Results 61 to 70 of about 5,184,182 (156)

Cell-type specific, inducible and acute degradation of targeted protein in mice by two degron systems

Nature Communications
Despite its broad application in in vitro studies, the application of targeted protein degradation (TPD) to animal models faces considerable challenges. Here, we develop inducible and cell-type specific TPD systems in mice using two degron systems: Oryza
Motoi Yamashita, Chihiro Ogawa, Baihao Zhang, Tetsuro Kobayashi, Aneela Nomura, Clive Barker, Chengcheng Zou, Satoshi Yamanaka, Ken-ichiro Hayashi, Yoichi Shinkai, Kazuyo Moro, Sidonia Fargarasan, Koshi Imami, Jun Seita, Fumiyuki Shirai, Tatsuya Sawasaki, Masato T. Kanemaki, Ichiro Taniuchi   +17 more
doaj   +1 more source

Molecular Glue Degraders in Early Development for Cancer Therapy

Medicinal Research Reviews, EarlyView.
ABSTRACT Molecular glue degraders are an emerging class of small molecule allosteric modulators that induce or stabilize protein‐protein interactions, enabling targeted degradation of previously intractable proteins. By redirecting E3 ligases to recognize neosubstrates, proteins that are not typically recognized by a specific E3 ubiquitin ligase, they ...
E. Sila Ozdemir, Hyunbum Jang, Ozlem Keskin, Attila Gursoy, Ruth Nussinov   +4 more
wiley   +1 more source

PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators

Journal of Enzyme Inhibition and Medicinal Chemistry
The degradation of overexpressed proteins has emerged as a promising strategy for halting disease progression, particularly in cancer. Traditional small-molecule drugs often face limitations in the elimination of pathogenic proteins, leading to the ...
Sunny Periyasamy, Thyla Jarrett, Joe Truong, Rachid Skouta   +3 more
doaj   +1 more source

Developing a toolkit for conditional targeted protein degradation with protease and sortase a responsiveness for cellular reprogramming

Chen, WilfredSmall molecule inhibitors have been a mainstay of pharmaceutical products since the inception of the industry. Breakout examples include penicillin, aspirin, and naproxen sodium. However, the successful development of small molecule programs
Yang, Hopen K.
core   +1 more source

Molecular glues: Recent advances in cereblon substrate identification and mechanistic insights

Smart Molecules, EarlyView.
Molecular glues exert diverse core biological functions by inducing or stabilizing protein–protein interactions, extending far beyond the traditional scope of targeted protein degradation. Key breakthroughs include expanded cereblon substrate recognition, sustained G protein‐coupled receptor megacomplex signaling, and the first orthosteric molecular ...
Qingyun Guan, Xiaoyu Shi, Qian Yang, Xiangyi Jiang, Xinyong Liu, Peng Zhan   +5 more
wiley   +1 more source

A guide to transcriptional cyclin‐dependent kinases in cancer

The FEBS Journal, EarlyView.
Transcriptional cyclin‐dependent‐kinases (tCDKs) facilitate gene expression by promoting RNA polymerase II (RNAPII) progression through discrete phases of the transcription cycle. Aberrant tCDK activity is detectable in different human cancers, thereby contributing to de‐regulated gene expression programs that drive oncogenic phenotypes.
Jennifer R. Devlin, Salla Kyheröinen, Ricky W. Johnstone   +2 more
wiley   +1 more source

Molecular glue-mediated targeted protein degradation: A novel strategy in small-molecule drug development

iScience
Summary: Small-molecule drugs are effective and thus most widely used. However, their applications are limited by their reliance on active high-affinity binding sites, restricting their target options.
Xueqiang Tan, Zuyi Huang, Hairun Pei, Zongchao Jia, Jimin Zheng   +4 more
doaj   +1 more source

Limiting Trial‐and‐Error: Linker‐Based 2D Descriptor Analysis to Support Very Early Proteolysis‐Targeting Chimeras Design

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
Can simple linker descriptors guide PROTAC design? Analysis of matched CRBN‐ and VHL‐recruiting degraders shows that basic 2D linker properties may capture trends linked to degradation efficiency, in vitro ADME and physicochemical properties. A practical approach to reduce trial‐and‐error in early targeted protein degradation programs. Targeted protein
Giulia Apprato, Serena Traversa, Giulia Caron, Giuseppe Ermondi   +3 more
wiley   +1 more source

The Expanding Role of Diazirines in Synthetic Methodology

European Journal of Organic Chemistry, Volume 29, Issue 38, 13 October 2026.
Beyond their established role in photoaffinity labeling, diazirines have emerged as versatile reagents in synthetic chemistry. This review highlights their dual reactivity as carbene and nitrogen‐transfer precursors, showcasing mechanistic insights and diverse applications in cyclopropanations, cycloadditions, skeletal editing, amination, heterocycle ...
Viktor Savic, Dominik Schnalzer, Marko D. Mihovilovic, Michael Schnürch   +3 more
wiley   +1 more source

Design principles for optogenetic-based targeted protein degradation

Synthetic and Systems Biotechnology
Precise regulation of protein abundance is essential for understanding dynamic cellular processes and for advancing therapeutic development. However, existing approaches lack the spatiotemporal resolution required to these cellular processes.
Yunyue Chen, Siyifei Wang, Leiying Xie, Luhao Zhang, Min Zhu, Yingke Xu   +5 more
doaj   +1 more source