Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2S,3R)‑N‑((S)‑3-(Cyclopent-1-en-1-yl)-1-((R)‑2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)‑2-(2-morpholinoacetamido)propanamido)propenamide)
Johnson, Henry W. B, Lowe, Eric, Anderl, Janet L, Fan, Andrea, Muchamuel, Tony, Bowers, Simeon, Moebius, David C, Kirk, Christopher, McMinn, Dustin L
Published in Journal of medicinal chemistry (27.12.2018)
Published in Journal of medicinal chemistry (27.12.2018)
Get full text
Journal Article
Global signal peptide profiling reveals principles of selective Sec61 inhibition
Wenzell, Nicole A., Tuch, Brian B., McMinn, Dustin L., Lyons, Matthew J., Kirk, Christopher J., Taunton, Jack
Published in Nature chemical biology (01.09.2024)
Published in Nature chemical biology (01.09.2024)
Get full text
Journal Article
Zetomipzomib (KZR-616) attenuates lupus in mice via modulation of innate and adaptive immune responses
Muchamuel, Tony, Fan, R Andrea, Anderl, Janet L, Bomba, Darrin J, Johnson, Henry W B, Lowe, Eric, Tuch, Brian B, McMinn, Dustin L, Millare, Beatriz, Kirk, Christopher J
Published in Frontiers in immunology (10.03.2023)
Published in Frontiers in immunology (10.03.2023)
Get full text
Journal Article
Selective and Potent Morpholinone Inhibitors of the MDM2–p53 Protein–Protein Interaction
Gonzalez, Ana Z, Eksterowicz, John, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan B, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, McMinn, Dustin L, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Medina, Julio C, Sun, Daqing
Published in Journal of medicinal chemistry (27.03.2014)
Published in Journal of medicinal chemistry (27.03.2014)
Get full text
Journal Article
Discovery of AMG 925, a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3
Li, Zhihong, Wang, Xianghong, Eksterowicz, John, Gribble, Michael W, Alba, Grace Q, Ayres, Merrill, Carlson, Timothy J, Chen, Ada, Chen, Xiaoqi, Cho, Robert, Connors, Richard V, DeGraffenreid, Michael, Deignan, Jeffrey T, Duquette, Jason, Fan, Pingchen, Fisher, Benjamin, Fu, Jiasheng, Huard, Justin N, Kaizerman, Jacob, Keegan, Kathleen S, Li, Cong, Li, Kexue, Li, Yunxiao, Liang, Lingming, Liu, Wen, Lively, Sarah E, Lo, Mei-Chu, Ma, Ji, McMinn, Dustin L, Mihalic, Jeffrey T, Modi, Kriti, Ngo, Rachel, Pattabiraman, Kanaka, Piper, Derek E, Queva, Christophe, Ragains, Mark L, Suchomel, Julia, Thibault, Steve, Walker, Nigel, Wang, Xiaodong, Wang, Zhulun, Wanska, Malgorzata, Wehn, Paul M, Weidner, Margaret F, Zhang, Alex J, Zhao, Xiaoning, Kamb, Alexander, Wickramasinghe, Dineli, Dai, Kang, McGee, Lawrence R, Medina, Julio C
Published in Journal of medicinal chemistry (24.04.2014)
Published in Journal of medicinal chemistry (24.04.2014)
Get full text
Journal Article
Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit
Johnson, Henry W. B, Anderl, Janet L, Bradley, Erin K, Bui, John, Jones, Jeffrey, Arastu-Kapur, Shirin, Kelly, Lisa M, Lowe, Eric, Moebius, David C, Muchamuel, Tony, Kirk, Christopher, Wang, Zhengping, McMinn, Dustin
Published in ACS medicinal chemistry letters (13.04.2017)
Published in ACS medicinal chemistry letters (13.04.2017)
Get full text
Journal Article
207 Small molecule inhibitors of Sec61 cotranslational translocation regulate the phagocytosis checkpoint molecule CD47
Whang, Jennifer, Fan, Andrea, Kirk, Christopher, Lowe, Eric, McMinn, Dustin, Millare, Beatriz, Rao, Meera
Published in Journal for immunotherapy of cancer (01.11.2020)
Published in Journal for immunotherapy of cancer (01.11.2020)
Get full text
Journal Article
Efforts toward Expansion of the Genetic Alphabet: DNA Polymerase Recognition of a Highly Stable, Self-Pairing Hydrophobic Base
McMinn, Dustin L, Ogawa, Anthony K, Wu, Yiqin, Liu, Jianquan, Schultz, Peter G, Romesberg, Floyd E
Published in Journal of the American Chemical Society (15.12.1999)
Published in Journal of the American Chemical Society (15.12.1999)
Get full text
Journal Article
A Practical Synthesis of a Potent and Selective Diacylglycerol Acyltransferase-1 (DGAT-1) Inhibitor
Shin, Youngsook, Bergeron, Philippe, Fox, Brian M., Kayser, Frank, McGee, Lawrence R., McKendry, Sharon, McMinn, Dustin L., Labelle, Marc, Cushing, Timothy D.
