Results 91 to 100 of about 11,341 (256)

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

Affinity Purification of Biologically Active andInactive Forms of Recombinant Human Protein C Produced in Porcine Mammary Gland [PDF]

, 1996
Recombinant human protein C (rhPC) secreted in the milk of transgenic pigs was studied. \u27Ikansgenes having different regulatory elements of the murine milk protein, whey acidic protein, were used with cDNA and genomic human protein C (hPC) DNA ...
Drohan, William N, Gwazdauskas, Francis C, Lee, Tim, Jerome Holland Laboratory, American Red Cross, Rockville, MD 20855, USA, Lubon, Henryk, Van Cott, Kevin E., Velander, William H., Williams, Barry, Department of Chemical Engineering,Virginia Tech University, Blacksburg, VA 24061, USA   +6 more
core   +1 more source

Androgen Receptor‐Induced Lactoferrin Accelerates Prostate Tumorigenesis Through Modulating Ferroptosis

Advanced Science, EarlyView.
This study demonstrates that transcription factor androgen receptor (AR) directly binds the LF promoter, driving lactoferrin overexpression to promote ferritin (FTH1/FTL) upregulation and inhibit p53‐ALOX12‐mediated ferroptosis in prostate cancer. Lactoferrin could be a new potential therapeutic target in prostate cancer.
Can Liu, Qiu Peng, Xiaoyue Zhang, Zhengshuo Li, Yangge Wu, Yuqing Wen, Run Zheng, Shuanglong Wu, Chenfei Zhou, Zhengyu Hu, Lanjun Shu, Xinyi Ma, Qiuyang Li, Ya Ma, Chunlin Ou, Ming Zhao, Songqing Fan, Lingyu Wei, Jian Ma   +18 more
wiley   +1 more source

Advantages of PROTACs in achieving selective degradation of homologous protein families

Beilstein Journal of Organic Chemistry
Proteolysis-targeting chimeras (PROTACs) have emerged as a promising therapeutic modality and now represent an important addition to the toolkit of medicinal chemists.
Luxi Yang, Xinfei Mao, Jingyi Zhang, Jing Shu, Wenhai Huang, Xiaowu Dong, Yinqiao Chen, Mingfei Wu   +7 more
doaj   +1 more source

De Novo Design of an Androgen Receptor DNA Binding Domain‐Targeted peptide PROTAC for Prostate Cancer Therapy

Advanced Science, 2022
Androgen receptor splice variant‐7 (AR‐V7), one of the major driving factors, is the most attractive drug target in castration‐resistant prostate cancer (CRPC). Currently, no available drugs efficiently target AR‐V7 in clinical practice.
Bohan Ma, Yizeng Fan, Dize Zhang, Yi Wei, Yanlin Jian, Donghua Liu, Zixi Wang, Yang Gao, Jian Ma, Yule Chen, Shan Xu, Lei Li   +11 more
doaj   +1 more source

Leveraging Macrophage Metabolic Reprogramming for Enhanced Anti‐Tumor Immunity

Advanced Science, EarlyView.
Tumor‐associated macrophages (TAMs) are key regulators of the tumor microenvironment (TME), with their metabolic states playing a critical role in tumor progression or regression. This review summarizes current understanding of TAM metabolic plasticity alongside cutting‐edge bioengineering innovations, outlining a roadmap for transforming the ...
Zhiyun Liu, Lingyao Zeng, Xulin Gan, Yilin Zhou, Han Shen, Dan Wu, Xin Shou, Minmin Jiang, Liyun Shi   +8 more
wiley   +1 more source

BRAFV600E‐PROTAC versus inhibitors in melanoma cells: Deep transcriptomic characterization

Clinical and Translational Medicine
Aims This study compares the suppression of Mitogen‐activated protein kinase (MAPK) signalling and early resistance potential between a proteolysis‐targeting chimera (PROTAC) and inhibitors targeting BRAFV600E.
Solomon O. Alhassan, Zakaria Y. Abd Elmageed, Youssef Errami, Guangdi Wang, Joe A. Abi‐Rached, Emad Kandil, Mourad Zerfaoui   +6 more
doaj   +1 more source

From PROTAC to TPD: Advances and Opportunities in Targeted Protein Degradation

Pharmaceuticals
PROTAC is a rapidly developing engineering technology for targeted protein degradation using the ubiquitin–proteasome system, which has promising applications for inflammatory diseases, neurodegenerative diseases, and malignant tumors. This paper gives a
Siqi Wang, Fuchu He, Chunyan Tian, Aihua Sun   +3 more
doaj   +1 more source

Strongly enhanced atomic parity violation due to close levels of opposite parity

, 2014
We present calculations of nuclear-spin-dependent and nuclear-spin-independent parity violating amplitudes in Ba, Ra, Ac+, Th and Pa. Parity nonconservation in these systems is greatly enhanced due to the presence of very close electronic energy levels ...
Dzuba, V. A., Flambaum, V. V., Roberts, B. M.   +2 more
core   +1 more source

Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader [PDF]

, 2019
Inducing post-translational protein knockdown is an important approach to probe biology and validate drug targets. An efficient strategy to achieve this involves expression of a protein of interest fused to an exogenous tag, allowing tag-directed ...
Alessi, Dario, Ciulli, Alessio, Macartney, Thomas, Maniaci, Chiara, Prescott, Alan, Testa, Andrea, Tovell, Hannah, Zhou, Houjiang   +7 more
core   +4 more sources