- |||||||||| chymotrypsin / Generic mfg.
Journal: The Enzyme Effect: Broadening the Horizon of MS Optimization to Nontryptic Digestion in Proteomics. (Pubmed Central) - Jan 13, 2025
We investigated this by conducting LC-MS/MS measurements with different enzymes, including trypsin, Arg-C, Glu-C, Asp-N, and chymotrypsin, at varying collision energies...This optimized method boosts the performance and provides insight into the impact of enzyme specificity. Data sets are available in the MassIVE repository (MSV000095066).
- |||||||||| chymotrypsin / Generic mfg.
Journal: A fluidic device for continuous on-line inductive sensing of proteolytic cleavages. (Pubmed Central) - Jan 12, 2025
Finally, we observe the release of the magnetic particles from the chips under conditions of proteolytic cleavage and measure resulting changes in inductive signals, demonstrating a detection sensitivity for chymotrypsin in the hundreds of nM. The methods we establish here have the potential to aid progress toward sensors comprised of disposable fluidic chips measured by inexpensive detection devices that may one day facilitate ubiquitous protease activity monitoring.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Replacement of a single residue changes the primary specificity of thrombin. (Pubmed Central) - Jan 12, 2025
Consistent with these structural features, a single amino acid replacement (D189A) switches thrombin specificity from trypsin-like to chymotrypsin-like, converting the substrate preference from H-D-Phe-Pro-Arg-p-nitroanilide to H-D-Phe-Pro-Phe-p-nitroanilide and preferential stability enhancement from PPACK to PPPCK. The observation that thrombin specificity is controlled mainly by a single residue establishes a new paradigm in the field of trypsin-like proteases.
- |||||||||| chymotrypsin / Generic mfg.
Journal: The High-Affinity Chymotrypsin Inhibitor Eglin C Poorly Inhibits Human Chymotrypsin-Like Protease: Gln192 and Lys218 Are Key Determinants. (Pubmed Central) - Jan 3, 2025
In order to identify the underlying structural aspects of this unique deviation, we performed comparative molecular dynamics simulations on experimental and AlphaFold model structures of bovine CTRA and human CTRL. Our results indicate that in CTRL, the primary determinants of the observed weak inhibition are amino-acid positions 192 and 218 (using conventional chymotrypsin numbering), which participate in shaping the S1 substrate-binding pocket and thereby affect the stability of the protease-inhibitor complexes.
- |||||||||| NexoBrid (bromelain) / MediWound, Kaken Pharma, Teva
Review, Journal: Proteolytic enzymes and wound debridement: a literature review. (Pubmed Central) - Dec 12, 2024
The advantages of enzymatic debridement over surgical debridement, particularly in nontraumatic applications and with enhanced healing times with the former, underscore its potential in clinical settings. Further research is warranted to optimize use of enzymatic debridement and understand the full scope of benefits and limitations of these enzymes in wound management.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Pharmacological and structural understanding of the Trypanosoma cruzi proteasome provides key insights for developing site-specific inhibitors. (Pubmed Central) - Dec 6, 2024
Using these mutant proteasomes, we show that some selective parasite proteasome inhibitors only partially inhibit the chymotrypsin-like activity, including a newly developed 5-(phenoxymethyl)furan-2-carboxamide-based proteasome inhibitor...This work highlights the need, and provides approaches, to precisely assess proteasome substrate selectivity and pharmacology. It enables structure-guided drug discovery for this promising Chagas disease drug target, provides a new chemical starting point for drug discovery, and paves the road for development of robust proteasome drug discovery programmes for other eukaryotic infectious diseases.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Characterization of the digestive enzymes of juvenile Dormitator latifrons (Richardson, 1844). (Pubmed Central) - Nov 18, 2024
For AR, chymotrypsin was pH 7.0; for the remaining digestive regions, it was pH 9.0-11.0...CaCl2 did not affect enzyme activity except for amylase and lipase (only in PR and HP, respectively). The acid proteolytic activity (pH 2.0) found in AR and the proteolytic inhibition by pepstatin suggest the presence of a stomach.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Cation effects and charge inversion contribute to the electrostatic stabilisation of protein bioconjugates in neat ionic liquids. (Pubmed Central) - Nov 13, 2024
Also, the biocompatibility of DESs towards enzymes can be varied by changing the molar ratios of the constituent components of DESs to facilitate the expansion of applicability of DESs in biocatalysis. myoglobin, ?-chymotrypsin, and regenerated silk fibroin having predominant ?-helical, ?-sheet, and random coiled secondary structures, respectively, were prepared by electrostatic coupling with polyethylene-glycol (PEG)-based polymer-surfactant (PS)...Lower diffusivity of long alkyl chain [MEZ] cations of AIL leads to a depletion zone of IL ions between the two PS-cCT complexes (separation <70
- |||||||||| heparin sodium injection / Generic mfg.
