未登录 Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease 临床候选PF-06648671的发现: 一种有效的 γ-分泌酶调节剂,用于治疗阿尔茨海默氏病 Pettersson, Martin; Johnson, Douglas S.; Humphrey, John M.; Am Ende, Christopher W.; Butler, Todd W.; Dorff, Peter H.; Efremov, Ivan V.; Evrard, Edelweiss; Green, Michael E.; Helal, Christopher J.; Kauffman, Gregory W.; Mullins, Patrick B.; Navaratnam, Thayalan; O'Donnell, Christopher J.; O'Sullivan, Theresa J.; Patel, Nandini C.; Stepan, Antonia F.; Stiff, Cory M.; Subramanyam, Chakrapani; Trapa, Patrick; Tran, Tuan P.; Vetelino, Beth Cooper; Yang, Eddie; Xie, Longfei; Pustilnik, Leslie R.; Steyn, Stefanus J.; Wood, Kathleen M.; Bales, Kelly R.; Hajos-Korcsok, Eva; Verhoest, Patrick R. 分享 收藏
A chemical probe to modulate human GID4 Pro/N-degron interactions Owens, Dominic D. G.; Maitland, Matthew E. R.; Yazdi, Aliakbar Khalili; Song, Xiaosheng; Reber, Viviane; Schwalm, Martin P.; Machado, Raquel A. C.; Bauer, Nicolas; Wang, Xu; Szewczyk, Magdalena M.; Dong, Cheng; Dong, Aiping; Loppnau, Peter; Calabrese, Matthew F.; Dowling, Matthew S.; Lee, Jisun; Montgomery, Justin I.; O'Connell, Thomas N.; Subramanyam, Chakrapani; Wang, Feng; Adamson, Ella C.; Schapira, Matthieu; Gstaiger, Matthias; Knapp, Stefan; Vedadi, Masoud; Min, Jinrong; Lajoie, Gilles A.; Barsyte-Lovejoy, Dalia; Owen, Dafydd R.; Schild-Poulter, Caroline; Arrowsmith, Cheryl H. 分享 收藏
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex Yazdi, Aliakbar Khalili; Perveen, Sumera; Dong, Cheng; Song, Xiaosheng; Dong, Aiping; Szewczyk, Magdalena M.; Calabrese, Matthew F.; Casimiro-Garcia, Agustin; Chakrapani, Subramanyam; Dowling, Matthew S.; Ficici, Emel; Lee, Jisun; Montgomery, Justin I.; O'Connell, Thomas N.; Skrzypek, Grzegorz J.; Tran, Tuan P.; Troutman, Matthew D.; Wang, Feng; Young, Jennifer A.; Min, Jinrong; Barsyte-Lovejoy, Dalia; Brown, Peter J.; Santhakumar, Vijayaratnam; Arrowsmith, Cheryl H.; Vedadi, Masoud; Owen, Dafydd R. 分享 收藏
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; Levesque, Maxime; Lajoie, Gilles; Avoli, Massimo; Amitai, Gabriel; Lefker, Bruce; Subramanyam, Chakrapani; Shilton, Brian; Barr, Haim; Rosenblum, Kobi 分享 收藏
Anti-Extra Domain B Splice Variant of Fibronectin Antibody-Drug Conjugate Eliminates Tumors with Enhanced Efficacy When Combined with Checkpoint Blockade 纤连蛋白抗体-药物偶联物的抗外域B剪接变体与检查点阻断相结合可消除肿瘤,并提高疗效 Hooper, Andrea T.; Marquette, Kimberly; Chang, Chao -Pei Betty; Golas, Jonathon; Jain, Sadhana; Lam, My-Hanh; Guffroy, Magali; Leal, Mauricio; Falahatpisheh, Hadi; Mathur, Divya; Chen, Ting; Kelleher, Kerry; Khandke, Kiran; Muszynska, Elwira; Loganzo, Frank; Rosfjord, Edward; Lucas, Judy; Kan, Zhengyan; Subramanyam, Chakrapani; O'Donnell, Christopher; Neri, Dario; Gerber, Hans-Peter; May, Chad; Sapra, Puja 分享 收藏
Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library Kung, Pei-Pei; Bingham, Patrick; Burke, Benjamin J.; Chen, Qiuxia; Cheng, Xuemin; Deng, Ya-Li; Dou, Dengfeng; Feng, Junli; Gallego, Gary M.; Gehring, Michael R.; Grant, Stephan K.; Greasley, Samantha; Harris, Anthony R.; Maegley, Karen A.; Meier, Jordan; Meng, Xiaoyun; Montano, Jose L.; Morgan, Barry A.; Naughton, Brigitte S.; Palde, Prakash B.; Paul, Thomas A.; Richardson, Paul; Sakata, Sylvie; Shaginian, Alex; Sonnenburg, William K.; Subramanyam, Chakrapani; Timofeevski, Sergei; Wan, Jinqiao; Yan, Wen; Stewart, Albert E. 分享 收藏
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 分享 收藏
Covalent Docking Identifies a Potent and Selective MKK7 Inhibitor Shraga, Amit; Olshvang, Evgenia; Davidzohn, Natalia; Khoshkenar, Payam; Germain, Nicolas; Shurrush, Khriesto; Carvalho, Silvia; Avram, Liat; Albeck, Shira; Unger, Tamar; Lefker, Bruce; Subramanyam, Chakrapani; Hudkins, Robert L.; Mitchell, Amir; Shulman, Ziv; Kinoshita, Takayoshi; London, Nir 分享 收藏
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Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors Wager, Travis T.; Galatsis, Paul; Chandrasekaran, Ramalakshmi Y.; Butler, Todd W.; Li, Jianke; Zhang, Lei; Mente, Scot; Subramanyam, Chakrapani; Liu, Shenping; Doran, Angela C.; Chang, Cheng; Fisher, Katherine; Grimwood, Sarah; Hedde, Joseph R.; Marconi, Michael; Schildknegt, Klaas 分享 收藏
Design, Synthesis, and Cytotoxic Evaluation of Novel Tubulysin Analogues as ADC Payloads Leverett, Carolyn A.; Sukuru, Sai Chetan K.; Vetelino, Beth C.; Musto, Sylvia; Parris, Kevin; Pandit, Jayvardhan; Loganzo, Frank; Varghese, Alison H.; Bai, Guoyun; Liu, Bin; Liu, Dingguo; Hudson, Sarah; Doppalapudi, Venkata Ramana; Stock, Joseph; O'Donnell, Christopher J.; Subramanyam, Chakrapani 分享 收藏
Optimization of Tubulysin Antibody-Drug Conjugates: A Case Study in Addressing ADC Metabolism Tumey, L. Nathan; Leverett, Carolyn A.; Vetelino, Beth; Li, Fengping; Rago, Brian; Han, Xiaogang; Loganzo, Frank; Musto, Sylvia; Bai, Guoyun; Sukuru, Sai Chetan K.; Graziani, Edmund I.; Puthenveetil, Sujiet; Casavant, Jeffrey; Ratnayake, Anokha; Marquette, Kimberly; Hudson, Sarah; Doppalapudi, Venkata Ramana; Stock, Joseph; Tchistiakova, Lioudmila; Bessire, Andrew J.; Clark, Tracey; Lucas, Judy; Hosselet, Christine; O'Donnell, Christopher J.; Subramanyam, Chakrapani 分享 收藏
Natural Product Splicing Inhibitors: A New Class of Antibody-Drug Conjugate (ADC) Payloads 天然产物剪接抑制剂: 一类新的抗体-药物偶联物 (ADC) 有效载荷 Puthenveetil, Sujiet; Loganzo, Frank; He, Haiyin; Dirico, Ken; Green, Michael; Teske, Jesse; Musto, Sylvia; Clark, Tracey; Rago, Brian; Koehn, Frank; Veneziale, Robert; Falahaptisheh, Hadi; Han, Xiaogang; Barletta, Frank; Lucas, Judy; Subramanyam, Chakrapani; O'Donnell, Christopher J.; Tumey, L. Nathan; Sapra, Puja; Gerber, Hans Peter; Ma, Dangshe; Graziani, Edmund I. 分享 收藏
Determination of Antibody-Drug Conjugate Released Payload Species Using Directed in Vitro Assays and Mass Spectrometric Interrogation Bessire, Andrew J.; Ballard, T. Eric; Charati, Manoj; Cohen, Justin; Green, Michael; Lam, My-Hanh; Loganzo, Frank; Nolting, Birte; Pierce, Betsy; Puthenveetil, Sujiet; Roberts, Lee; Schildknegt, Klaas; Subramanyam, Chakrapani 分享 收藏
