- |||||||||| Nucynta (tapentadol) / Collegium Pharma, Grunenthal
Journal: Effects of Different Opioid Drugs on Oxidative Status and Proteasome Activity in SH-SY5Y Cells. (Pubmed Central) - Dec 12, 2022
In fact, while prolonged morphine exposure significantly increased the proteolytic activity of both subunits and β5 mRNA levels, buprenorphine and tapentadol either reduced or did not alter these parameters. These results, showing different actions of the selected opioid drugs on the investigated parameters, suggest that a low µ receptor intrinsic efficacy could be related to a smaller oxidative stress and proteasome activation and could be useful to shed more light on the role of the investigated cellular processes in the occurrence of these opioid drug side effects.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Embryonic alcohol exposure disrupts the ubiquitin-proteasome system. (Pubmed Central) - Dec 9, 2022
Furthermore, pharmacologic inhibition of chymotrypsin-like proteasome activity potentiates the teratogenic effects of EAE on craniofacial structure, the nervous system, and the endoderm. Our studies identify the proteasome as a target of EtOH exposure and signify that UPS disruptions contribute to craniofacial, neurological, and endodermal phenotypes in FASDs.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Functional dynamics of SARS-CoV-2 3C-like protease as a member of clan PA. (Pubmed Central) - Dec 8, 2022
SARS-CoV-2 3C-like protease (3CL), a potential therapeutic target for COVID-19, consists of a chymotrypsin fold and a C-terminal α-helical domain (domain III), the latter of which mediates dimerization required for catalytic activation...As a reference, monomeric 3C proteases belonging to the more distant family Picornaviridae (family C3) lacking domain III are compared with C30, and it is shown that the 3C proteases are rigid enough to maintain their structures in the active state. The online version contains supplementary material available at 10.1007/s12551-022-01020-x.
- |||||||||| Hemlibra (emicizumab-kxwh) / Roche
Factor VIII Mimetic Rescue of Hemophilia B Causing Factor IX Variants ((VIRTUAL PROGRAM)) - Dec 7, 2022 - Abstract #ASH2022ASH_8118;
Identified rescuable variants likely has dysfunctional FVIIIa-binding (K5E, L6S) and/or disturbed allosteric activation (E387K, I397T). FVIII mimetics may be an alternative prophylactic hemostatic therapy for HB patients with such rescuable variants.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Fast quinazolinone synthesis by combining enzymatic catalysis and photocatalysis. (Pubmed Central) - Nov 30, 2022
The α-Chymotrypsin catalyzed the cyclization of aldehyde and 2-aminobenzamide, which was subsequently followed by White LED-induced oxidation of 2-phenyl-2, 3-dihydroquinazolin-4(1H)-one to obtain quinazolinone...Furthermore, the plausible mechanism was investigated by control experiments and DFT calculations. This protocol provides an alternative synthetic route for the preparation of quinazolinone derivatives.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Exploring the Interactive Effects of Thymol and Thymoquinone: Moving towards an Enhanced Performance, Gross Margin, Immunity and Aeromonas sobria Resistance of Nile Tilapia (Oreochromis niloticus). (Pubmed Central) - Nov 16, 2022
Notably, the expression of the genes encoding digestive enzymes (pepsinogen, chymotrypsinogen, α-amylase and lipase) and muscle and intestinal antioxidant enzymes (glutathione peroxidase, catalase and superoxide dismutase) was significantly upregulated in Thy/ThQ-fed fish...Furthermore, Thy/ThQ protective effect against A. sobria was evidenced via downregulating the expression of its aero and hly virulence genes with higher fish survival rates. Overall, the current study encouraged the inclusion of Thy/ThQ in fish diets to boost their growth rates, promote digestive and antioxidant genes expression, improve their immune responses and provide defense against A. sorbia infections with great economic benefits.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Potential toxicity of bisphenol A to α-chymotrypsin and the corresponding mechanisms of their binding. (Pubmed Central) - Nov 16, 2022
The above phenomenon explained the result that the activity of α-chymotrypsin increased to 139% when exposed to high dose BPA (40 μM). Taken together, the effects of BPA on the structure and function of α-chymotrypsin were clarified at the molecular level, which made up the gap in the mechanism of BPA on the proteolytic enzyme, and provided a reliable basis for disease avoidance and prevention.
