Results 121 to 130 of about 13,155 (273)

Aspergillus nidulans ambient pH signaling does not require endocytosis

, 2015
9 p.-6 fig.-1 tab.Aspergillus nidulans (Pal) ambient pH signaling takes place in cortical structures containing components of the ESCRT pathway, which are hijacked by the alkaline pH-activated, ubiquitin-modified version of the arrestin-like protein PalF
Arst, HN, Galindo, A, Lucena-Agell, D, Penalva, MA   +3 more
core   +1 more source

Effective targeting of the survivin dimerization interface with small molecule inhibitors [PDF]

, 2016
Many oncoproteins are considered undruggable because they lack enzymatic activities. In this study, we present a small-molecule–based anticancer agent that acts by inhibiting dimerization of the oncoprotein survivin, thereby promoting its degradation ...
Dong, Zizheng, Liu, Jianguo, Liu, Jingyuan, Peery, Robert C., Qi, Jing, Zhang, Jian-Ting, Zhang, Shaobo   +6 more
core   +1 more source

A Plug‐and‐Play Platform for Customizing Multivalent Degraders and Degrader‐Drug Conjugates

Advanced Science, EarlyView.
Membrane proteins remain challenging targets for conventional TPD approaches. Here, the authors develop UPTAB, a modular platform leveraging ultrahigh‐affinity orthogonal Im/CL protein pairs for lysosomal degradation of membrane proteins. Mono‐targeted (Type‐I), dual‐targeted (Type‐II), and tri‐targeted (Type‐III) UPTABs enable simultaneous degradation
Mengqing Zhao, Yan Deng, Jianjian Han, Yong Xie, Kai Bao, Lixin Ma, Lilong Liu, Wuxiang Mao   +7 more
wiley   +1 more source

BCMA‐Engineered Dendritic Cell‐Derived Exosomes as Bi‐Functional Therapeutics Orchestrating Cytokine Sequestration and Immune Activation for Multiple Myeloma

Advanced Science, EarlyView.
A dual‐function cell‐free therapeutic based on DC2.4 cell‐derived exosomes engineered to display BCMA. (Left) Soluble Ligand Sequestration (Decoy Function): DB Exo act as molecular decoys that predominantly sequester soluble APRIL with partial BAFF attenuation, effectively disrupting the NF‐κB survival signaling axis and suppressing myeloma cell ...
Yuqing Zeng, Chao He, Zhibin He, Hongbo Chen, Fang Cheng, Yongjiang Zheng   +5 more
wiley   +1 more source

Characterization of Hsp70 binding and nucleotide exchange by the yeast Hsp110 chaperone Sse1. [PDF]

, 2006
SSE1 and SSE2 encode the essential yeast members of the Hsp70-related Hsp110 molecular chaperone family. Both mammalian Hsp110 and the Sse proteins functionally interact with cognate cytosolic Hsp70s as nucleotide exchange factors.
Morano, Kevin A, Shaner, Lance, Sousa, Rui   +2 more
core   +1 more source

Effect of carbamazepine on the pharmacokinetics of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader, in healthy adults

British Journal of Clinical Pharmacology, EarlyView.
Aim To evaluate the effects of carbamazepine, a strong cytochrome P450 (CYP)3A4 inducer, on the pharmacokinetics and safety of vepdegestrant, a PROteolysis TArgeting Chimera estrogen receptor degrader. Methods This was a phase 1, open‐label, fixed‐sequence, two‐period study in healthy adult participants.
Hechuan Wang, Jennifer A. Winton, Kyle T. Matschke, Alexandre Stouffs, Kimberly C. Lee, Yuanyuan Zhang, Wenlian Qiao, Weiwei Tan   +7 more
wiley   +1 more source

Perspectives of autophagy-tethering compounds (ATTECs) in drug discovery

Medicine Plus
Degrader technologies provide unprecedented strategies to tackle diseases caused by pathogenic proteins that are difficult to target by the traditional inhibitor approach.
Yu Ding, Dong Xing, Yiyan Fei, Shouqing Luo, Boxun Lu   +4 more
doaj   +1 more source

RNA recognition by human TLR8 can lead to autoimmune inflammation. [PDF]

, 2013
Studies on the role of the RNA receptor TLR8 in inflammation have been limited by its different function in human versus rodents. We have generated multiple lines of transgenic mice expressing different levels of human TLR8. The high copy number chimeras
Ablasser, Alma-Martina Cepika, Barbalat, Barrat, Berry, Campbell, Cassidy, Chad Crain, Christensen, Claudio Tripodo, Cristiana Guiducci, Deane, Demaria, Döring, Ewald, Finkelberg, Forsbach, Franck J. Barrat, Fukui, Ganguly, Gantier, Gorden, Guiducci, Guiducci, Hattermann, Heil, Hemmi, Janke, John J. Cush, Lan, Liu, Lynda Bennett, Maschalidi, Mei Gong, Mellins, Mouchess, Nickerson, Pascual, Pierre Quartier, Pisitkun, Prinz, Quartier, Robert L. Coffman, Sacre, Sarvestani, Sparwasser, Subramanian, Virginia Pascual, Vollmer, Walsh, Wang, Zandieh, Zhaohui Xu   +52 more
core   +2 more sources

Engineering Murine Cross‐Reactivity Into an Affibody to Human Death Receptor 5

Biotechnology and Bioengineering, EarlyView.
ABSTRACT Interspecies cross‐reactive protein therapeutics that target conserved epitopes across species are critical for translational research. The present study showcases the engineering of an affibody molecule, originally discovered for binding to human death receptor 5 (hDR5) with 94 nM affinity, to simultaneously acquire cross‐reactivity to murine
Tse‐Han Kuo, Nagamani Vunnam, Jonathan N. Sachs, Benjamin J. Hackel   +3 more
wiley   +1 more source

Interpretable PROTAC Degradation Prediction With Structure‐Informed Deep Ternary Attention Framework

Advanced Science
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional ligands bridging Proteins‐Of‐Interest (POIs) and E3 ligases for ubiquitin‐proteasome degradation, promising to target the ‘undruggable’.
Zhenglu Chen, Chunbin Gu, Shuoyan Tan, Xiaorui Wang, Yuquan Li, Mutian He, Ruiqiang Lu, Shijia Sun, Chang‐Yu Hsieh, Xiaojun Yao, Huanxiang Liu, Pheng‐Ann Heng   +11 more
doaj   +1 more source