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Residue-Selective Inhibitors Discovery via Covalent DNA-Encoded Chemical Libraries with Diverse Warheads

Covalent Modifiers

Xinyuan Wu, Jiayi Pan, Rufeng Fan, Yiwei Zhang, Chao Wang, Guoliang Wang, Jiaxiang Liu, Mengqing Cui, Jinfeng Yue, Rui Jin, Zhiqiang Duan, Mingyue Zheng, Lianghe Mei, Lu Zhou, Minjia Tan, Jing Ai, and Xiaojie Lu Journal of the American Chemical Society 2025 147 (18), 15469-15481 DOI: 10.1021/jacs.5c01712

DNA 147
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Researchers devise new way to target and correct disease-related proteins

Broad Institute

By Leah Eisenstadt January 6, 2025 Credit: Courtesy of the Xavier and Schreiber labs. Also featured are the FKBP12 binding motif (light blue triangle), the DNA barcode (red double helix), and the combinatorial library element (red hexagon). Online Jan 2, 2025. Paper cited Tan ZY, et al. Cell Chemical Biology.

Disease 139
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Rational Design of CDK12/13 and BRD4 Molecular Glue Degraders

Covalent Modifiers

2025 , e202508427. Nathanael Schiander Gray , Zhe Zhuang , Woong Sub Byun , Zuzanna Kozicka , Katherine Donovan , Brendan Dwyer , Abby Thornhill , Hannah Jones , Zixuan Jiang , Xijun Zhu , Eric Fischer , Nicolas Thomä , Angew.

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Allosteric Covalent Inhibitors of the STAT3 Transcription Factor from Virtual Screening

Covalent Modifiers

Keserű ACS Medicinal Chemistry Letters 2025 16 (6), 991-997 DOI: 10.1021/acsmedchemlett.4c00622 Here, we have targeted a sparsely studied binding site at the junction of the coiled-coil and DNA-binding domains and discovered several new lead-like covalent inhibitors by virtual screening. Mihalovits, László Petri, Qirat F.

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NGS is evolving: collaboration and tech lead the way

Drug Target Review

Their latest assay processes four to 24 libraries per batch and detects gene amplifications, fusions, deletions and other cancer biomarkers from both DNA and RNA inputs. Their latest assay processes four to 24 libraries per batch and detects gene amplifications, fusions, deletions and other cancer biomarkers from both DNA and RNA inputs.

RNA 92
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Covalent Destabilizing Degrader of AR and AR-V7 in Androgen-Independent Prostate Cancer Cells

Covalent Modifiers

Nomura Journal of the American Chemical Society 2025 DOI: 10.1021/jacs.5c02801 However, these compounds cannot therapeutically access largely intrinsically disordered truncated splice variants of AR, such as AR-V7, which only possess the N-terminal transactivation domain and DNA-binding domain and are missing the ligand-binding domain.

DNA 130
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Scientists engineer CRISPR enzymes that evade the immune system

Broad Institute

Scientists engineer CRISPR enzymes that evade the immune system By Allessandra DiCorato January 9, 2025 Breadcrumb Home Scientists engineer CRISPR enzymes that evade the immune system The new genome-editing tools could lead to safer, more efficient gene therapies. Online January 2, 2025. Tan Molecular Therapeutics Center at MIT.