- |||||||||| chymotrypsin / Generic mfg.
Journal: From Nature to Synthetic Compounds: Novel 1(N),2,3 Trisubstituted-5-oxopyrrolidines Targeting Multiple Myeloma Cells. (Pubmed Central) - Nov 16, 2022
The ability of the most effective molecules to inhibit the proteasome was evaluated and the binding mode of the most promising compounds in the proteasome chymotrypsin binding pocket was deciphered through molecular modeling simulations. Compounds 13 and 14 are more potent than Hib-ester, demonstrating that our strategy was suitable for the identification of a novel chemotype for developing possible drug candidates and hopefully widening the drug armamentarium against MM.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Uncovering a Subtype of Microviridins via the Biosynthesis Study of FR901451. (Pubmed Central) - Nov 15, 2022
Furthermore, in vivo gene coexpression facilitated the production of chitinoviridin A1 (FR901451) and two novel microviridin-class compounds chitinoviridin A2A and chitinoviridin A2B, with an extra macrolactone ring. All of these peptides showed potent inhibitory effects against elastase and chymotrypsin independently.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: In vivo developmental studies of Helicoverpa armigera and in silico molecular interactions with trypsin reveal the bio-insecticidal potential of trypsin inhibitor (SSTI) isolated from Solanum surattense. (Pubmed Central) - Nov 15, 2022
Gene expression studies revealed down regulation in trypsin (HaTry 1, 2, 3, 4, 6, 8) and chymotrypsin (HaChy 1, 2, 3, 4) genes of the larval gut upon treatment of SSTI...Molecular dynamic (MD) simulation revealed the stable interactions of the rigid CIL of SSTI at the active site of trypsin, leading to its destabilization. Conserved lysine63 of the P1 site in SSTI forms a strong hydrogen bonding network with residues Asp189 and Ser190 of trypsin.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Investigation of the Expression of Serine Protease in Vibrio vulnificus. (Pubmed Central) - Nov 12, 2022
vulnificus NCIMB2137, a metalloprotease-negative strain isolated from a diseased eel, produces a 45-kDa chymotrypsin-like alkaline serine protease known as VvsA...Although serine proteases were produced, they were cleaved at different sites and no active mature forms were detected. These results indicate that the operon encoding vvsA and vvsB is a gene constructed to be specifically expressed in V. vulnificus.
- |||||||||| chymotrypsin / Generic mfg.
Chymotrypsinogen C (CTRC) promoter mutations are not associated with chronic pancreatitis (Coastal 1-5) - Nov 7, 2022 - Abstract #APAPancreatic2022APA_Pancreatic_225;
The identified genetic variants in the 1.4 kb long 5’ upstream region of the CTRC gene are not associated with chronic pancreatitis. Accumulation of the c.-913A > G variant in patients can be explained by its linkage with the known pathogenic c.180C > T mutation.
- |||||||||| Hemlibra (emicizumab-kxwh) / Roche
Factor VIII Mimetic Rescue of Hemophilia B Causing Factor IX Variants (ENMCC - Hall D) - Nov 4, 2022 - Abstract #ASH2022ASH_3870;
Identified rescuable variants likely has dysfunctional FVIIIa-binding (K5E, L6S) and/or disturbed allosteric activation (E387K, I397T). FVIII mimetics may be an alternative prophylactic hemostatic therapy for HB patients with such rescuable variants.
