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Last update 23 Jan 2025

Chitin synthase

Last update 23 Jan 2025

Basic Info

Synonyms

chitin-UDP acetyl-glucosaminyl transferase, 壳多糖合酶

Introduction-

Drugs associated with Chitin synthase

Myc-102

Target

Chitin synthase

Mechanism

Chitin synthase inhibitors

Active Org.-

Originator Org.

TGV-Laboratories Group of Cos.

Active Indication

Gingivitis [+1]

Inactive Indication

Aspergillosis [+7]

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

MYC-053

Target

Chitin synthase

Mechanism

Chitin synthase inhibitors

Active Org.

National Institutes of Health [+1]

Originator Org.

TGV-Health, Inc.

Active Indication

Candidiasis [+1]

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Nikkomycin Z

Target

Chitin synthase

Mechanism

Chitin synthase inhibitors

Active Org.-

Originator Org.

Valley Fever Solutions, Inc.

Active Indication-

Inactive Indication

Coccidioidomycosis

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with Chitin synthase

NCT01647256

/ TerminatedPhase 1IIT

Comparison of Nikkomycin Z Bioavailability After Single Dose Administration Under Fed (High Fat Meal) Compared to Fasting Conditions

The primary purpose of this study is to evaluate if eating a high fat meal versus not eating any food affects how the study drug (Nikkomycin Z) is absorbed into the body. The second purpose is to gain further information about the safety of Nikkomycin Z in healthy adults.

Start Date01 Jul 2012

Sponsor / Collaborator

University of Arizona

NCT00834184

/ CompletedPhase 1IIT

Phase I, Randomized, Double-blind, Placebo Controlled, Multiple-dose Evaluation of the Safety Tolerance and Pharmacokinetics of Nikkomycin Z in Healthy Subjects

Start Date01 Oct 2008

Sponsor / Collaborator

University of Arizona

NCT00614666

/ TerminatedPhase 1/2IIT

Phase I/II Evaluation of the Safety, Pharmacokinetics, and Preliminary Effectiveness of Nikkomycin Z in the Treatment of Patients With Uncomplicated Coccidioides Pneumonia

The purpose of this study is to determine if nikkomycin Z is safe when administered at different dose levels for 14 days. The study will also determine blood levels and urinary excretion of nikkomycin Z in relation to dose administered. Patients with mild forms of Valley Fever pneumonia will be eligible to participate and will be allocated to receive treatment with nikkomycin Z (various doses) or a placebo. A secondary goal of this study is to evaluate the effectiveness and dose response of nikkomycin Z in an exploratory analysis.

Start Date01 Sep 2007

Sponsor / Collaborator

University of Arizona

100 Clinical Results associated with Chitin synthase

100 Translational Medicine associated with Chitin synthase

0 Patents (Medical) associated with Chitin synthase

874

Literatures (Medical) associated with Chitin synthase

01 Mar 2025·Comparative Biochemistry and Physiology Part C: Toxicology & Pharmacology

miR-9a and miR-10482-5p regulate the expression of chitin synthase and chitinase genes, enhancing lufenuron tolerance in Spodoptera frugiperda

Article

Author: Wu, Mengyan ; Li, Jianhong ; Ma, Kangsheng ; Ling, Shanshan ; Lv, Haixiang ; Guo, Zhimin ; Tang, Jiahui

Spodoptera frugiperda is a significant agricultural pest, severely impacting the yield and quality of grain. Chitin is the momentous component of exoskeletons, which has a significant impact on the growth and development of insects. Our previous study found that exposure to lufenuron can reduce the expression of chitinase gene (SfCHT5) and increase the expression of chitin synthase gene (SfCHSB), two key genes for chitin synthesis in S. frugiperda. However, the post-transcriptional regulatory mechanisms of these key genes in S. frugiperda remain unclear. With miRNA as the entry point, target site prediction, dual luciferase reporter assays, and mimics/inhibitors injection were used to explore the post-transcriptional regulatory mechanism of SfCHSB and SfCHT5. The combined results confirm that miR-10482-5p targets SfCHT5 and regulates its expression, while miR-9a targets and regulates the expression of both SfCHT5 and SfCHSB. Additionally, injection of miR-10482-5p and miR-9a mimic significantly reduced the mortality rates of S. frugiperda treated with lufenuron, increased pupation rate, and emergence rate. These findings underscore the critical regulatory role of miR-10482-5p and miR-9a in modulating the expression of key genes involved in chitin synthesis, thereby enhancing the tolerance of S. frugiperda to lufenuron and influencing its growth and development. In summary, this study preliminarily elucidates the post-transcriptional regulatory mechanisms of miRNA-mediated SfCHSB and SfCHT5 expression.

08 Jan 2025·Journal of Agricultural and Food Chemistry

Enantioselectivity Mechanism of Etoxazole Enantiomers in Tetranychus cinnabarinus: Acaricidal Activity, Metabolic Difference, and Target Binding

Article

Author: Zhang, Ping ; Guo, Xingxing ; He, Lin ; Cheng, Jinhui ; Feng, Kaiyang ; Lin, Ting ; Liu, Peilin ; Xu, Zhifeng ; Wang, Tongyang

Etoxazole, a widely used mite growth inhibitor, contains a chiral center in its chemical structure, resulting in two mirror-image enantiomers. These enantiomers of etoxazole display significant differences in biological activity and environmental behavior. In bioassays conducted against Tetranychus cinnabarinus, it was observed that S-etoxazole demonstrated approximately 279.63 times greater activity against mite eggs compared to R-etoxazole, and its efficacy against adult mites was approximately 5 times higher than that of R-etoxazole. Furthermore, S-etoxazole was found to be more potent in inhibiting chitin synthesis. To elucidate the underlying mechanism for the observed differences in enantiomeric activity, we conducted metabolism assays using crude enzymes, revealing that R-etoxazole undergoes metabolism more readily than S-etoxazole. Subsequent molecular docking and Microscale Thermophoresis (MST) experiments showed that R-etoxazole exhibits weaker binding affinity to the target protein, chitin synthase 1, compared to S-etoxazole. This study thus demonstrates that the differential enantiomeric activity of etoxazole was attributable to a combination of factors, including detoxification metabolism and target protein binding.

11 Dec 2024·Journal of Agricultural and Food Chemistry

Enhancing Mycoprotein Yield: Metabolic Modulation of Chitin Synthase in Fusarium venenatum

Article

Author: Hong, Ruru ; Chen, Wuxi ; Li, Demao ; Chen, Yuxiang ; Tong, Sheng ; Chai, Mengdan ; Liu, Xizhen

Fusarium venenatum is being extensively utilized for microbial protein production. However, its high dietary fiber content results in substantial carbon loss. Inhibition of chitin biosynthesis presents a promising strategy to improve the mycoprotein yield. Through transcriptomic and bioinformatics analyses, chitin synthase gene FvChs3 was identified as crucial for chitin synthesis in F. venenatum. Knockout of the FvChs3 gene resulted in mycelial expansion and a 26% reduction in the chitin content of strain ΔFvChs3. Ethanol production from fermentation decreased by 47%, while the carbon conversion efficiency and protein conversion increased by 16% and 36%, respectively. Transcriptomic analysis revealed an upregulation of nitrogen metabolism in ΔFvChs3, while genes related to the glycolysis pathway for ethanol synthesis were downregulated. Further knockout of pyruvate decarboxylase gene FvPDC6 in ΔFvChs3 accelerated growth, leading to improvements in carbon and protein conversion of 29% and 40%, respectively. This research lays the foundation for enhancing fungal protein production.

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Chitin synthase

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