Delving into the Latest Updates on Zhongshan Institute for Drug Discovery with Synapse

Overview

Tags

Neoplasms

Endocrinology and Metabolic Disease

Urogenital Diseases

Small molecule drug

Proteolysis-targeting chimeras (PROTAC)

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	6
Endocrinology and Metabolic Disease	3
Infectious Diseases	2
Nervous System Diseases	2
Immune System Diseases	2
Hemic and Lymphatic Diseases	1

Top 5 Drug Type	Count

Small molecule drug	5
Proteolysis-targeting chimeras (PROTAC)	1

Top 5 Target	Count

PTPN2(Tyrosine-protein phosphatase non-receptor type 2)	1
FBXO22 x NSD2 x VHL	1
CSK x SRC	1
IRAK4(Interleukin-1 receptor-associated kinase 4)	1
PTP1B x PTPN2 x PTPs	1

AbstractPhytochemical study of the n-BuOH extract of Ilex asprella resulted in the discovery of ten new pentacyclic triterpenoid glycosides, comprising nine ursane-type glycosides (1−9) and one oleanane-type glycoside (10), along with seven known compounds (11−17). Compound 1 is the first reported 19,22-epoxy ursane triterpenoid glycoside, whereas 4 and 5 are rare examples of ursane triterpenoid glycosides containing a 28,19-lactone group. The structural characterization of these compounds was achieved using spectroscopic and chemical techniques, as well as single-crystal X-ray analysis. Compounds 7, 12, 15, and 17 exhibited moderate cytotoxic activities against H1975 and HCC827 cancer cells.Graphical abstract

01 Aug 2025·Bioorganic & Medicinal Chemistry

Recent advances in the synthesis of poly (ADP-ribose)

Review

Author: Tang, Li ; Wu, Yidan ; Liu, Qiang

Poly (ADP-ribose) (PAR), a dynamic and reversible post-translational modification, is a structurally complex biopolymer synthesized via ADP-ribosylation, utilizing NAD⁺ as a substrate and catalyzed by ADP-ribosyltransferases (ARTs). PAR exists as linear or branched chains of up to 200 ADP-ribose units, playing pivotal roles in DNA repair, chromatin remodeling, transcriptional regulation, and cell death. The structural intricacy of PAR-marked by labile pyrophosphate linkages, stereochemical diversity, and branching architectures-poses significant synthetic challenges, necessitating innovative strategies integrating carbohydrate chemistry, enzymatic engineering, and phosphate coupling. Recent advances over the past decade have enabled the chemical and chemoenzymatic synthesis of well-defined PAR fragments, oligomers, and probes, facilitating breakthroughs in structural biology, interactome mapping, and therapeutic discovery. This review highlights key methodologies, including phosphoramidite-based assembly, development of photoaffinity probes and chemoenzymatic elongation with engineered ARTs, which collectively advance our understanding of PAR's biological functions and therapeutic potential.

01 Aug 2025·Food Chemistry

Targeted characterisation of bioactive prenylated flavonoids from Ficus carica L. fruits

Article

Author: Aisa, Haji Akber ; Yuan, Yue ; Li, Zuopeng

Figs (Ficus carica L.) are rich in bioactive prenylated flavonoids (PFs), which have garnered considerable attention owing to their potential health benefits. In this study, feature-based molecular networking was used to facilitate the targeted isolation of PFs components. Fifty flavonoids, including eight pairs of enantiomers, were isolated, and thirty-eight were identified as PFs. Structural characterisation of the ten novel flavonoids was achieved through comprehensive spectroscopic analysis and quantum chemical calculations. Fig extracts exhibited potent free radical scavenging capacities against DPPH and ABTS radicals. The identification of forty-two polyphenolics using UHPLC-Q-Exactive Orbitrap MS analysis further supported these results. Several compounds showed moderate inhibitory effects against the NF-κB and STAT3 pathways. Structure-activity relationship analysis revealed that the prenyl type and substitution position played a pivotal role in influencing anti-mycobacterial activity. These findings provide novel insights into the targeted isolation, structural features, and activity profiles of PFs in figs.

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 10 May 2025

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

Discovery

4

1

Preclinical

IND Approval

3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

TT-9701 ( Chk1 )	Refractory acute myeloid leukemia More	IND Approval
TLX83 ( Chk1 x FLT3 )	Relapsing acute myeloid leukemia More	IND Approval
KYHY2303	Hematologic Neoplasms More	IND Approval
PVD-06 ( PTPN2 )	Neoplasms More	Preclinical
CN118851935 ( CSK x SRC )	Gout More	Discovery