- |||||||||| CM-AT / Curemark
Enrollment change: A Trial of CM-AT in Children With Autism With All Levels of FCT (The Blum Study) (clinicaltrials.gov) - Oct 26, 2022
P3, N=190, Completed,
The application of TESB in enzyme immobilization has the potential to facilitate a greater degree of enzymatic digestion with higher sequence coverage than traditional immobilization or crosslinking reagents for bottom-up proteomics. N=335 --> 190
- |||||||||| Gilotrif (afatinib) / Boehringer Ingelheim
Journal: Virtual screening of quinoline derived library for SARS-COV-2 targeting viral entry and replication. (Pubmed Central) - Oct 19, 2022
An in-depth analysis of the interactions and G-score compared to the controls like hydroxyquinoline and remdesivir has been presented...Further MD simulations and MM-PBSA calculations showed that afatinib works best to interfere with the the activity of RNA dependent RNA polymerase of SARS-COV-2, thereby inhibiting replication process of single stranded RNA virus. Communicated by Ramaswamy H. Sarma.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Novel inhibitors and activity-based probes targeting serine proteases. (Pubmed Central) - Oct 18, 2022
This present study provides synthetic details for the preparation of additional examples of this ABP chemotype, which function as potent irreversible inhibitors of their respective target serine protease. We describe their use for the activity-based profiling of a broad range of serine proteases including trypsin, the trypsin-like protease plasmin, chymotrypsin, cathepsin G, and neutrophil elastase (NE), including the profiling of the latter protease in clinical samples obtained from patients with cystic fibrosis.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Phytochemical, enzymatic and biological studies of root extracts of Farsetia hamiltonii Royle. (Pubmed Central) - Oct 18, 2022
The dichloromethane extract possesses significant lipoxygenase, chymotripsin and cholinesterase enzyme inhibition activities, whereas methanol extract possess lipoxygenase, alpha glucosidase, chymotrypsin and acetylcholinesterase enzyme inhibition activities...The enzyme inhibition assays on anti-cholinesterase, anti-alpha glucosidase, antilipoxygenase, antichymotripsin and antibacterial activities were found significant for the extracts of root parts of F. hamiltonii. Therefore, results of this study justify folkloric therapeutic potential of F. hamiltonii root in treating diabetes, inflammations and infectious diseases.
- |||||||||| chymotrypsin / Generic mfg.
Journal: The Effect of Supplemental Concentrate Feeding on the Morphological and Functional Development of the Pancreas in Early Weaned Yak Calves. (Pubmed Central) - Oct 15, 2022
(5) The main differential metabolites of the pancreas in the test group were significantly higher than those of the control group, such as D-proline, hypoxanthine, acetylcysteine, gamma-glutamylcysteine, thiazolidine-4-carboxylic acid, piperidinic acid, ellagic acid, nicotinamide, tropolone, D-serine, ribulose-5-phosphate, (+/-)5(6)-epoxyeicosatrienoic acid(EET), 2-hydroxycinnamic acid, L-phenylalanine, creatinine, tetrahydrocorticosterone, pyridoxamine, xanthine, 5-oxoproline, asparagine, DL-tryptophan, in-dole-3-acrylic acid, thymine, trehalose, docosapentaenoic acid, docosahexaenoic acid, fatty acid esters of hydroxy fatty acids(FAHFA) (18:1/20:3), fatty acid esters of hydroxy fatty acids(FAHFA) (18:2/20:4), adrenic acid and xanthosine. In conclusion, supplemental concentrate feeding promoted the good development of morphological and functional properties of the pancreas in early weaned yak calves to improve the digestion and absorption of feed nutrients, so as to enhance the growth and development quality of early weaned yak calves.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Supplemental Enzyme and Probiotics on the Growth Performance and Nutrient Digestibility of Broilers Fed with a Newly Harvested Corn Diet. (Pubmed Central) - Sep 25, 2022
