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Overview

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Neoplasms

Proteolysis-targeting chimeras (PROTAC)

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	1

Top 5 Drug Type	Count

Proteolysis-targeting chimeras (PROTAC)	1
Small molecule drug	1

Top 5 Target	Count

PTPN2(Tyrosine-protein phosphatase non-receptor type 2)	1

Author: Huang, Jian-yuan ; Chanda, Francis ; Shu, Chi ; Zhang, Hui-Juan ; Lin, Kai-Xuan ; Chaurembo, Abdallah Iddy ; Huang, Jian-Yuan ; Xu, Yun-jing ; Cui, Hao-dong ; Zhang, Hui-juan ; Lin, Han-Bin ; Deng, Wen-hui ; Fu, Li-Dan ; Xing, Na ; Deng, Wen-Hui ; Lin, Kai-xuan ; Xu, Yun-Jing ; Cui, Hao-Dong ; Li, Yuan ; Fu, Li-dan ; Lin, Han-bin ; Chen, Yang

Air pollution, particularly fine particulate matter (PM_2.5) with <2.5 μm in diameter, is a major public health concern. Studies have consistently linked PM_2.5 exposure to a heightened risk of cardiovascular diseases (CVDs) such as ischemic heart disease (IHD), heart failure (HF), and cardiac arrhythmias. Notably, individuals with pre-existing age-related cardiometabolic conditions appear more susceptible. However, the specific impact of PM_2.5 on CVDs susceptibility in older adults remains unclear. Therefore, this review addresses this gap by discussing the factors that make the elderly more vulnerable to PM_2.5-induced CVDs. Accordingly, we focused on physiological aging, increased susceptibility, cardiometabolic risk factors, CVDs, and biological mechanisms. This review concludes by examining potential interventions to reduce exposure and the adverse health effects of PM_2.5 in the elderly population. The latter includes dietary modifications, medications, and exploration of the potential benefits of supplements. By comprehensively analyzing these factors, this review aims to provide a deeper understanding of the detrimental effects of PM_2.5 on cardiovascular health in older adults. This knowledge can inform future research and guide strategies to protect vulnerable populations from the adverse effects of air pollution.

01 Dec 2024·Bioorganic Chemistry

Discovery of N-Benzylpiperidinol derivatives as USP7 inhibitors against Hematology

Article

Author: Zhang, Jingyu ; Zhou, Yubo ; Pan, Youlu ; Fu, Jingfeng ; Chen, Runmei ; Che, Jinxin ; Chen, Haifeng ; Huang, Wenhai ; Dong, Xiaowu ; Wang, Peipei ; Geng, Shuangshuang

USP7 has been recognized as a potential target for the treatment of hematologic malignancies by stabilizing multiple cancer-relevant proteins. Nevertheless, drug-like USP7 inhibitors are still lacking. Herein, compound J21 (USP7 IC₅₀: 41.35 ± 2.16 nM) was discovered based on the structure of L55 and its co-crystal complex with USP7. Additionally, J21 exhibited greater metabolic stability (T_1/2: 1.25 h, C_max: 394.1 ± 48.3 ng/mL, and AUC_0-t: 597.8 ± 44.8 ng/mL∙h) compared to L55. These findings may further pave the way for the development of USP7 inhibitors for the treatment of hematologic malignancies.

01 Nov 2024·Journal of Chromatography A

Multi-step HPLC fractionation enabled in-depth and unbiased characterization of histone PTMs

Article

Author: Zhang, Mingya ; Zhao, Wensi ; Chen, Kaifeng ; Guo, Jingli ; Xie, Dong ; Tan, Minjia ; Xu, Junyu ; Zhang, Jun

Histone post-translational modifications (PTMs) are critical epigenetic regulatory factors. Histone PTMs are highly dynamic and complicated, encompassing over 30 structurally diverse modifications across nearly 180 amino acid residues, which generated extensive information regarding histone marks. In proteomics-based characterization of histone PTMs, chemical derivatization and antibody-based affinity enrichment were frequently utilized to improve the identification depth. However, chemical derivatization suffered from the occurrence of side reactions, and antibody-based affinity enrichment focused on specific PTM types of interest. In this research, we developed a multi-step fractionation strategy for comprehensively unbiased detection of histone PTM sites. By combining protein-level fractionation with peptide-level alkaline and acid phase fractionation, we developed the Multidimensional Fractionation based Histone Mark Identification Technology (MudFIT) and increased PTM identification to a total of 264 histone PTM sites. To the best of our knowledge, this strategy achieved the most comprehensive characterization of histone PTM sites in a single proteomics study. Using the same starting amount of sample, MudFIT identified more Kac sites and Kac peptides than those in antibody-based acetylated peptide enrichment. Moreover, in addition to well-studied histone marks, we discovered 36 potential new histone PTM sites including H2BK116bu, H4R45me2, H1K63pr, and uncovered unknown histone PTM types like aminoadipic on lysine and nitrosylation on tyrosine. Our data provided a method and resource for in-depth characterization of histone PTM sites, facilitating further biological understanding of histone marks.

100 Deals associated with Zhongshan Institute for Drug Discovery

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100 Translational Medicine associated with Zhongshan Institute for Drug Discovery

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Pipeline

Pipeline Snapshot as of 24 Dec 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

1

IND Application

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