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Last update 01 Nov 2024

OSC

Last update 01 Nov 2024

Basic Info

Synonyms

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

+ [6]

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:7639730, PubMed:26200341). 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

RO0717625

Target

OSC

Mechanism

OSC inhibitors

Active Org.

Roche Holding AG

Originator Org.

Roche Holding AG

Active Indication

Hypercholesterolemia

Inactive Indication-

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

891

Literatures (Medical) associated with OSC

01 Dec 2024·Data in Brief

Data of crystal structure of the large Stokes shift fluorescent protein tKeima

Article

Author: Xu, Yongbin ; Nam, Ki Hyun

Large Stokes shift (LSS) fluorescent proteins (FPs) are important for dual-color fluorescence cross-correlation spectroscopy and multicolor imaging. tKeima is a tetrameric LSS FP from the stony coral Montipora sp. Analyzing the tetrameric interface of tKeima is necessary to understand the oligomeric state of the Keima family and to provide insights into engineering oligomeric FPs to generate monomeric FPs, which are useful for FP-based molecular and cell biology studies. Here, detailed experimental procedures for tKeima were reported, including spontaneous crystal growth, data collection for X-ray diffraction, and structure determination. This information can be used for future experiments to obtain the high-resolution structure of tKeima, providing accurate structural information to comprehensively understand the molecular function of tKeima and the protein engineering of tetrameric FPs.

01 Dec 2024·Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology

Cloning of down-regulated genes under cold stress and identification of important genes related to cold tolerance in zebrafish (Danio rerio)

Article

Author: Zhong, Shan ; Song, Ziwei ; Cui, Zongbin ; Zhang, Lang

Low-temperature stress poses a significant risk to the survival of both cultivated and wild fish populations. Existing studies have found that the pre-acclimation of fishes to moderate cold stress can stimulate the activation of acclimation pathways, thereby enhancing their tolerance to cold stress. The fitness of fish relies heavily on appropriately controlled transcriptional reactions to environmental changes. Despite previous characterization of gene expression profiles in various fish species during cold acclimation, the specific genes responsible for essential functions in this process remain largely unknown, particularly the down-regulated genes induced by cold acclimation. To investigate the genes involved in cold acclimation, this study employed real-time quantitative PCR (RT-qPCR), molecular cloning, microinjection techniques, and cold stress experiments to determine the genes that play an essential part in cold acclimation. Consequently, 18 genes were discovered to be down-regulated in larval zebrafish experiencing cold stress. All 18 genes successfully detected overexpression in zebrafish at 96 and 126 hpf (fold change ≥3), which declined with the growth of zebrafish. Following microinjection, it was observed that her8a, cyp51, lss, txnipb, and bhlha9 had an adverse impact on the survival rate of zebrafish larvae under cold stress. These genes have been identified to play significant roles in various biological processes. For instance, bhlha9 has been found to be involved in both limb development and temperature sensing and her8a has been implicated in neural development. Additionally, cyp51 and lss have been identified as participants in the cholesterol synthesis pathway. Txnipb has been reported to induce cell apoptosis, thereby potentially influencing the survival rate of zebrafish larvae under cold stress. These findings offered crucial data for the analysis of molecular processes related to cold tolerance and the development of cold-resistant fish breeding.

01 Nov 2024·Digestive and Liver Disease

Identification of key markers for the stages of nonalcoholic fatty liver disease: An integrated bioinformatics analysis and experimental validation

Article

Author: Reyes-Jimenez, Edilburga ; Velazquez-Enriquez, Juan Manuel ; Villa-Treviño, Saul ; Vásquez-Garzón, Verónica Rocío ; Muriel, Pablo ; Arellanes-Robledo, Jaime ; Villaseñor-Altamirano, Ana Beatriz ; Baltiérrez-Hoyos, Rafael ; Reyes-Avendaño, Itayetzi ; Piña-Vázquez, Carolina

BACKGROUNDThe identification of biomarkers for the early diagnosis of nonalcoholic fatty liver disease (NAFLD) is urgently needed. Here, we aimed to identify NAFLD biomarkers in the early stages of steatosis (SS) and nonalcoholic steatohepatitis (NASH) based on differential gene expression from bioinformatics data.METHODSA meta-analysis was performed from transcriptomic databases retrieved from public repositories containing data from biopsies of patients at various stages of NAFLD development. The status of the selected molecules was validated in the serum of patients with NAFLD by ELISA.RESULTSWe identified 121 differentially expressed genes (DEGs) associated with SS and 402 associated with NASH. Gene Ontology (GO) enrichment revealed that the altered genes were primarily associated with dysfunction of primary cellular processes, and pathway analyses were mainly related to cholesterol metabolism. We identified ACSS2, PCSK9, and CYP7A1 as candidate biomarkers for SS and ANGPTL3, CD36, CYP51A1, FASN, FAS, FDFT1, and LSS as candidate biomarkers for NASH.CONCLUSIONSBy experimental validation of bioinformatics data from patients with NAFLD, we identified promising biomarkers for detecting SS and NASH that might be useful for screening and diagnosing early NAFLD stages in humans.

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