Compared to the newly harvested corn diet (NC), supplemental enzyme of DE increased the activity of chymotrypsin (p = 0.016), however, no differences in the digestibility of three kinds of organic matter, digesta emptying time, visual fecal water content, or performance were found...Pediococcus acidilactici BCC-1 (10 cfu/kg), protease (800,000 U/g) individually, or protease (800,000 U/g) in combination with glucoamylase (800,000 U/g) were supplemented in newly harvested corn diets for growing broilers. Hence, this study mainly explores the alleviation effect of enzyme and probiotics on the negative phenomenon caused by the utilization of newly harvested corn in broilers and provides a better solution for the utilization of newly harvested corn in production practice.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal, IO biomarker: Alpha-Chymotrypsin Protects Against Acute Lung, Kidney, and Liver Injuries and Increases Survival in CLP-Induced Sepsis in Rats Through Inhibition of TLR4/NF-κB Pathway. (Pubmed Central) - Sep 20, 2022
α-ch has protective potential against sepsis through lowering tissue expression of TLR4, NF-κB, MPO, and iNOS leading to decreased oxidative stress and inflammatory signals induced by sepsis. This effect appeared to alleviate the damage to the lungs, liver, and kidneys and increase survival in rats subjected to sepsis.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Methionine played a positive role in improving the intestinal digestion capacity, anti-inflammatory reaction and oxidation resistance of grass carp, Ctenopharyngodon idella, fry. (Pubmed Central) - Sep 20, 2022
After an 8-week breeding experiment, the results revealed that 0.71%-1.20% dietary methionine levels markedly upregulated the mRNA levels of intestinal digestion including trypsin, amylase, chymotrypsin and AKP, and 0.71%-0.87% dietary methionine level significantly increased intestinal trypsin activities compared with the 0.33% dietary methionine level...In summary, 0.71%-1.20% dietary methionine levels played a positive role in improving the intestinal digestion capacity of digestion, anti-inflammatory reaction and oxidation resistance of grass carp fry. This study provided a theoretical basis for improving the survival rate and growth of grass carp fry.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Protein Myristoylation Plays a Role in the Nuclear Entry of the Parvovirus Minute Virus of Mice. (Pubmed Central) - Sep 20, 2022
We also showed, in addition to protein myristoylation, a chymotrypsin-like activity, which may come from cellular proteasomes, is required for MVM to get myristoylated and enter the nucleus. These findings deepen our understanding on how MVM and other related PVs infect host cells and provide new insights for the development of PV-based anti-cancer therapies.
- |||||||||| chymotrypsin / Generic mfg.
Journal: The effects of dietary ellagic acid supplementation on growth performance, immune response, antioxidant activity, digestive enzyme activities, and intestinal functions in yellow-feathered broilers. (Pubmed Central) - Sep 11, 2022
The inclusion of 200 mg/kg EA in the broiler diets increased intestinal chymotrypsin, pepsin, and lipase activities (P < 0.05)...Moreover, in birds fed EA-containing diets, the levels of acetate, butyrate, and total short-chain fatty acids in the cecum were higher (P < 0.05) than those in control birds. These findings indicated that dietary EA had ameliorative effects on antioxidant capability, digestive enzyme activity, immune function and intestinal functions, which led to strengthened growth performance.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Proteasome activator 28γ (PA28γ) allosterically activates trypsin-like proteolysis by binding to the α-ring of the 20S proteasome. (Pubmed Central) - Sep 10, 2022
Alternative hypotheses have been proposed for the molecular mechanism of PA28γ, including the following: (1) substrate selection, (2) allosteric upregulation of the trypsin-like (T-L) site, (3) allosteric inhibition of the chymotrypsin-like (CT-L) and caspase-like (C-L) sites, (4) conversion of the CT-L or C-L sites to new T-L sites, and (5) gate opening alone or in combination with a previous hypothesis...Finally, using Cryo-EM, we visualized the PA28γ-proteasome complex at 4.3 Å and confirmed its expected quaternary structure and proteasome binding mode. The results of this study provide unambiguous evidence that PA28γ can function by binding the 20S proteasome to allosterically activate the Trypsin-like proteolytic site.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Effect of Protein-Protein Interactions on Translational Diffusion of Spheroidal Proteins. (Pubmed Central) - Sep 3, 2022
