypothesis for Understanding Agonist Response
McClure, Kim F, Darout, Etzer, Guimarães, Cristiano R. W, DeNinno, Michael P, Mascitti, Vincent, Munchhof, Michael J, Robinson, Ralph P, Kohrt, Jeffrey, Harris, Anthony R, Moore, Dianna E, Li, Bryan, Samp, Lacey, Lefker, Bruce A, Futatsugi, Kentaro, Kung, Daniel, Bonin, Paul D, Cornelius, Peter, Wang, Ruduan, Salter, Eben, Hornby, Sam, Kalgutkar, Amit S, Chen, Yue
Published in Journal of medicinal chemistry (24.03.2011)
Published in Journal of medicinal chemistry (24.03.2011)
Get full text
Journal Article
A Novel, Non‐Prostanoid EP2 Receptor‐Selective Prostaglandin E2 Agonist Stimulates Local Bone Formation and Enhances Fracture Healing
LI, Mei, KE, Hua Zhu, QI, Hong, Healy, David R, LI, Yan, Crawford, D Todd, Paralkar, Vishwas M, Owen, Thomas A, Cameron, Kimberly O, Lefker, Bruce A, Brown, Thomas A, Thompson, David D
Published in Journal of bone and mineral research (01.11.2003)
Published in Journal of bone and mineral research (01.11.2003)
Get full text
Journal Article
From partial to full agonism: Identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor
Futatsugi, Kentaro, Mascitti, Vincent, Guimarães, Cristiano R.W., Morishita, Nao, Cai, Cuiman, DeNinno, Michael P., Gao, Hua, Hamilton, Michael D., Hank, Richard, Harris, Anthony R., Kung, Daniel W., Lavergne, Sophie Y., Lefker, Bruce A., Lopaze, Michael G., McClure, Kim F., Munchhof, Michael J., Preville, Cathy, Robinson, Ralph P., Wright, Stephen W., Bonin, Paul D., Cornelius, Peter, Chen, Yue, Kalgutkar, Amit S.
Published in Bioorganic & medicinal chemistry letters (01.01.2013)
Published in Bioorganic & medicinal chemistry letters (01.01.2013)
Get full text
Journal Article
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor
Mascitti, Vincent, Stevens, Benjamin D., Choi, Chulho, McClure, Kim F., Guimarães, Cristiano R.W., Farley, Kathleen A., Munchhof, Michael J., Robinson, Ralph P., Futatsugi, Kentaro, Lavergne, Sophie Y., Lefker, Bruce A., Cornelius, Peter, Bonin, Paul D., Kalgutkar, Amit S., Sharma, Raman, Chen, Yue
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
Published in Bioorganic & medicinal chemistry letters (01.03.2011)
Get full text
Journal Article
A Nonprostanoid EP4 Receptor Selective Prostaglandin E2 Agonist Restores Bone Mass and Strength in Aged, Ovariectomized Rats
Ke, Hua Zhu, Crawford, D Todd, Qi, Hong, Simmons, Hollis A, Owen, Thomas A, Paralkar, Vishwas M, Li, Mei, Lu, Bihong, Grasser, William A, Cameron, Kimberly O, Lefker, Bruce A, DaSilva‐Jardine, Paul, Scott, Dennis O, Zhang, Qing, Tian, Xiao Yan, Jee, Webster SS, Brown, Thomas A, Thompson, David D
Published in Journal of bone and mineral research (01.04.2006)
Published in Journal of bone and mineral research (01.04.2006)
Get full text
Journal Article
Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility
Kalgutkar, Amit S., Frederick, Kosea S., Hatch, Heather L., Ambler, Catherine M., Perry, David A., Garigipati, Ravi S., Chang, George C., Lefker, Bruce A., Clark, Ronald W., Morehouse, Lee A., Francone, Omar, Hu, Xiao
Published in Xenobiotica (01.07.2014)
Published in Xenobiotica (01.07.2014)
Get full text
Journal Article
Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications
Li, Jie Jack, Iula, Donna M, Nguyen, Maria N, Hu, Lain-Yen, Dettling, Danielle, Johnson, Theodore R, Du, Daniel Y, Shanmugasundaram, Veerabahu, Van Camp, Jennifer A, Wang, Zhi, Harter, William G, Yue, Wen-Song, Boys, Mark L, Wade, Kimberly J, Drummond, Elena M, Samas, Brian M, Lefker, Bruce A, Hoge, Garrett S, Lovdahl, Mark J, Asbill, Jeffrey, Carroll, Matthew, Meade, Mary Ann, Ciotti, Susan M, Krieger-Burke, Theresa
Published in Journal of medicinal chemistry (13.11.2008)
Published in Journal of medicinal chemistry (13.11.2008)
Get full text
Journal Article
Correction: Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins
Wu, Jiang, Shin, Julia, Williams, Cara M. M, Geoghegan, Kieran F, Wright, Stephen W, Limburg, David C, Sahasrabudhe, Parag, Bonin, Paul D, Lefker, Bruce A, Ramsey, Simeon J
Published in MedChemComm (05.01.2015)
Published in MedChemComm (05.01.2015)
Get full text
Journal Article
Discovery of CP-533536 : An EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation
CAMERON, Kimberly O, LEFKER, Bruce A, LI YU, THOMPSON, David D, KE, Hua Z, MEI LI, ZAWISTOSKI, Michael P, TJOA, Christina M, WRIGHT, Ann S, DENINNO, Shari L, PARALKAR, Vishwas M, OWEN, Thomas A
Published in Bioorganic & medicinal chemistry letters (01.04.2009)
Published in Bioorganic & medicinal chemistry letters (01.04.2009)
Get full text
Journal Article
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity
Liu, Kevin K.-C., Lefker, Bruce A., Dombroski, Mark A., Chiang, Phoebe, Cornelius, Peter, Patterson, Terrell A., Zeng, Yuan, Santucci, Stephanie, Tomlinson, Elizabeth, Gibbons, Colleen P., Marala, Ravi, Brown, Janice A., Kong, Jimmy X., Lee, Eunsun, Werner, Wendy, Wenzel, Zane, Giragossian, Craig, Chen, Hou, Coffey, Steven B.
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Get full text
Journal Article
Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production
Mitchell, Lorna H., Hu, Lain-Yen, Nguyen, Maria, Fakhoury, Stephen, Smith, Yvonne, Iula, Donna, Kostlan, Catherine, Carroll, Matthew, Dettling, Danielle, Du, Daniel, Pocalyko, David, Wade, Kimberly, Lefker, Bruce
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Get full text
Journal Article
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging
Liang, Steven H., Chen, Jinshan Michael, Normandin, Marc D., Chang, Jeanne S., Chang, George C., Taylor, Christine K., Trapa, Patrick, Plummer, Mark S., Para, Kimberly S., Conn, Edward L., Lopresti-Morrow, Lori, Lanyon, Lorraine F., Cook, James M., Richter, Karl E. G., Nolan, Charlie E., Schachter, Joel B., Janat, Fouad, Che, Ye, Shanmugasundaram, Veerabahu, Lefker, Bruce A., Enerson, Bradley E., Livni, Elijahu, Wang, Lu, Guehl, Nicolas J., Patnaik, Debasis, Wagner, Florence F., Perlis, Roy, Holson, Edward B., Haggarty, Stephen J., El Fakhri, Georges, Kurumbail, Ravi G., Vasdev, Neil
Published in Angewandte Chemie (08.08.2016)
Published in Angewandte Chemie (08.08.2016)
Get full text
Journal Article