Evidence map›Paper›PMID 39735913›Full record

ArticleJACS Au2024

Structure-Based Design of "Head-to-Tail" Macrocyclic PROTACs.

Chungen Li, Yihan Chen, Weixue Huang, Yudi Qiu, Shengjie Huang, Yang Zhou, Fengtao Zhou, Jian Xu, Xiaomei Ren, Jinwei Zhang and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in JACS Au, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors.

Chungen LiState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.
Yihan ChenState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.
Weixue HuangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.
Yudi QiuKey Laboratory of Structure-Based Drugs Design and Discovery of Ministry of Education, Shengyang Pharmaceutical University, Shenyang 110016, China.
Shengjie HuangInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, No. 855 Xingye Avenue East, Guangzhou 511400, China.
Yang ZhouInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, No. 855 Xingye Avenue East, Guangzhou 511400, China.ORCID https://orcid.org/0000-0003-4167-6413
Fengtao ZhouInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, No. 855 Xingye Avenue East, Guangzhou 511400, China.ORCID https://orcid.org/0000-0003-2518-7855
Jian XuLivzon Research Institute, Livzon Pharmaceutical Group Inc., No. 38, Chuangye North Road, Jinwan District, Zhuhai 519000, China.
Xiaomei RenState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.
Jinwei ZhangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.
Zhen WangState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.ORCID https://orcid.org/0000-0001-8762-6089
Ming DingSchool of Life Science and Technology, China Pharmaceutical University, No. 639 Longmian Avenue, Nanjing 211198, China.
Ke DingState Key Laboratory of Chemical Biology, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, No. 345 Lingling Road, Shanghai 200032, China.ORCID https://orcid.org/0000-0001-9016-812X

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Macrocyclization is a compelling strategy for conventional drug design for improving biological activity, target specificity, and metabolic stability, but it was rarely applied to the design of PROTACs possibly due to the mechanism and structural complexity. Herein, we report the rational design of the first series of "Head-to-Tail" macrocyclic PROTACs. The resulting molecule

Identifiers

PMID39735913
PMCPMC11672125

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.