Published in Synthesis (Stuttgart) (01.07.2014)
Published in Synthesis (Stuttgart) (01.07.2014)
Get more information
Journal Article
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11β-HSD1 inhibitors
Rew, Yosup, DeGraffenreid, Michael, He, Xiao, Jaen, Juan C., McMinn, Dustin L., Sun, Daqing, Tu, Hua, Ursu, Stefania, Powers, Jay P.
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Get full text
Journal Article
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines
Kaizerman, Jacob A., Aaron, Wade, An, Songzhu, Austin, Richard, Brown, Matt, Chong, Angela, Huang, Tom, Hungate, Randall, Jiang, Ben, Johnson, Michael G., Lee, Gary, Lucas, Brian S., Orf, Jessica, Rong, Minqing, Toteva, Maria M., Wickramasinghe, Dineli, Xu, Guifen, Ye, Qiuping, Zhong, Wendy, McMinn, Dustin L.
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
Get full text
Journal Article
Efforts toward the Expansion of the Genetic Alphabet: Information Storage and Replication with Unnatural Hydrophobic Base Pairs
Ogawa, Anthony K, Wu, Yiqin, McMinn, Dustin L, Liu, Jianquan, Schultz, Peter G, Romesberg, Floyd E
Published in Journal of the American Chemical Society (12.04.2000)
Published in Journal of the American Chemical Society (12.04.2000)
Get full text
Journal Article
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
Brown, Matthew L., Aaron, Wade, Austin, Richard J., Chong, Angela, Huang, Tom, Jiang, Ben, Kaizerman, Jacob A., Lee, Gary, Lucas, Brian S., McMinn, Dustin L., Orf, Jessica, Rong, Minqing, Toteva, Maria M., Xu, Guifen, Ye, Qiuping, Zhong, Wendy, DeGraffenreid, Michael R., Wickramasinghe, Dineli, Powers, Jay P., Hungate, Randall, Johnson, Michael G.
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Get full text
Journal Article
Synthesis, in Vitro Covalent Binding Evaluation, and Metabolism of (14)C-Labeled Inhibitors of 11β-HSD1
Sun, Daqing, Ye, Qiuping, Yan, Xuelei, Rew, Yosup, Fan, Peter, He, Xiao, Jiang, Min, McMinn, Dustin L, Monshouwer, Mario, Tu, Hua, Powers, Jay P
Published in ACS medicinal chemistry letters (13.11.2014)
Published in ACS medicinal chemistry letters (13.11.2014)
Get full text
Journal Article
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors
Rew, Yosup, McMinn, Dustin L., Wang, Zhulun, He, Xiao, Hungate, Randall W., Jaen, Juan C., Sudom, Athena, Sun, Daqing, Tu, Hua, Ursu, Stefania, Villemure, Elisia, Walker, Nigel P.C., Yan, Xuelei, Ye, Qiuping, Powers, Jay P.
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
Get full text
Journal Article
Synthesis, in Vitro Covalent Binding Evaluation, and Metabolism of 14C‑Labeled Inhibitors of 11β-HSD1
Sun, Daqing, Ye, Qiuping, Yan, Xuelei, Rew, Yosup, Fan, Peter, He, Xiao, Jiang, Min, McMinn, Dustin L, Monshouwer, Mario, Tu, Hua, Powers, Jay P
Published in ACS medicinal chemistry letters (13.11.2014)
Published in ACS medicinal chemistry letters (13.11.2014)
Get full text
Journal Article
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
McMinn, Dustin L., Rew, Yosup, Sudom, Athena, Caille, Seb, DeGraffenreid, Michael, He, Xiao, Hungate, Randall, Jiang, Ben, Jaen, Juan, Julian, Lisa D., Kaizerman, Jacob, Novak, Perry, Sun, Daqing, Tu, Hua, Ursu, Stefania, Walker, Nigel P.C., Yan, Xuelei, Ye, Qiuping, Wang, Zhulun, Powers, Jay P.
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
Get full text
Journal Article
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
Sun, Daqing, Wang, Zhulun, Caille, Seb, DeGraffenreid, Michael, Gonzalez-Lopez de Turiso, Felix, Hungate, Randall, Jaen, Juan C., Jiang, Ben, Julian, Lisa D., Kelly, Ron, McMinn, Dustin L., Kaizerman, Jacob, Rew, Yosup, Sudom, Athena, Tu, Hua, Ursu, Stefania, Walker, Nigel, Willcockson, Maren, Yan, Xuelei, Ye, Qiuping, Powers, Jay P.
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
Published in Bioorganic & medicinal chemistry letters (01.01.2011)
Get full text
Journal Article
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists
Lucas, Brian S., Aaron, Wade, An, Songzhu, Austin, Richard J., Brown, Matthew, Chan, Hon, Chong, Angela, Hungate, Randall, Huang, Tom, Jiang, Ben, Johnson, Michael G., Kaizerman, Jacob A., Lee, Gary, McMinn, Dustin L., Orf, Jessica, Powers, Jay P., Rong, Minqing, Toteva, Maria M., Uyeda, Craig, Wickramasinghe, Dineli, Xu, Guifen, Ye, Qiuping, Zhong, Wendy
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Get full text
Journal Article