Results 81 to 90 of about 13,155 (273)

Targeted protein degradation in cancers: Orthodox PROTACs and beyond

The Innovation, 2023
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology can be used to target proteins by hijacking the ubiquitin-proteasome ...
Jin Li, Xinxin Chen, Aiping Lu, Chao Liang   +3 more
doaj   +1 more source

MRF4 negatively regulates adult skeletal muscle growth by repressing MEF2 activity [PDF]

, 2016
The myogenic regulatory factor MRF4 is highly expressed in adult skeletal muscle but its function is unknown. Here we show that Mrf4 knockdown in adult muscle induces hypertrophy and prevents denervation-induced atrophy.
Abraham, Reimar, Agatea, Lisa, Akimoto, Takayuki, Bicciato, Silvio, Blaauw, Bert, Calabria, Elisa, Carvajal, Jaime J., Ciciliot, Stefano, Dyar, Kenneth A., Forcato, Mattia, Moretti, Irene, Murgia, Marta, Pierre, Philippe, Rigby, Peter W. J., Schiaffino, Stefano, Uhlenhaut, N. Henriette   +15 more
core   +5 more sources

Understanding and Overcoming Antibody‐Drug Conjugate Resistance: Biological Mechanisms and Emerging Analytical Frameworks in Breast Cancer

Advanced Science, EarlyView.
Antibody–drug conjugates (ADCs) transform breast cancer therapy, yet resistance limits their durability. Emerging evidence reveals that ADC failure is not solely tumor‐intrinsic but shaped by dynamic tumor–microenvironment interactions that alter drug delivery, processing, and response.
Minji Seo, Jangsoon Lee, Naoto T. Ueno
wiley   +1 more source

Targeting STAT3 with Proteolysis Targeting Chimeras and Next-Generation Antisense Oligonucleotides

Molecular Cancer Therapeutics, 2021
AbstractSTAT3 has been recognized for its key role in the progression of cancer, where it is frequently upregulated or constitutively hyperactivated, contributing to tumor cell proliferation, survival, and migration, as well as angiogenesis and suppression of antitumor immunity.
Shiah, Jamie V, Grandis, Jennifer R, Johnson, Daniel E   +2 more
openaire   +5 more sources

Halofuginone is a Molecular Glue Degrader of Integrin β4

Advanced Science, EarlyView.
Integrin β4 overexpression is linked to aggressive tumors and poor prognosis, but targeted therapies are lacking. We identified halofuginone (HF) as a molecular glue degrader that promotes integrin β4 degradation via the CRL4BWDR18 E3 ligase. HF suppresses tumor progression in vitro and in vivo, offering a new strategy for targeting oncogenic ...
Wei Gong, Di Yang, Junrui Tian, Yufei Chai, Tiantian Yu, Qingnan Wu, Yan Wang, Weimin Zhang, Qimin Zhan   +8 more
wiley   +1 more source

Proteolysis of the type III glutamine synthetase from Bacteroides fragilis causes expedient crystal-packing rearrangements [PDF]

, 2016
This work details the intentional modifications that led to the first structure of a type III glutamine synthetase enzyme (GSIII). This approach followed the serendipitous discovery of digestion caused by an extracellular protease from a contaminating ...
Abratt, Valarie, Belrhali, Hassan, Sewella, Trevor B, van Rooyen, Jason   +3 more
core  

Membrane anchoring stabilizes and favors secretion of New Delhi metallo-β-lactamase [PDF]

, 2015
Carbapenems, 'last-resort' β-lactam antibiotics, are inactivated by zinc-dependent metallo-β-lactamases (MBLs). The host innate immune response withholds nutrient metal ions from microbial pathogens by releasing metal-chelating proteins such as ...
A Kovacs-Simon, A Rokney, Alejandro J Vila, B Johne, BD Corbin, C Rumbo, C Schwechheimer, C Zhang, CA Schneider, D King, Elizabeth M Nolan, G Fiorilli, G Patel, G Periyannan, Guillermo Bahr, HJ Bootsma, J Morán-Barrio, JE Irazoqui, JM Bomberger, JM González, JM González, K Hede, KH Choi, KP Haley, L Dortet, L Poirel, LB Randall, Lisandro J González, LJ González, M Cerasi, M Hernandez Valladares, M Hussain, M Park, MB Brophy, ME Kovach, MF Haurat, MI Hood, MR Meini, MS Aschtgen, MW Crowder, N Selevsek, NC Kesty, P Marchiaro, P Ravasi, PD Veith, PS Borra, R Gläser, R Kitagawa, Robert A Bonomo, S Devos, S Santos, S Tottey, S Wommer, TA Murphy, Toshiki G Nakashige, TR Walsh, TR Walsh, V Schaar, V Schaar, VG Pederick, X Chen, Y Kim, Y Luo, Z Hu   +63 more
core   +3 more sources

Cryo‐EM Structure Guided Engineering of Botulinum Neurotoxin A With Advanced Receptor Binding Affinity and Therapeutical Benefits

Advanced Science, EarlyView.
The butterfly unfolded wing in an open form structure of botulinum neurotoxin type A (BoNT/A) at physiological‐state was confirmed at 2.85 Å resolution by cryo‐electron microscopy (cryo‐EM). Structure‐guided protein engineering significantly enhanced the receptor‐binding affinity, therapeutic efficacy, and safety of the engineered toxin variants ...
Wenrui Wang, Zhaxi Zerang, Linjin You, Ziye Liu, Rong Nie, Fuwei Qi, Fenfen Gao, Chengmu Zhao, Wantong Ma, Jinghan He, Xiaoru Wang, Shanquan Wu, Bo Liu, Xinyao Liu, Dongsheng Lei, Dejuan Zhi, Dongsheng Wang   +16 more
wiley   +1 more source

Ubiquitous regulation of cerebrovascular diseases by ubiquitin‐modifying enzymes

Clinical and Translational Medicine
Cerebrovascular diseases (CVDs) are a major threat to global health. Elucidation of the molecular mechanisms underlying the pathology of CVDs is critical for the development of efficacious preventative and therapeutic approaches.
Jingyong Huang, Zhenhu Zhu, Dirk Schlüter, Kate Lykke Lambertsen, Weihong Song, Xu Wang   +5 more
doaj   +1 more source

IRT5 Probiotics Changes Immune Modulatory Protein Expression in the Extraorbital Lacrimal Glands of an Autoimmune Dry Eye Mouse Model [PDF]

, 2020
PURPOSE. While the association between the gut microbiome and the immune system has been studied in autoimmune disorders, little is known about ocular disease.
Choi, Se Hyun, IM, SIN HYEOG, Kim, Hye Min, Kim, Kwang Pyo, Kim, Mee Kum, Oh, Jae Won, Ryu, Jin Suk   +6 more
core   +1 more source