Interaction between Collagen IV and Heparin-Binding Sites in the Activity, Distribution and Clearance of Factor IX(a) (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_4102;
The collagen site had a dominant effect on protease distribution, while the heparin site had similar effects on both zymogen and protease. Disruption of the heparin site modulated the impact of the K5A variant in the protease, and along with the contradictory effects of K5R, suggest potential interaction between these binding sites in the protease.
- |||||||||| chymotrypsin / Generic mfg.
Journal: The Sex Dependent and Independent Effects of Dietary Whey Proteins Are Passed from the Mother to the Offspring. (Pubmed Central) - Nov 4, 2024
Disruption of the heparin site modulated the impact of the K5A variant in the protease, and along with the contradictory effects of K5R, suggest potential interaction between these binding sites in the protease. The effect of whey proteins on growth can be passed from the mother to the offspring without a sex preference, whereas the transmission of gut activity and adiposity are dependent on the sex of the offspring.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Transcriptomic Analysis of the Response of the Dioryctria abietella Larva Midgut to Bacillus thuringiensis 2913 Infection. (Pubmed Central) - Oct 26, 2024
At 12 h after Bt 2913 ingestion, chymotrypsin was potentially involved in degrading the active core fragment of Vip3Aa toxin, and the detoxification enzymes in the larvae contributed to the metabolic detoxification of the Bt toxin...At 24 h after Bt 2913 ingestion, many activated toxins were bound to receptor proteins such as APN in the larval midgut, resulting in membrane perforation. Here, we clarified the mechanism of Bt 2913 infection in D. abietella larvae, as well as the larval immune defense response to Bt 2913, which provides a theoretical basis for the subsequent control of D. abietella using B. thuringiensis.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Drug Combination Studies of Isoquinolinone AM12 with Curcumin or Quercetin: A New Combination Strategy to Synergistically Inhibit 20S Proteasome. (Pubmed Central) - Oct 16, 2024
Within the 20S proteasome barrel-like structure, the catalytic subunits, ?1, ?2 and ?5, are responsible for different proteolytic activities: caspase-like (C-L), trypsin-like (T-L) and chymotrypsin-like (ChT-L), respectively...In the case of the combination AM12 + curcumin, an increasing synergism was observed from 50% to 90% of proteasome inhibition, while in the case of the combination AM12 + quercetin an additive effect was observed only from 50% to 70% of ?5 subunit inhibition. These results suggest that combining AM12 with curcumin is a more promising strategy than combining it with quercetin for potential therapeutic applications, especially in treating tumors.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Synthesis and Optimization of Small Molecule Inhibitors of Prostate Specific Antigen. (Pubmed Central) - Sep 20, 2024
Further, we also evaluated the selectivity profile of compound 20 (CDD-3290) by testing against closely related proteases and demonstrated excellent inhibition of PSA versus ?-chymotrypsin and elastase and similar potency versus thrombin. Thus, compound 20 is an improved PSA inhibitor that can be tested for efficacy in vitro or in the female reproductive tract.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Plasma Biochemistry, Intestinal Health, and Transcriptome Analysis Reveal Why Laying Hens Produce Translucent Eggs. (Pubmed Central) - Sep 14, 2024
Enrichment analysis showed that the up-regulated genes, such as GSTT1, GSTO2, and GSTA3, were mostly enriched in metabolism of xenobiotics by cytochrome P450, drug metabolism-cytochrome P450, and oxidative phosphorylation pathways. The results of our study indicate that plasma lipid metabolism disorder, decreased intestinal antioxidant capacity, and altered intestinal metabolism capabilities may influence the formation of translucent eggs.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Alternating vs. random amphiphilic polydisulfides: aggregation, enzyme activity inhibition and redox-responsive guest release. (Pubmed Central) - Sep 9, 2024
Furthermore, the well-ordered assembly of P1 exhibited an excellent surface-functional group display (zeta potential of -32 mV compared to -14 mV for P2), which resulted in the effective recognition of the ?-chymotrypsin (Cht) protein surface by electrostatic interaction. Consequently, P1 significantly (>70%) suppressed the enzymatic activity of Cht, while in the presence of P2, the enzyme was still active with >70% efficacy.
