Macrophage P2Y6R activation aggravates psoriatic inflammation through IL-27-mediated Th1 responses

Yin, Li; Zhang, Enming; Mao, Tianqi; Zhu, Yifan; Ni, Shurui; Li, Yehong; Liu, Chunxiao; Fang, Yafei; Ni, Kexin; Lu, Yuhe; Li, Huanqiu; Zhou, Mengze; Hu, Qinghua

doi:10.1016/j.apsb.2024.06.008

Acta Pharmaceutica Sinica B

2024

DOI: 10.1016/j.apsb.2024.06.008

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Macrophage P2Y6R activation aggravates psoriatic inflammation through IL-27-mediated Th1 responses

Li Yin,

Enming Zhang,

Tianqi Mao

et al.

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Cited by 2 publications

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Functionalized Congeners of 2H-Chromene P2Y6 Receptor Antagonists

Oliva,

Pramanik,

Jung

et al. 2024

Cells

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The P2Y6 receptor (P2Y6R), a Gq-coupled receptor, is a potential drug discovery target for various inflammatory and degenerative conditions. Antagonists have been shown to attenuate colitis, acute lung injury, etc. In the search for competitive antagonists, we have investigated the SAR of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives, although high affinity is lacking. We now reveal that long-chain amino-functionalized congeners display greatly enhanced affinity in the antagonism of UDP-induced Ca2+ mobilization in human (h) P2Y6R-transfected 1321N1 astrocytoma cells. A 6-(Boc-amino-n-heptylethynyl) analogue 30 (MRS4940) had an IC50 of 162 nM, which was a 123-fold greater affinity than the corresponding unprotected primary alkylamine, 107-fold greater than the corresponding pivaloyl derivative 30, and 132-fold selective compared to the P2Y14R. However, similar Boc-amino chains attached at the 8-position produced weak µM affinity. Thus, the P2Y6R affinity depended on the chain length, attachment point, and terminal functionality. Off-target activities, at 45 sites, were tested for acylamino derivatives 20, 24, 26, 30, 31, and 37, which showed multiple interactions, particularly at the biogenic amine receptors. The more potent analogues may be suitable for evaluation in inflammation and cancer models, which will be performed in future studies.

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Functionalized Congeners of 2H-Chromene P2Y6 Receptor Antagonists

Oliva,

Pramanik,

Jung

et al. 2024

Cells

View full text Add to dashboard Cite

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Nanocarrier-Based Transdermal Drug Delivery Systems for Dermatological Therapy

Kang,

Zhang,

Wang

et al. 2024

Pharmaceutics

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Dermatoses are among the most prevalent non-fatal conditions worldwide. Given this context, it is imperative to introduce safe and effective dermatological treatments to address the diverse needs and concerns of individuals. Transdermal delivery technology offers a promising alternative compared to traditional administration methods such as oral or injection routes. Therefore, this review focuses on the recent achievements of nanocarrier-based transdermal delivery technology for dermatological therapy, which summarizes diverse delivery strategies to enhance skin penetration using various nanocarriers including vesicular nanocarriers, lipid-based nanocarriers, emulsion-based nanocarriers, and polymeric nanocarrier according to the pathogenesis of common dermatoses. The fundamentals of transdermal delivery including skin physiology structure and routes of penetration are introduced. Moreover, mechanisms to enhance skin penetration due to the utilization of nanocarriers such as skin hydration, system deformability, disruption of the stratum corneum, surface charge, and tunable particle size are outlined as well.

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Macrophage P2Y6R activation aggravates psoriatic inflammation through IL-27-mediated Th1 responses

Cited by 2 publications

References 58 publications

Functionalized Congeners of 2H-Chromene P2Y6 Receptor Antagonists

Functionalized Congeners of 2H-Chromene P2Y6 Receptor Antagonists

Nanocarrier-Based Transdermal Drug Delivery Systems for Dermatological Therapy

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