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Last update 08 May 2025

OSC

Last update 08 May 2025

Basic Info

Synonyms

2,3-epoxysqualene--lanosterol cyclase, hOSC, Lanosterol synthase

+ [5]

Introduction

Key enzyme in the cholesterol biosynthesis pathway. Catalyzes the cyclization of (S)-2,3 oxidosqualene to lanosterol, a reaction that forms the sterol nucleus (PubMed:14766201, PubMed:26200341, PubMed:7639730). Through the production of lanosterol may regulate lens protein aggregation and increase transparency (PubMed:26200341).

Drugs associated with OSC

ZD-9720

Target

OSC

Mechanism

OSC inhibitors

Active Org.

AstraZeneca PLC

Originator Org.

AstraZeneca PLC

Active Indication

Hypercholesterolemia

Inactive Indication-

Drug Highest PhaseClinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

RO-488071

Target

OSC

Mechanism

OSC inhibitors

Active Org.

F. Hoffmann-La Roche Ltd. [+1]

Originator Org.

Roche Holding AG

Active Indication

Castration-Resistant Prostatic Cancer [+1]

Inactive Indication

Hyperlipidemias

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

MM-0299

Target

OSC

Mechanism

OSC inhibitors

Active Org.

The University of Texas Southwestern Medical Center

Originator Org.

The University of Texas Southwestern Medical Center

Active Indication

Glioma

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with OSC

NCT02229773

/ CompletedPhase 1

Pharmacodynamics, Preliminary Pharmacokinetics and Tolerability After Multiple Oral Doses of 0.25 mg, 0.5 mg and 1 mg o.d. BIBB 1464 (Tablet) or Pravastatin 20 mg Over 2 Weeks in Hyperlipemic Healthy Male Subjects (Parallel Group Comparison, Randomized, Placebo Controlled, Partly Double Blind [Pravastatin Open])

Lipid lowering effect, investigation of pharmacodynamics (inhibition of oxidosqualene cyclase, monoepoxysqualene (MES) as marker), safety / tolerability and preliminary pharmacokinetics

Start Date01 Jan 2000

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02229838

/ CompletedPhase 1

Safety/Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of 0.25 mg, 0.75 mg, 2 mg, 6 mg, and 10 mg BIBB 1464 MS (Tablet) in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food of the Dose of 0.75 mg or 2 mg or 6 mg (Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase)

Safety, pharmacodynamics and pharmacokinetics of 0.25, 0.75, 2.0, 6.0, and 10 mg BIBB 1464 p.o once daily in a rising dose group-comparison (placebo controlled, double blind, randomized per dose level).
Relative Bioavailability of 0.75 mg or 2 mg or 6 mg ( tablet vs. solution, intraindividual comparison), preliminary assessment of food effects (interindividual comparison)
Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).
MS (Tablet) in Healthy Male Subjects, Combined With Preliminary Evaluation of Relative Bioavailability and Effect of Food of the Dose of 0.75 mg or 2 mg or 6 mg (Two-stage Trial Design With Randomised Double Blind Placebo Controlled Rising Dose Phase and Subsequent Randomised, Open Parallel Group Phase).

Start Date01 Jul 1999

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02266485

/ CompletedPhase 1

Pharmacodynamics, Preliminary Pharmacokinetics and Tolerability After Multiple Oral Doses of 2.5 mg o.d. BIBB 515 BS (Capsule) or Pravastatin 20 mg Over 2 Weeks in Hyperlipemic Healthy Male Subjects (Parallel Group Comparison, Randomized, Placebo Controlled, Partly Double Blind [Pravastatin Open])

Investigation of pharmacodynamics (inhibition of oxidosqualene cyclase, MES as marker), effect on routine lipid profile parameters, safety and preliminary pharmacokinetics

Start Date01 Jul 1998

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with OSC

100 Translational Medicine associated with OSC

0 Patents (Medical) associated with OSC

702

Literatures (Medical) associated with OSC

31 Dec 2025·Science and Technology of Advanced Materials

Scalable fabrication of precise flexible strain sensors using organic semiconductor single crystals

Article

Author: Watanabe, Shun ; Murata, Tomohiro ; Takeya, Jun ; Yamashita, Yu ; Matsumoto, Takafumi ; Usami, Yoshihisa ; Ito, Masataka

Organic semiconductor (OSC) single crystals feature flexibility, solution processability, and high-mobility coherent carrier transport, which are advantageous for printed flexible electronic applications. A mechanical strain sensor is a target device whose high sensitivity and wide measurement range have been demonstrated when OSC single crystals were employed as the active channel. However, there have been limited reports on scalable fabrication of devices and reliable measurements, which limits the use of strain sensors in a wide range of applications. In this study, we present a comprehensive approach to address these issues through advanced device processing, design, and measurements. Our resistive strain sensors showed a small drift owing to the stable and effective p-type chemical doping of the OSC single crystals. A Wheatstone bridge circuit and compact lock-in amplifier were designed to accurately measure resistance changes at low noise levels. The experimental results demonstrated a substantial reduction in noise and achieved high-precision measurements with precision of ± 1.8 ppm. These results demonstrate the scalable fabrication of organic semiconductor strain sensors with high precision and reliability, which opens up the possibility of employing them in various industrial sectors.