- |||||||||| chymotrypsin / Generic mfg.
Journal: A homo-FRET assay for patatin-specific proteolytic activity. (Pubmed Central) - Sep 8, 2024
Consequently, P1 significantly (>70%) suppressed the enzymatic activity of Cht, while in the presence of P2, the enzyme was still active with >70% efficacy. For Chymotrypsin, BODIPY-patatin provided a 39
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Defatted Wheat Germ Protein-Derived Peptides Showed Multiple Biological Activities from the Stomach to Small Intestine: In Silico and In Vitro Approaches. (Pubmed Central) - Sep 4, 2024
In this work, in silico digestion of these peptides with trypsin, thermolysin, and chymotrypsin produced 67 peptide fragments...For DPP-IV inhibition, their IC50 values were 0.5, 1.6, and 4.0 mM, respectively. This research pioneers new directions in the emerging field of multifunctional peptides, providing scientific evidence to support the utilization of wheat germ as value-added food ingredients.
- |||||||||| Tudcabil (tauroursodeoxycholic acid) / Bruschettini
Preclinical, Journal: A common CTRB misfolding variant associated with pancreatic cancer risk causes ER stress and inflammation in mice. (Pubmed Central) - Sep 1, 2024
The pancreas of homozygous mutant mice displays reduced chymotrypsin activity and total protein synthesis...Administration of TUDCA or sulindac partially alleviates the phenotype...- Truncated CTRB1 misfolds and accumulates in the ER; yet, mutant mice display a histologically normal pancreas at 3 months age.- CTRB1 and associated chaperones colocalize in the ER, the cytoplasm, and the nucleus of acinar cells.- Transcriptomics analysis reveals reduced activity of the acinar program and increased activity of pathways involved in ER stress, unfolded protein response, and inflammation.- Mutant mice are sensitized to pancreatic damage and do not recover properly from a mild caerulein-induced pancreatitis.- TUDCA administration partially relieves the ER stress in mutant mice.How might it impact on clinical practice in the foreseeable future?: - The new mouse model provides a tool to identify the mechanisms leading to increased pancreatic cancer risk in CTRB2 exon 6 carriers. - The findings suggest that drugs that cause ER stress relief and/or reduce inflammation might provide preventive opportunities.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Multi-Omics Revealed Resveratrol and ?-Hydroxy-?-methyl Butyric Acid Alone or in Combination Improved the Jejunal Function in Tibetan Sheep. (Pubmed Central) - Aug 31, 2024
The results showed that RES and HMB improved the antioxidant capacity (CAT, GSH-Px, SOD, and T-AOC), immunity (IgA, IgG, and IgM), and digestive enzyme activity (?-amylase, lipase, and chymotrypsin) of the experimental lambs (p < 0.05)...Metabolome analysis revealed that alpha ketoglutarate, succinic semialdehyde, and diacetyl as well as butanoate metabolism pathways connected to the improvements in butyrate concentration by RES and (or) HMB supplementation. Collectively, our results suggested that RES and (or) HMB supplementation improved butyrate concentration via regulating the microbial community (Methanobrevibacter, Actinobacteriota and Bacillus) and metabolism (alpha ketoglutarate, succinic semialdehyde, and diacetyl), thus contributing to jejunal morphology, antioxidant capacity, immune response, digestive enzyme activity, and barrier function.
