Bioconjugate Chemistry最新文献_第9页

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

Rozan Tannous, Chi Zhang and Doron Shabat*,

引用次数: 0

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

Ying Chen, Yao Chen, Hong Xu, Jianan Liu, Yan Wang, Yingjie Zeng, Hongyu Chen, Yuening Cao, Chen Sun, Xian Ge, Tingting Zhang, Xiaoke Shi, Xiujun Cao, Yilan Liu*, Bo Ren*, Tianbao Wang* and Jun Lu*,

引用次数: 0

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

Linhui Lv, and , Ke Qu*,

引用次数: 0

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

Guozhen Dong, Liyan Gong, Qianqian Zhang, Wenqing Yao, Yiying Shi, Zongwen Gu, Xianmin Yang, Xiang Gao, Yaning Zheng and Chuanliang Zhang*,

引用次数: 0

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

Genglian Liu, Ru Li, Jingwei Gao, Cong Lin, Hongyuan Li, Yinghua Peng*, Hongshuang Wang* and Xiaohui Wang*,

引用次数: 0

Carrier Free 1,2,3,4,6-O-Pentagalloylglucose Nanoparticles for Treatment of Acute Lung Injury. 无载体1,2,3,4,6- o -五五烯基葡萄糖纳米颗粒治疗急性肺损伤

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21 Epub Date: 2025-05-08 DOI: 10.1021/acs.bioconjchem.5c00197

Qi Zhang, Ying Wang, Zixuan Yang, Zhiming Xin, Haohua Deng, Wei Chen

引用次数: 0

Glycosylation Modification Balances the Aqueous Solubility of Lipidated Peptides and Facilitates Their Biostability. 糖基化修饰平衡脂化肽的水溶性并促进其生物稳定性。

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21 Epub Date: 2025-04-09 DOI: 10.1021/acs.bioconjchem.5c00057

Guozhen Dong, Liyan Gong, Qianqian Zhang, Wenqing Yao, Yiying Shi, Zongwen Gu, Xianmin Yang, Xiang Gao, Yaning Zheng, Chuanliang Zhang

{"title":"Glycosylation Modification Balances the Aqueous Solubility of Lipidated Peptides and Facilitates Their Biostability.","authors":"Guozhen Dong, Liyan Gong, Qianqian Zhang, Wenqing Yao, Yiying Shi, Zongwen Gu, Xianmin Yang, Xiang Gao, Yaning Zheng, Chuanliang Zhang","doi":"10.1021/acs.bioconjchem.5c00057","DOIUrl":"10.1021/acs.bioconjchem.5c00057","url":null,"abstract":"Protein tyrosine phosphatase N1 (PTPN1) is a key regulator of insulin and leptin signaling pathways, making it an attractive therapeutic target for type 2 diabetes. Recent studies have identified fatty acid conjugated BimBH3 analogues as promising PTPN1 inhibitors with antidiabetic potential. Peptide therapeutics have proven successful in the treatment of a wide range of medical conditions, yet challenges such as poor aqueous solubility, proteolytic degradation, and limited bioavailability still hinder their clinical application. In this study, we developed a series of novel BimBH3 peptide analogues through dual modifications involving fatty acid lipidation and glycosylation to address these limitations. These modifications significantly improved the peptides' solubility, proteolytic stability, and plasma half-life while preserving potent PTPN1 inhibitory activity, which is essential for enhancing insulin signaling in type 2 diabetes treatment. Among the analogues, compound L3 exhibited the most balanced profile, with an aqueous solubility increase over 10-fold, a half-life extension in rat plasma of 9.92-fold compared to the lead compound, and an IC50 of 0.78 μM against PTPN1. In vivo studies further demonstrated L3's efficacy in lowering blood glucose levels in mice. This study demonstrates the utility of glycosylation in overcoming the solubility and stability challenges associated with lipidated peptides. The optimized analogue L3 could serve as a proof of concept for developing novel long-acting PTPN1 inhibitors.","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"1004-1012"},"PeriodicalIF":4.0,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143952148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

V. Arun, Minju Lee, Hongseo Choi, Sangwoo Lee, Junwon Choi, Tae Hyeon Yoo, Wook Kim* and Eunha Kim*,

引用次数: 0

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21

Szilvia H. Toth, Anca D. Stoica* and Cristian Sevcencu,

引用次数: 0

In Vivo Interrogation of Cell-Penetrating Peptide Function: Accumulation in Tumors and the Potential as a Specific PET Probe. 细胞穿透肽功能的体内研究：肿瘤中的积累和作为特异PET探针的潜力。

IF 4 2区化学

Bioconjugate Chemistry Pub Date : 2025-05-21 Epub Date: 2025-04-09 DOI: 10.1021/acs.bioconjchem.5c00128

Zhan Si, Lulu Tian, Hongxin Zhou, Jiasheng Lin, Jun Zhou

{"title":"In Vivo Interrogation of Cell-Penetrating Peptide Function: Accumulation in Tumors and the Potential as a Specific PET Probe.","authors":"Zhan Si, Lulu Tian, Hongxin Zhou, Jiasheng Lin, Jun Zhou","doi":"10.1021/acs.bioconjchem.5c00128","DOIUrl":"10.1021/acs.bioconjchem.5c00128","url":null,"abstract":"We aimed to evaluate the biodistribution and specificity of 68Ga-DOTA-TAT and RHO-TAT using MGC-803 and HT-29 tumor cells as well as tumor-xenografted nude mice and to demonstrate its application in positron emission tomography (PET) imaging. The in vitro evaluation of 68Ga-DOTA-TAT was assessed in MGC-803 and HT-29 cell lines, and the in vivo evaluation of 68Ga-DOTA-TAT was also performed in mice bearing MGC-803 or HT-29 tumors, respectively. Fluorescence microscopy was also employed to evaluate the specificity of RHO-TAT in vitro in MGC-803 and HT-29 cells as well as ex vivo in tumor slices of the corresponding tumor models. The in vivo imaging differences between 68Ga-DOTA-TAT and 18F-FDG in MGC-803 and HT-29 tumors were also studied. The biodistribution and micro-PET results demonstrated significant uptake of 68Ga-DOTA-TAT in non-FDG-avid MGC-803 tumors, whereas there was negligible uptake in FDG-avid HT-29 tumors. RHO-TAT showed superior fluorescence microscopy imaging effects in MGC-803 cells and tumor slices but not in HT-29 cells and tumor slices, which were consistent with the in vivo results. 68Ga-DOTA-TAT combined with 18F-FDG can be applied noninvasively in cancers with PET imaging for potential patient selection and stratification. We demonstrated a higher binding of 68Ga-DOTA-TAT and RHO-TAT to MGC-803 cells as well as to non-FDG-avid MGC-803 xenografted tumors and a lower binding to HT-29 cells and FDG-avid xenografted tumors. These results suggest that TAT has the potential to be a ligand for targeting certain tumors.","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"1088-1097"},"PeriodicalIF":4.0,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12101444/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810197","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0