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Discovery and Characterization of PVTX-321 as a Potent and Orally Bioavailable Estrogen Receptor Degrader for ER+/HER2-Breast Cancer PVTX-321的发现与表征：一种强效且口服生物利用度高的雌激素受体降解剂，用于ER+/HER2-乳腺癌 Xu, Guozhang; Havens, Courtney G.; Deng, Qiaolin; Lowenstein, Cassandra; Samanta, Debangshu; Vidal, Brian; Behshad, Elham; Russell, Mike; Orth, Peter; Rice, Cory T.; Nagilla, Rakesh; Kirchhoff, Paul; Chen, Zhixiang; Rej, Rohan Kalyan; Acharyya, Ranjan Kumar; Wu, Dimin; Wang, Shaomeng; Zhang, Weihong; Wu, Wenxue; Jolivette, Larry; Strickland, Corey; Sui, Zhihua; Mohammad, Helai P.; Zhang, Xuqing; Priestley, E. Scott 分享 收藏
Discovery of Potent, Highly Selective, and Efficacious SMARCA2 Degraders Li, Zhenwu; Harikrishnan, Lalgudi S.; Xu, Guozhang; Samanta, Debangshu; Clemente, Jose C.; Leng, Lingying; Tu, Wenbin; Yang, Lin; Huang, Liyue; Wang, Mi; Wang, Shaomeng; Deng, Qiaolin; Behshad, Elham; Nagilla, Rakesh; Orth, Peter; Rice, Cory; Strickland, Corey; Mohammad, Helai P.; Priestley, E. Scott; Sui, Zhihua 分享 收藏
Development of a Biocatalytic Aerobic Oxidation for the Manufacturing Route to Islatravir Shaw, Megan H.; Fryszkowska, Anna; Alvizo, Oscar; Attadgie, Ilana; Borra-Garske, Margie; Devine, Paul N.; Duan, Da; Grosser, Shane T.; Forstater, Jacob H.; Hughes, Gregory J.; Maloney, Kevin M.; Margelefsky, Eric L.; Mattern, Keith A.; Miller, Margaret T.; Nawrat, Christopher C.; Nazor, Jovana; Orth, Peter; Ouimet, Claire M.; Robaire, Sandra A.; Ruccolo, Serge; Schwalm, Erica L.; Verma, Deeptak; Xiao, Li; Zhang, Victoria 分享 收藏
Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor MK-1084的发现: 一种口服生物利用度和低剂量的KRASG12C抑制剂 Ma, Xiaoshen; Sloman, David L.; Duggal, Ruchia; Anderson, Kenneth D.; Ballard, Jeanine E.; Bharathan, Indu; Brynczka, Christopher; Gathiaka, Symon; Henderson, Timothy J.; Lyons, Thomas W.; Miller, Richard; Munsell, Erik V.; Orth, Peter; Otte, Ryan D.; Palani, Anandan; Rankic, Danica A.; Robinson, Michelle R.; Sather, Aaron C.; Solban, Nicolas; Song, Xuelei Sherry; Wen, Xin; Xu, Zangwei; Yang, Yi; Yang, Ruojing; Day, Phil J.; Stoeck, Alexander; Bennett, David Jonathan; Han, Yongxin 分享 收藏
Discovery and characterization of PVTX-321, an estrogen receptor heterobifunctional degrader Havens, Courtney G.; Xu, Guozhang; Lowenstein, Cass; Samanta, Debangshu; Vidal, Brian; Behshad, Elham; Nagilla, Rakesh; Russell, Mike; Orth, Peter; Wu, Winston; Jolivette, Larry; Priestley, Scott; Mohammad, Helai; Sui, Zhihua 分享 收藏
Discovery of oral SMARCA2 degraders for the treatment of SMARCA4 mutant tumors Clemente, Jose C.; Harikrishnan, Lal; Knight, Steve; Samanta, Debangshu; Li, Zhenwu; Nagilla, Rakesh; Kendsersky, Nathan; Joshi, Shreyas; Orth, Peter; Tudor, Matt; Deng, Qiaolin; Aguilar-Bonavides, Clemente; Behshad, Elham; Sui, Zhihua; Strickland, Corey; Jolivette, Larry J.; Mohammad, Helai P. 分享 收藏
Discovery and characterization of a p300-selective degrader with potent anti-tumor activity in CBP mutant cancers Russell, Mike R.; Lowenstein, Cassandra L.; Zhang, Xuqing; Roach, Jeremy; Song, Jianing; Nagilla, Rakesh; Kendsersky, Nathan; Joshi, Shreyas; Orth, Peter; Tudor, Matt; Deng, Qiaolin; Aguilar-Bonavides, Clemente; Behshad, Elham; Banjade, Sudeep; Sui, Zhihua; Strickland, Corey; Jolivette, Larry; Mohammad, Helai P. 分享 收藏
