Results 41 to 50 of about 823,777 (226)
Acta Materia Medica, 2023 Viral infections represent a major threat to human health and the global economy; however, most of the currently available antiviral drugs are not fully effective in restricting viral replication and selecting for drug-resistant variants.
Yang Zhou +6 more
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Versatile Nano‐PROTAC‐Induced Epigenetic Reader Degradation for Efficient Lung Cancer Therapy
Advanced Science, 2022 Recent evidence has indicated that overexpression of the epigenetic reader bromodomain‐containing protein 4 (BRD4) contributes to a poor prognosis of lung cancers, and the suppression of its expression promotes cell apoptosis and leads to tumor shrinkage.
Huan‐Tian Zhang +10 more
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PROteolysis TArgetting Chimeras (PROTACs) Strategy Applied to Kinases: Recent Advances [PDF]
Advanced Therapeutics, 2020 AbstractSince the development of the first protein kinase inhibitor in the early 1980s, followed by the FDA approval of imatinib in 2001, kinases are one of the most intensively pursued targets in current medicinal chemistry research. These proteins are overrepresented in various diseases such as cancer, inflammation or autoimmune pathologies and play ...
Feral, Anthony +3 more
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PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future
Drug Discovery Today: Technologies, 2019 The majority of currently used therapeutics are small molecule-based and utilize occupancy-driven pharmacology as the mode of action (MOA), in which the protein function is modulated via temporary inhibition. New modalities that operate using alternative MOAs are essential for tapping into the "undruggable" proteome.
Mariell Pettersson, Craig M. Crews
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, 2022 Enhancer of zeste homolog 2 (EZH2), a catalytic subunit of polycomb repressive complex 2 (PRC2), is overexpressed in triple-negative breast cancer (TNBC), correlating with poor prognosis.
Chengwei Zhang (573927) +10 more
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Acta Pharmaceutica Sinica BIn light of the burgeoning successes of cancer immunotherapy, glioblastoma (GBM) remains refractory due to an immunosuppressive microenvironment originating from its molecular heterogeneity.
Yeongji Jang +13 more
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PROTACs: A novel strategy for cancer drug discovery and development
MedComm, 2023 Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists of three components: a small molecule that binds to a target protein, an ...
Xin Han, Yi Sun
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Neural Regeneration Research, 2021 Neurological diseases such as stroke, Alzheimer’s disease, Parkinson’s disease, and Huntington’s disease are among the intractable diseases for which appropriate drugs and treatments are lacking.
Ke Ma +3 more
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Self-Assembled Nano-PROTAC Enables Near-Infrared Photodynamic Proteolysis for Cancer Therapy
, 2023 Confining the protein degradation activity of proteolysis-targeting chimera (PROTAC) to cancer lesions ensures precision treatment. However, it still remains challenging to precisely control PROTAC function in tumor regions in vivo.
Weishan Wang (2698738) +11 more
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Antiviral PROTACs: Opportunity borne with challenge
Cell Insight, 2023 Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of the ubiquitin-proteasome-system has become a promising strategy in drug design. The overwhelming advantages of PROTAC technology have ensured a rapid and wide usage,
Jinsen Liang +6 more
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