Preclinical to Clinical Translation of Antibody-Drug Conjugates Using PK/PD Modeling: a Retrospective Analysis of Inotuzumab Ozogamicin 使用PK/PD建模的抗体-药物结合物的临床前到临床翻译: Inotuzumab Ozogamicin的回顾性分析 Betts, Alison M.; Haddish-Berhane, Nahor; Tolsma, John; Jasper, Paul; King, Lindsay E.; Sun, Yongliang; Chakrapani, Subramanyam; Shor, Boris; Boni, Joseph; Johnson, Theodore R. 分享 收藏
Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability Pettersson, Martin; Johnson, Douglas S.; Humphrey, John M.; Butler, Todd W.; Ende, Christopher W. Am; Fish, Benjamin A.; Green, Michael E.; Kauffman, Gregory W.; Mullins, Patrick B.; O'Donnell, Christopher J.; Stepan, Antonia F.; Stiff, Cory M.; Subramanyam, Chakrapani; Tran, Tuan P.; Vetelino, Beth Cooper; Yang, Eddie; Xie, Longfei; Bales, Kelly R.; Pustilnik, Leslie R.; Steyn, Stefanus J.; Wood, Kathleen M.; Verhoest, Patrick R. 分享 收藏
Discovery of Cytotoxic Dolastatin 10 Analogues with N-Terminal Modifications Maderna, Andreas; Doroski, Matthew; Subramanyam, Chakrapani; Porte, Alexander; Leverett, Carolyn A.; Vetelino, Beth C.; Chen, Zecheng; Risley, Hud; Parris, Kevin; Pandit, Jayvardhan; Varghese, Alison H.; Shanker, Suman; Song, Cynthia; Sukuru, Sai Chetan K.; Farley, Kathleen A.; Wagenaar, Melissa M.; Shapiro, Michael J.; Musto, Sylvia; Lam, My-Hanh; Loganzo, Frank; O'Donnell, Christopher J. 分享 收藏
Design, Synthesis, and Pharmacological Evaluation of a Novel Series of Pyridopyrazine-1,6-dione γ-Secretase Modulators Pettersson, Martin; Johnson, Douglas S.; Subramanyam, Chakrapani; Bales, Kelly R.; Ende, Christopher W. Am; Fish, Benjamin A.; Green, Michael E.; Kauffman, Gregory W.; Mullins, Patrick B.; Navaratnam, Thayalan; Sakya, Subas M.; Stiff, Cory M.; Tran, Tuan P.; Xie, Longfei; Zhang, Liming; Pustilnik, Leslie R.; Vetelino, Beth C.; Wood, Kathleen M.; Pozdnyakov, Nikolay; Verhoest, Patrick R.; O'Donnell, Christopher J. 分享 收藏
Ligand-Protein Interactions of Selective Casein Kinase 1δ Inhibitors Mente, Scot; Arnold, Eric; Butler, Todd; Chakrapani, Subramanyam; Chandrasekaran, Ramalakshmi; Cherry, Kevin; DiRico, Ken; Doran, Angela; Fisher, Katherine; Galatsis, Paul; Green, Michael; Hayward, Matthew; Humphrey, John; Knafels, John; Li, Jianke; Liu, Shenping; Marconi, Michael; McDonald, Scott; Ohren, Jeff; Paradis, Vanessa; Sneed, Blossom; Walton, Kevin; Wager, Travis 分享 收藏
Tumor cells selected for resistance to an antibody-drug conjugate retain sensitivity to ADCs with modified linkers and payloads. Tan, Xingzhi; Jin, Guixian; Myers, Jeremy; Diesl, Veronica; Follettie, Max; Lam, Mv-Hanh; Musto, Sylvia; Khandke, Kiran; Charati, Manoj; Graziani, Edmund; Maderna, Andreas; Subramanyam, Chakrapani; Koehn, Frank; Dushin, Russell; Arndt, Kim; O'Donnell, Christopher J.; Gerber, Hans-Peter; Loganzo, Frank 分享 收藏