The selective IKZF2 molecular glue degrader, PVTX-405, counters Treg immune suppression,shows significant tumor growth delay as single agent and synergistic response with immune checkpoint therapies (ICTs) Dhruv, Harshil D.; McEachern, Donna; Bai, Longchuan; Zhang, Xuqing; Chen, Zhixiang; Nagilla, Rakesh; Behshad, Elham; Han, Bomie; Orth, Peter; Rej, Rohan; Kirchhoff, Paul; Shin, Niu; Jolivette, Larry; Strickland, Corey; Sui, Zhihua; Priestley, Scott; Wang, Shaomeng; Mohammad, Helai 分享 收藏
Predictive wild-type RAS/BRAF and pharmacogenetic biomarkers drive selection of metastatic colorectal cancer patients fit for intensive first-line FIr-C/FOx-C schedule adding cetuximab to triplet chemotherapy Russell, Mike; Lowenstein, Cassandra L.; Zhang, Xuqing; Roach, Jeremy; Song, Jianing; Nagilla, Rakesh; Orth, Peter; Tudor, Matt; Deng, Qiaolin; Sui, Zhihua; Strickland, Corey; Jolivette, Larry J.; Priestley, E. Scott; Mohammad, Helai P. 分享 收藏
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors Tucker, Thomas J.; Embrey, Mark W.; Alleyne, Candice; Amin, Rupesh P.; Bass, Alan; Bhatt, Bhavana; Bianchi, Elisabetta; Branca, Danila; Bueters, Tjerk; Buist, Nicole; Ha, Sookhee N.; Hafey, Mike; He, Huaibing; Higgins, John; Johns, Douglas G.; Kerekes, Angela D.; Koeplinger, Kenneth A.; Kuethe, Jeffrey T.; Li, Nianyu; Murphy, BethAnn; Orth, Peter; Salowe, Scott; Shahripour, Aurash; Tracy, Rodger; Wang, Weixun; Wu, Chengwei; Xiong, Yusheng; Zokian, Hratch J.; Wood, Harold B.; Walji, Abbas 分享 收藏
Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling Lim, Shuhui; Boyer, Nicolas; Boo, Nicole; Huang, Chunhui; Venkatachalam, Gireedhar; Juang, Yu-Chi Angela; Garrigou, Michael; Kaan, Kristal; Duggal, Ruchia; Peh, Khong Ming; Sadruddin, Ahmad; Gopal, Pooja; Yuen, Tsz Ying; Ng, Simon; Kannan, Srinivasaraghavan; Brown, Christopher J.; Verma, Chandra; Orth, Peter; Peier, Andrea; Ge, Lan; Yu, Xiang; Bhatt, Bhavana; Chen, Feifei; Wang, Erjia; Li, Nianyu Jason; Gonzales, Raymond J.; Stoeck, Alexander; Henry, Brian; Sawyer, Tomi K.; Lane, David; Johannes, Charles W.; Biswas, Kaustav; Partridge, Anthony W. 分享 收藏
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design 从mRNA显示屏衍生并通过基于结构的设计优化的一系列新型高效环肽PCSK9抑制剂 Alleyne, Candice; Amin, Rupesh P.; Bhatt, Bhavana; Bianchi, Elisabetta; Blain, J. Craig; Boyer, Nicolas; Branca, Danila; Embrey, Mark W.; Ha, Sookhee N.; Jette, Kelli; Johns, Douglas G.; Kerekes, Angela D.; Koeplinger, Kenneth A.; LaPlaca, Derek; Li, Nianyu; Murphy, Beth; Orth, Peter; Ricardo, Alonso; Salowe, Scott; Seyb, Kathleen; Shahripour, Aurash; Stringer, Joseph R.; Sun, Yili; Tracy, Rodger; Wu, Chengwei; Xiong, Yusheng; Youm, Hyewon; Zokian, Hratch J.; Tucker, Thomas J. 分享 收藏
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9 Petrilli, Whitney L.; Adam, Gregory C.; Erdmann, Roman S.; Abeywickrema, Pravien; Agnani, Vijayalakshmi; Ai, Xi; Baysarowich, Jen; Byrne, Noel; Caldwell, John P.; Chang, Wonsuk; DiNunzio, Edward; Feng, Zhe; Ford, Rachael; Ha, Sookhee; Huang, Yongcheng; Hubbard, Brian; Johnston, Jennifer M.; Kavana, Michael; Lisnock, Jean-Marie; Liang, Rui; Lu, Jun; Lu, Zhijian; Meng, Juncai; Orth, Peter; Palyha, Oksana; Parthasarathy, Gopal; Salowe, Scott P.; Sharma, Sujata; Shipman, Jennifer; Soisson, Stephen M.; Strack, Alison M.; Youm, Hyewon; Zhao, Kake; Zink, Deborah L.; Zokian, Hratch; Addona, George H.; Akinsanya, Karen; Tata, James R.; Xiong, Yusheng; Imbriglio, Jason E. 分享 收藏
Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease Scott, Jack D.; Li, Sarah W.; Brunskill, Andrew P. J.; Chen, Xia; Cox, Kathleen; Cumming, Oared N.; Forman, Mark; Gilbert, Eric J.; Hodgson, Robert A.; Hyde, Lynn A.; Jiang, Qin; Iserloh, Ulrich; Kazakevich, Irina; Kuvelkar, Reshma; Mei, Hong; Meredith, John; Misiaszek, Jeffrey; Orth, Peter; Rossiter, Lana M.; Slater, Meagan; Stone, Julie; Strickland, Corey O.; Voigt, Johannes H.; Wang, Ganfeng; Wang, Hongwu; Wu, Yusheng; Greenlee, William J.; Parker, Eric M.; Kennedy, Matthew E.; Stamford, Andrew W. 分享 收藏
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates Mandal, Mihirbaran; Wu, Yusheng; Misiaszek, Jeffrey; Li, Guoqing; Buevich, Alexei; Caldwell, John P.; Liu, Xiaoxiang; Mazzola, Robert D.; Orth, Peter; Strickland, Corey; Voigt, Johannes; Wang, Hongwu; Zhu, Zhaoning; Chen, Xia; Grzelak, Michael; Hyde, Lynn A.; Kuvelkar, Reshma; Leach, Prescott T.; Terracina, Giuseppe; Zhang, Lili; Zhang, Qi; Michener, Maria S.; Smith, Brad; Cox, Kathleen; Grotz, Diane; Favreau, Leonard; Mitra, Kaushik; Kazakevich, Irina; McKittrick, Brian A.; Greenlee, William; Kennedy, Matthew E.; Parker, Eric M.; Cumming, Jared N.; Stamford, Andrew W. 分享 收藏
Mechanism of Action and Epitopes of Clostridium difficile Toxin B-neutralizing Antibody Bezlotoxumab Revealed by X-ray Crystallography Orth, Peter; Xiao, Li; Hernandez, Lorraine D.; Reichert, Paul; Sheth, Payal R.; Beaumont, Maribel; Yang, Xiaoyu; Murgolo, Nicholas; Ermakov, Grigori; DiNunzio, Edward; Racine, Fred; Karczewski, Jerzy; Secore, Susan; Ingram, Richard N.; Mayhood, Todd; Strickland, Corey; Therien, Alex G. 分享 收藏
Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme-1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation Mandal, Mihirbaran; Zhu, Zhaoning; Cumming, Jared N.; Liu, Xiaoxiang; Strickland, Corey; Mazzola, Robert D.; Caldwell, John P.; Leach, Prescott; Grzelak, Michael; Hyde, Lynn; Zhang, Qi; Terracina, Giuseppe; Zhang, Lili; Chen, Xia; Kuvelkar, Reshma; Kennedy, Matthew E.; Favreau, Leonard; Cox, Kathleen; Orth, Peter; Buevich, Alexei; Voig, Johannes; Wang, Hongwu; Kazakevich, Irina; McKittrick, Brian A.; Greenlee, William; Parker, Eric M.; Stamford, Andrew W. 分享 收藏
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction Stamford, Andrew W.; Scott, Jack D.; Li, Sarah W.; Babu, Suresh; Tadesse, Dawit; Hunter, Rachael; Wu, Yusheng; Misiaszek, Jeffrey; Cumming, Jared N.; Gilbert, Eric J.; Huang, Chunli; McKittrick, Brian A.; Hong, Liwu; Guo, Tao; Zhu, Zhaoning; Strickland, Corey; Orth, Peter; Voigt, Johannes H.; Kennedy, Matthew E.; Chen, Xia; Kuvelkar, Reshma; Hodgson, Robert; Hyde, Lynn A.; Cox, Kathleen; Favreau, Leonard; Parker, Eric M.; Greenlee, William J. 分享 收藏
Design, Synthesis, and X-ray Crystallographic Analysis of a Novel Class of HIV-1 Protease Inhibitors (vol 54, pg 7176, 2011) Ganguly, Ashit K.; Alluri, Sesha S.; Caroccia, Danielle; Biswas, Dipshikha; Wang, Chih-Hung; Kang, Eunhee; Zhang, Yong; McPhail, Andrew T.; Carroll, Steven S.; Burlein, Christine; Munshi, Vandna; Orth, Peter; Strickland, Corey 分享 收藏
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