These proteins are rigid globular α-chymotrypsin (ChTr) and human serum albumin (HSA), and partly disordered α-casein (α-CN) and β-lactoglobulin (β-Lg)...The decrease of van der Waals interactions for β-Lg is probably associated with the formation of stable oligomers by this protein. The PPI, estimated with the help of interaction potential and idealized spherical molecular geometry, are in good agreement with experimental data.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Dry Powder Inhalers for Proteins Using Cryo-Milled Electrospun Polyvinyl Alcohol Nanofiber Mats. (Pubmed Central) - Sep 3, 2022
The milled nanofiber mats were successfully prepared, while retaining the enzymatic activity of α-chymotrypsin; furthermore, the activity of milled fiber mats that had been stored for 6 months was comparable to the activity of those that were freshly prepared. This novel method may be suitable for the DPI preparation of various drugs because it avoids the heating step during the DPI preparation process.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: A Mouse Model of Celiac Disease. (Pubmed Central) - Aug 24, 2022
Detailed protocols to prepare pepsin-trypsin digested gliadin (PT-gliadin) or chymotrypsin-digested gliadin (CT-gliadin), which allow antibody detection against native or deamidated gluten peptides, are also provided in this unit...Current Protocols published by Wiley Periodicals LLC. Basic Protocol 1: Induction of celiac-like disease in DQ8-D -villin-IL-15tg mice Basic Protocol 2: Histological assessment of villous atrophy Support Protocol 1: Morphometric assessment of villous/crypt ratio Support Protocol 2: Evaluation of epithelial cells renewal Support Protocol 3: Evaluation of the density of intraepithelial lymphocytes Basic Protocol 3: Analysis of cytotoxic intraepithelial lymphocytes Basic Protocol 4: Transglutaminase 2 activation and measurement of antibodies against native and deamidated gluten peptides Support Protocol 4: Preparation of CT-gliadin Support Protocol 5: Preparation of PT-gliadin.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Transesterification of Non-Activated Esters Promoted by Small Molecules Mimicking the Active Site of Hydrolases. (Pubmed Central) - Aug 24, 2022
The high reaction rates and specificity showed by natural hydrolases presents an attractive target, and yet the preparation of suitable small molecule mimics remains challenging, requiring activated substrates to achieve productive outcomes. Here we present small synthetic artificial enzymes which mimic the catalytic site and the oxyanion hole of chymotrypsin and N-terminal hydrolases and are able to perform, for the first time, the transesterification of a non-activated ester such as ethyl acetate with methanol under mild and neutral reaction conditions.
- |||||||||| chymotrypsin / Generic mfg.
Journal: A proteomics approach reveals digestive and nutritional responses to food intake in anadromous Coilia nasus. (Pubmed Central) - Aug 22, 2022
In addition to gastric acid secretion caused by gastric distention, a functional analysis suggested that a series of DEPs were involved mainly in the regulation of protein digestion (e.g., carboxypeptidase A1 and chymotrypsin A-like), immune response (e.g., lysozyme and alpha 2-macroglobulin), and nutrition metabolism (e.g., glyceraldehyde 3-phosphate dehydrogenase, glycogenin, long-chain acyl-CoA synthetase, and creatine kinase)...These results indicate that the nutrients obtained through food were effectively utilized by C. nasus, thereby providing energy for swimming, gonadal maturation, primary metabolism, and an enhanced immune function to better resist pathogen interference. This research contributes to the elucidation of nutritional regulation mechanisms of C. nasus to better protect the wild population.
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