- |||||||||| chymotrypsin / Generic mfg.
Journal: How D-amino acids embedded in the protein sequence modify its digestibility: Behaviour of digestive enzymes tested on a model peptide used as target. (Pubmed Central) - Aug 24, 2024
In this work the behaviour of the main stomach and gut digestive enzymes (pepsin, trypsin, and chymotrypsin) in the presence of D-amino acids in the protein chain was monitored over time using a model peptide, Ac-LDAQSAPLRVYVE-NH2 (belonging to ?-lactoglobulin, position 48-60), where L-amino acids were systematically substituted by D-amino acids...The effect seemed more pronounced in the case of pepsin rather than the gut enzymes, possibly indicating a better resilience of the upper gut phase of digestion to racemization. These results demonstrated that racemization could impair nutritional value by slowing down digestibility and has different effects according to the enzyme/amino acids involved.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Typical structural characteristics and hepatoprotective effects of novel high Fischer ratio oligopeptides from Antarctic krill on acute alcoholic liver injury. (Pubmed Central) - Aug 20, 2024
Herein, HFOPs-AK, with a Fischer ratio of 29 g/g (40.22 mol/mol) (MW < 1000 Da), were prepared via two-step enzymatic hydrolysis using chymotrypsin and flavourzyme and aromatic amino acid removal...Additionally, HFOPs-AK (800 mg per kg bw per d) attenuated liver inflammation by down-regulating the mRNA levels of TNF-?, IL-1?, and IL-6 by 40.45%, 38.48%, and 35.83%, respectively. Therefore, HFOPs-AK may have the potential as a new nutritional supplement for the treatment of alcoholic liver injury.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Secretagogue-induced pancreatitis in mice devoid of chymotrypsin. (Pubmed Central) - Aug 19, 2024
Taken together, the results confirm and extend prior observations demonstrating that chymotrypsin safeguards the pancreas against pancreatitis by limiting pathologic trypsin activity. In mice, the CTRB1 isoform, which constitutes about 90% of the total chymotrypsin content, is responsible primarily for the anti-trypsin defenses and protection against pancreatitis, however, the minor isoform CTRL also contributes to an appreciable extent.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Pancreas and pancreatitis: Exocrine pancreatic insufficiency. (Pubmed Central) - Aug 6, 2024
In this review, we discuss the nuances of diagnosis and management of EPI in CF. We also present emerging evidence on the effects of CFTR modulating agents on the management of EPI, and speculate that these medications may lead to greater heterogeneity in management of EPI in CF moving forward.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Crystal structures of the 3C proteases from Coxsackievirus B3 and B4. (Pubmed Central) - Aug 5, 2024
The crystal structures were solved by the molecular-replacement method and contained a typical chymotrypsin-like fold and a conserved His40-Glu71-Cys147 catalytic triad. Comparison with the structures of 3C proteases from other enteroviruses revealed high similarity with minor differences, which will guide the design of 3C-targeting inhibitors with broad-spectrum properties.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Cryomilled electrospun nanofiber mats containing d-mannitol exhibit suitable for aerosol delivery of proteins. (Pubmed Central) - Jul 31, 2024
Dry powders were prepared by cryomilling nanofiber mats composed of polyvinyl alcohol, D(-)-mannitol (Man), and ?-chymotrypsin (?-Chy) as the model drug using the electrospinning method...Furthermore, single inhalation induced no significant lung tissue damage as evidenced by lactate dehydrogenase activity assays of mouse bronchoalveolar lavage fluid. This novel DPI formulation process may facilitate the safe and efficient inhalational delivery of therapeutic proteins.
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