Explanipedia

Role of tankyrase scaffolding in the β-catenin destruction complex and WNT signaling Open

Qian Wang, Liping Li, Lin You, Lei Han, Yong Lu , et al. · 2025

Aberrant WNT/β-catenin signaling drives tumorigenesis and metastasis in cancer. Although enzymatic inhibitors of tankyrase (TNKS) effectively block AXIN degradation and stabilize the β-catenin destruction complex (DC), they have demonstrat…

Role of tankyrase scaffolding in the β-catenin destruction complex and WNT signaling Open

Qian Wang, Liping Li, Lin You, Shuai Wang, Lei Han , et al. · 2025

Aberrant WNT/β-catenin signaling drives tumorigenesis and metastasis in cancer. Although enzymatic inhibitors of tankyrase (TNKS) effectively block AXIN degradation and stabilize the β-catenin destruction complex (DC), they have demonstrat…

The STING pathway drives noninflammatory neurodegeneration in NGLY1 deficiency Open

Kun Yang, Gustavo Torres-Ramirez, Nicole Dobbs, Jie Han, Makoto Asahina , et al. · 2025

The STING pathway is increasingly recognized as a key regulator of neuroinflammation in neurodegenerative disease, but its role in noninflammatory conditions remains unclear. We generated a postnatal inducible whole-body Ngly1 knockout mou…

CCDC 846595: Experimental Crystal Structure Determination Open

Zhiqiang Ma, Lin You, Chuo Chen · 2025

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …

Corrigendum to “Selective degradation of FGFR1/2 overcomes antiestrogen resistance in ER+ breast cancer with FGFR1/2 alterations” [619 1 (2025) 217668 1–13] Open

Yasuaki Uemoto, Chang-Ching Lin, Bingnan Wang, Dan Ye, Yisheng Fang , et al. · 2025

Identification and removal of a cryptic impurity in pomalidomide-PEG based PROTAC Open

Bingnan Wang, Yong Lu, Chuo Chen · 2025

Chemically induced dimerization is a powerful tool for studying protein function, wherein the IMiD (the “immunomodulatory drug”) class of PROTAC molecules with a PEG linker is frequently used to promote targeted protein degradation. The st…

Orthogonal Hydroxyl Functionalization of cGAMP Confers Metabolic Stability and Enables Antibody Conjugation Open

Yong Lu, Lin You, Liping Li, Jessica A. Kilgore, Shun Liu , et al. · 2023

cGAMP is a signaling molecule produced by the cGAS-DNA complex to establish antimicrobial and antitumor immunity through STING. Whereas STING activation holds potential as a new strategy to treat cancer, cGAMP is generally considered unsui…

Repurposing Iron‐ and 2‐Oxoglutarate‐Dependent Oxygenases to Catalyze Olefin Hydration Open

Bingnan Wang, Yong Lu, Lide Cha, Tzu‐Yu Chen, Philip M. Palacios , et al. · 2023

Mononuclear nonheme iron(II) and 2‐oxoglutarate (Fe/2OG)‐dependent oxygenases and halogenases are known to catalyze a diverse set of oxidative reactions, including hydroxylation, halogenation, epoxidation, and desaturation in primary metab…

Repurposing Iron‐ and 2‐Oxoglutarate‐Dependent Oxygenases to Catalyze Olefin Hydration Open

Bingnan Wang, Yong Lu, Lide Cha, Tzu‐Yu Chen, Philip M. Palacios , et al. · 2023

Mononuclear nonheme iron(II) and 2‐oxoglutarate (Fe/2OG)‐dependent oxygenases and halogenases are known to catalyze a diverse set of oxidative reactions, including hydroxylation, halogenation, epoxidation, and desaturation in primary metab…

Exceptional reactivity of the bridgehead amine on bicyclo[1.1.1]pentane Open

Yong Lu, Chuo Chen · 2023

Bicyclo[1.1.1]pentane (BCP) has received substantial interest in the field of synthetic chemistry recently for its potential use as a benzene isostere in medicinal chemistry. Whereas bicyclo[2.2.2]octane (BCO) has also been used as a biois…

10th anniversary of discovering cGAMP: synthesis and beyond Open

Chuo Chen · 2023

This article describes how the synergy between chemistry and biology facilitated the development of cyclic dinucleotides as a potential new treatment for cancer.

Tumor-targeted delivery of a STING agonist improves cancer immunotherapy Open

Youtong Wu, Yan Fang, Wei Qi, Heping Shi, Huiling Tan , et al. · 2022

The cGAS-STING pathway is essential for immune defense against microbial pathogens and malignant cells; as such, STING is an attractive target for cancer immunotherapy. However, systemic administration of STING agonists poses safety issues…

A phosphine-based redox method for direct conjugation of disulfides Open

Yong Lu, Lin You, Chuo Chen · 2022

Redox-assisted Disulfide Direct Conjugation (RDDC) allows for disulfide functionalization under mild aqueous conditions without prior reduction.