01 Jul 2025·Cancer Letters

SQLE amplification accelerates esophageal squamous cell carcinoma tumorigenesis and metastasis through oncometabolite 2,3-oxidosqualene repressing Hippo pathway

Article

Author: Zhan, Qimin ; Wu, Qingnan ; Zhao, Dongyu ; Min, Qingjie ; Liu, Xuesong ; Gong, Ying ; Chen, Jie ; Lv, Mengzhu ; Feng, Bicong ; Zhang, Weimin ; Li, Jinting ; Wang, Yan

Esophageal squamous cell carcinoma (ESCC) is one of the most prevalent cancers worldwide, characterized by a dismal prognosis and elusive therapeutic targets. Dysregulated cholesterol metabolism is a critical hallmark of cancer cells, facilitating tumor progression. Here, we used whole genome sequencing data from several ESCC cohorts to identify the important role of squalene epoxidase (SQLE) in promoting ESCC tumorigenesis and metastasis. Specifically, our findings highlight the significance of 2,3-oxidosqualene, an intermediate metabolite of cholesterol biosynthesis, synthesized by SQLE and metabolized by lanosterol synthase (LSS), as a key regulator of ESCC progression. Mechanistically, the interaction between 2,3-oxidosqualene and vinculin enhances the nuclear accumulation of Yes-associated protein 1 (YAP), thereby increasing YAP/TEAD-dependent gene expression and accelerating both tumor growth and metastasis. In a 4-nitroquinoline 1-oxide (4-NQO)-induced ESCC mouse model, overexpression of Sqle resulted in accelerated tumorigenesis compared to wild-type controls, highlighting the pivotal role of SQLE in vivo. Furthermore, elevated SQLE expression in ESCC patients correlates with a poorer prognoses, suggesting potential therapeutic avenues for treatment. In conclusion, our study elucidates the oncogenic function of 2,3-oxidosqualene as a naturally occurring metabolite and proposes modulation of its levels as a promising therapeutic strategy for ESCC.

01 Jun 2025·Toxicon

The DHCR7 is the key target of lipotoxic liver injury caused by matrine through abnormal activation of the cholesterol synthesis pathway

Article

Author: Li, Jiaqi ; Zhang, Wenting ; Tao, Xiaoyu ; Li, Zhiqi ; Zhao, Chongjun ; Fan, Qiqi ; Gao, Yifei ; Chen, Linzhen ; Wu, Jiarui ; Lu, Shan

BACKGROUNDMatrine, the main active ingredient in Sophora flavescens and Sophorae tonkinensis radix et rhizome, is a highly effective insecticide. However, its hepatotoxicity to some extent affects its application value. This study aimed to explore the mechanism underlying matrine-induced liver injury.METHODSThe zebrafish (Danio rerio) and L02 cell model were utilized to investigate the toxic dose of matrine and its effects on liver tissue damage, liver cell morphology and activity, and expression levels of ALT and AST. Zebrafish and L02 cell samples were then collected for transcriptomic testing to further explore the possible mechanism by which matrine induced liver injury. Finally, integrated bioinformatics methods and experiments were used to elucidate the possible mechanisms behind matrine-induced liver injury.RESULTSThe result presented solid in vivo evidence of matrine-induced hepatotoxicity, supported by abnormal changes of liver morphological, disturbed liver cell structure, obvious apoptosis, as well as elevated levels of ALT and AST in zebrafish. In addition, in vitro L02 cell experiments also showed that matrine can produce significant liver cell damage effects. The integrated bioinformatics analysis results revealed that differentially expressed genes (DEGs) were substantially enriched in multiple pathways related to lipid regulation. Among which, the steroid biosynthesis was the most key signaling pathway, evidenced by the enhanced expression of eight genes, including DHCR7, SQLE, CYP51, CYP24A1, SC5D, LSS, MSMO1 and SOAT1. Furthermore, AY9944, the targeted inhibitor of DHCR7, could offset the toxic effect, as reflected by diminished liver phenotype damage, steatosis, and cholesterol accumulation caused by matrine.CONCLUSIONSMatrine can upregulate the expression of key genes in steroid biosynthesis pathway, resulting in cholesterol accumulation and then inducing hepatotoxicity. Among them, targeted inhibition of DHCR7 gene expression can alleviate matrine-induced liver injury.

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