Results 221 to 230 of about 11,335 (243)

PI3K PROTAC overcomes the lapatinib resistance in PIK3CA-mutant HER2 positive breast cancer.

Cancer Letters
Although anti-HER2 therapy has made significant strides in reducing metastasis and relapse in HER2-positive breast cancer, resistance to agents like trastuzumab, pertuzumab, and lapatinib frequently develops in patients undergoing treatment.
Hongyan Zhang, Longlong Zhang, Yuna He, Dewei Jiang, Jian Sun, Qianmei Luo, Huichun Liang, Tiantian Wang, Fubing Li, Yu Tang, Zimo Yang, Wenjing Liu, Yu Rao, Ceshi Chen   +13 more
semanticscholar   +1 more source

Application and challenges of nitrogen heterocycles in PROTAC linker.

European journal of medicinal chemistry
The absence of effective active pockets makes traditional molecularly targeted drug strategies ineffective against 80 % of human disease-related proteins.
Yang Li, Junfeng Qu, Lizhi Jiang, Xiaoyu Peng, Kaiyue Wu, Miao Chen, Yuanyuan Peng, Xuan Cao   +7 more
semanticscholar   +1 more source

Efficient PROTAC-ing: combinational use of PROTACs with signaling pathway inhibitors

Trends in Biochemical Sciences
Targeted protein degradation is an innovative therapeutic modality for the degradation of disease-causing proteins. In a recent report combining high-throughput screening of small-molecule compounds and biochemical analyses, Mori et al. identified certain inhibitors of cellular pathways, such as PARylation and proteostatic pathways, which enhance ...
openaire   +2 more sources

Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2.

European journal of medicinal chemistry
Aberrant expression of EZH2, the main catalytic subunit of PRC2, has been implicated in numerous cancers, including leukemia, breast, and prostate. Recent studies have highlighted non-catalytic oncogenic functions of EZH2, which EZH2 catalytic inhibitors
J. Velez, Brandon Dale, Kwang-su Park, H. Kaniskan, Xufen Yu, Jian Jin   +5 more
semanticscholar   +1 more source

Discovery of Effective Dual PROTAC Degraders for Neurodegenerative Disease-Associated Aggregates.

Journal of Medicinal Chemistry
The aggregation of specific proteins is a histopathological hallmark in various neurodegenerative diseases (NDs), among which Alpha-synuclein (α-Syn) and tau have received increased attention.
Wentao Zhu, Wenqian Zhang, Jian Chen, Yichen Tong, Fang Xu, Jiyan Pang   +5 more
semanticscholar   +1 more source

Advancing Proteolysis Targeting Chimera (PROTAC) Nanotechnology in Protein Homeostasis Reprograming for Disease Treatment.

ACS Nano
Proteolysis targeting chimeras (PROTACs) represent a transformative class of therapeutic agents that leverage the intrinsic protein degradation machinery to modulate the hemostasis of key disease-associated proteins selectively.
Meng-Hao Wu, Yilan Zhao, Chi Zhang, Kanyi Pu   +3 more
semanticscholar   +1 more source

Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity

Nature Communications
Proteolysis-targeting chimeras (PROTACs) have been explored for the degradation of drug targets for more than two decades. However, only a handful of E3 ligase substrate receptors have been efficiently used. Downregulation and mutation of these receptors
M. Mabanglo, Brian J. Wilson, Mahmoud Noureldin, S. Kimani, A. Mamai, Chiara Krausser, Héctor González-Álvarez, Smriti Srivastava, Mohammed Mohammed, Laurent Hoffer, Manuel Chan, Jamie Avrumutsoae, A. Li, T. Hajian, Sarah Tucker, S R Green, Magdalena M. Szewczyk, Dalia Barsyte-Lovejoy, V. Santhakumar, S. Ackloo, P. Loppnau, Yanjun Li, Alma Seitova, T. Kiyota, Jue Wang, Gilbert G. Privé, Douglas A. Kuntz, Bhashant Patel, Vaibhavi Rathod, Anand Vala, Bhimsen Rout, A. Aman, Gennady Poda, D. Uehling, J. Ramnauth, L. Halabelian, Richard Marcellus, R. Al-Awar, M. Vedadi   +38 more
semanticscholar   +1 more source

Liposomal STAT3-Degrading PROTAC Prodrugs Promote Anti-Hepatocellular Carcinoma Immunity via Chemically Reprogramming Cancer Stem Cells.

Nano letters (Print)
Cancer stem cells (CSCs) with hyperactivated signal transducer and activator of transcription 3 (STAT3) are a major driver of hepatocellular carcinoma (HCC).
Xuan Wang, Youbo Zhao, Xin Li, Qiqi Zhang, Jinming He, Yingqi Liu, Menghuan Li, Zhong Luo   +7 more
semanticscholar   +1 more source

A Top-Down Design Approach for Generating a Peptide PROTAC Drug Targeting Androgen Receptor for Androgenetic Alopecia Therapy.

Journal of Medicinal Chemistry
While large-scale artificial intelligence (AI) models for protein structure prediction and design are advancing rapidly, the translation of deep learning models for practical macromolecular drug development remains limited.
Bohan Ma, Donghua Liu, Zhe Wang, Dize Zhang, Yanlin Jian, Kun Zhang, Tianyang Zhou, Yibo Gao, Yizeng Fan, Jian Ma, Yang Gao, Yule Chen, Si Chen, Jing Liu, Xiang Li, Lei Li   +15 more
semanticscholar   +1 more source

Development of PROTAC Degrader Drugs for Cancer

Annual Review of Cancer Biology
The development of novel drug modalities is necessary to overcome the current critical issues in the treatment of cancer, namely toxicity, insufficient efficacy, and the development of resistance.
Vesna Vetma, Suzanne O'Connor, Alessio Ciulli   +2 more
semanticscholar   +1 more source