Results 211 to 220 of about 107,280 (285)

Supplementary Figure S3 from High-Throughput Drug Screening of Clear Cell Ovarian Cancer Organoids Reveals Vulnerability to Proteasome Inhibitors and Dinaciclib and Identifies AGR2 as a Therapeutic Target

Takuma Yoshimura, Takashi Kamatani, Aki Ookubo, Mio Takahashi, Manabu Itoh, Toshiki Ebisudani, Yohei Masugi, Tomomi Toyonaga, Junko Hamamoto, Keiko Saotome, Kensuke Sakai, Tomoko Yoshihama, Nobuko Moritoki, Shinsuke Shibata, Hiroyuki Yasuda, Toshiro Sato, Taka-Aki Sato, Daisuke Aoki, Wataru Yamagami, Tatsuhiko Tsunoda, Tatsuyuki Chiyoda   +20 more
openalex   +1 more source

Potent and Selective IGF‐IIR‐Recruiting Bifunctional Molecules for Targeted Lysosomal Degradation of Extracellular and Membrane Proteins

Advanced Science, EarlyView.
Lysosome‐targeting chimeras (LYTACs) enable degradation of extracellular and membrane proteins via lysosomal trafficking. We report a novel IGF‐II mutant (Del1–7, Y27L) that selectively engages IGF‐IIR while avoiding IGF‐IR and IR‐A. mutIGF‐II–based LYTACs enhance target internalization and degradation and support a genetically encodable, all‐protein ...
Yuan Zhao, Yaxian Liao, Pengyun Li, Regina Stasser de Gonzalez, Xuankun Chen, Nicholas S. Nieto, Florence M. Brunel, Nick Cox, Joseph Stock, Matthew McHenry, Guangsen Fu, Penghsuan Huang, Wenxin Wu, Deqin Cai, Lingjun Li, Alexander N. Zaykov, Weiping Tang   +16 more
wiley   +1 more source

Carmaphycin B-Based Proteasome Inhibitors to Treat Human African Trypanosomiasis: Structure-Activity Relationship and <i>In Vivo</i> Efficacy. [PDF]

ACS Infect Dis
Liu LJ, Francisco KR, Sun YU, Serafim MSM, Amarasinghe DK, Teixeira TR, Lucero B, Kronenberger T, Elsayed W, Elwakeel H, Al-Hindy M, Almaliti J, Gerwick WH, O'Donoghue AJ, Caffrey CR.   +14 more
europepmc   +1 more source

Chaperone‐Mediated Autophagic Degradation of USP9X in Macrophages Exacerbates Postmyocardial Infarction Inflammation and Cardiac Dysfunction

Advanced Science, EarlyView.
This study demonstrates that inflammatory stimuli induce the acetylation‐triggered, chaperone‐mediated autophagic degradation of ubiquitin‐specific peptidase 9 X‐linked (USP9X) in macrophages. USP9X acts as a macrophage “inflammation switch” after myocardial infarction (MI). USP9X loss destabilizes tumor necrosis factor receptor‐associated factor (TRAF)
Biqing Wang, Xiangheng Cai, Mengqi Li, Xue Liu, Junhui Xue, Ye Liu, Ding Ai, Xinyang Hu   +7 more
wiley   +1 more source

Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria. [PDF]

Cell Chem Biol
Lawong A, Gahalawat S, Ray S, Ho N, Han Y, Ward KE, Deng X, Chen Z, Kumar A, Xing C, Hosangadi V, Fairhurst KJ, Tashiro K, Liszczak G, Shackleford DM, Katneni K, Chen G, Saunders J, Crighton E, Casas A, Robinson JJ, Imlay LS, Zhang X, Lemoff A, Zhao Z, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Campbell SF, Fidock DA, Laleu B, Charman SA, Ready JM, Phillips MA.   +33 more
europepmc   +1 more source

Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies

, 2018
Meng Lei, Huayun Feng, Enhe Bai, Hui Zhou, Jia Wang, Jingmiao Shi, Xueyuan Wang, Shihe Hu, Zhaogang Liu, Yongqiang Zhu   +9 more
openalex   +1 more source

Membralin Assembles a MAN1B1–VCP Complex to Target Foreign Glycoproteins from the Endoplasmic Reticulum to Lysosomes for Degradation

Advanced Science, EarlyView.
This study identifies Membralin as an ER‐phagy receptor that recruits MAN1B1 and VCP to form a selective ERLAD complex. By sensing dense N‐glycan clusters on viral fusion glycoproteins, this ubiquitin‐independent pathway directs SARS‐CoV‐2 spike, Ebola GP, influenza HA, and HIV‐1 Env to lysosomal degradation, thereby limiting viral infectivity ...
Jing Zhang, Xiaoran Lu, Sunan Li, Tao Wang, Iqbal Ahmad, Yong‐Hui Zheng   +5 more
wiley   +1 more source

Microglial GPR35 Ameliorates Epileptogenesis and Neuroinflammation via PDGFA Domain 2 Signaling

Advanced Science, EarlyView.
Activation of microglial G protein–coupled receptor 35 (GPR35) by L‐kynurenic acid (L‐Kyna) initiates a platelet‐derived growth factor A (PDGFA)–dependent phosphoinositide 3‐kinase–protein kinase B (PI3K–AKT) signaling cascade that dampens hippocampal neuroinflammation, thereby restraining epileptogenesis, lowering seizure susceptibility, and ...
Qi Wang, Tingting Qu, Qibing Sun, Ran Li, Junfei Dong, Yuming Du, Ziyin Xuan, Lei Wang, Hanli Li, Jianyun Sun, Fangliang Chen, Jinshuai Liu, Zifan Yang, Jianxiang Lei, Qian Yang, Bin Wang, Zhiming Zhou, Yu Wang   +17 more
wiley   +1 more source

GZ17-6.02 interacts with proteasome inhibitors to kill multiple myeloma cells. [PDF]

Oncotarget
Booth L, Roberts JL, West C, Dent P.
europepmc   +1 more source

Proteasome inhibitor ameliorates severe acute pancreatitis and associated lung injury of rats

, 2008
Xi Chen, Shunle Li, Tao Wu, Jidong Liu
openalex   +2 more sources