Identification of TRAMs as sphingolipid-binding proteins using a photoactivatable and clickable short-chain ceramide analog Open

Yaqin Deng, Lin You, Yong Lu, Sungwon Han, Jingcheng Wang , et al. · 2021

Ceramide is a lipid molecule that regulates diverse physiological and pathological reactions in part through inverting the topology of certain transmembrane proteins. This topological inversion is achieved through regulated alternative tra…

Avoid the trap: Targeting PARP1 beyond human malignancy Open

Chiho Kim, Chuo Chen, Yonghao Yu · 2021

Necroptosis-blocking compound NBC1 targets heat shock protein 70 to inhibit MLKL polymerization and necroptosis Open

Andrea N. Johnston, Yuyong Ma, Hua Liu, Shuzhen Liu, Sarah Hanna-Addams , et al. · 2020

Significance Necroptosis is a regulated form of necrotic cell death implicated in many human diseases, including infection, inflammation, neurodegeneration, and cancer. TNF-induced necroptosis results in the formation of MLKL tetramers, wh…

Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation Open

Shuai Wang, Lei Han, Jungsoo Han, Peng Li, Qing Ding , et al. · 2019

Response rates and lesion-level progression patterns of solid tumor patients in an academic phase I program: implications for tumour heterogeneity Open

Chuo Chen, Carmine Pinto, Charlotte S. Walmsley, Read Allen, Alona Muzikansky , et al. · 2019

Stereoselective fatty acylation is essential for the release of lipidated WNT proteins from the acyltransferase Porcupine (PORCN) Open

Rubina Tuladhar, Nageswari Yarravarapu, Yuyong Ma, Chengwei Zhang, Jeremiah Herbert , et al. · 2019

Installation of a cancer promoting WNT/SIX1 signaling axis by the oncofusion protein MLL-AF9 Open

Li-Shu Zhang, Xunlei Kang, Jianming Lü, Yuannyu Zhang, Xiaofeng Wu , et al. · 2018

A synthetic combinatorial approach to disabling deviant Hedgehog signaling Open

C-W. Fan, Nageswari Yarravarapu, Heping Shi, Ozlem Kulak, J. Kim , et al. · 2018

Installation of a Cancer Promoting WNT/SIX1 Signaling Axis by the Oncofusion Protein MLL-AF9 Open

Li-Shu Zhang, Xunlei Kang, Jianming Lü, Yuannyu Zhang, Xiaofeng Wu , et al. · 2018

Rapid access to the core skeleton of the [3 + 2]-type dimeric pyrrole–imidazole alkaloids by triplet ketone-mediated C–H functionalization Open

Lin You, Chuo Chen · 2017

Natural Products as Inspiration for the Development of New Synthetic Methods Open

Zhiqiang Ma, Chuo Chen · 2017

Natural products have played an important role in shaping modern synthetic organic chemistry. In particular, their complex molecular skeletons have stimulated the development of many new synthetic methods. We highlight in this article some…

Transcriptional Regulator TetR21 Controls the Expression of the Staphylococcus aureus LmrS Efflux Pump Open

Q. C. Truong-Bolduc, Julia Y. Wang, Chuo Chen, David C. Hooper · 2017

TetR21 controls the expression of Tet38 and LmrS efflux pumps. A tetR21 mutant, QT21, exhibited a 4-fold increase in the transcription level of lmrS . Staphylococcus aureus lmrS overexpressor showed increases of 4-fold and 2-fold, respecti…

Ketone-catalyzed photochemical C(sp3)–H chlorination Open

Lei Han, Ji‐Bao Xia, Lin You, Chuo Chen · 2017

cGAS is essential for the antitumor effect of immune checkpoint blockade Open

Hua Wang, Shuiqing Hu, Xiang Chen, Heping Shi, Chuo Chen , et al. · 2017

Significance The recent success of immune checkpoint blockades, such as the use of antibodies against CTLA4, PD-1, and PD-L1 in cancer therapies has reinvigorated the concept of intrinsic antitumor immunity, but how the immune system detec…

Development of a triazole class of highly potent Porcn inhibitors Open

Lin You, Chengwei Zhang, Nageswari Yarravarapu, Lorraine Morlock, Xiaolei Wang , et al. · 2016

Palladium-Catalyzed C–H Arylation of 1,2,3-Triazoles Open

Chengwei Zhang, Lin You, Chuo Chen · 2016

Palladium(II) acetate, in combination with triphenylphosphine, catalyzes direct arylation of 1,4-disubstituted 1,2,3-triazoles effectively. This C–H arylation reaction provides facile access to fully substituted triazoles with well-defined…

Asymmetric Synthesis of Axinellamines A and B Open

Zhiqiang Ma, Xiao Wang, Yuyong Ma, Chuo Chen · 2016

Axinellamines A and B are broad‐spectrum antibacterial pyrrole–imidazole alkaloids that have a complex polycyclic skeleton. A new asymmetric synthesis of these marine sponge metabolites is described herein, featuring an oxidative rearrange…

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