- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Pancreatitis severity in mice with impaired CFTR function but pancreatic sufficiency is mediated via ductal and inflammatory cells-Not acinar cells. (Pubmed Central) - Oct 6, 2021
Protease activation and necrosis were investigated in isolated acini, disease severity over 24h, pancreatic function by MRI, isolated duct stimulation and faecal chymotrypsin, and leucocyte function by ex vivo lipopolysaccharide (LPS) stimulation...LPS stimulation of splenocytes from CFTR resulted in increased INF-γ and IL-6, but decreased IL-10 secretion. CFTR mutations that preserve residual pancreatic function significantly increase the severity of experimental pancreatitis-mostly via impairing duct cell function and a shift towards a pro-inflammatory phenotype, not by rendering acinar cells more susceptible to pathological stimuli.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Female Mice Reaching Exceptionally High Old Age Have Preserved 20S Proteasome Activities. (Pubmed Central) - Sep 29, 2021
The results show different age-related changes depending on the tissue and the activity considered, so there is no universal decline in proteasome function with age in female mice. Interestingly, exceptionally old mice displayed better maintained proteasome activities, suggesting that preserved 20S proteasome is associated with successful aging.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Reversible Photoswitchable Inhibitors Generate Ultrasensitivity in Out-of-Equilibrium Enzymatic Reactions. (Pubmed Central) - Sep 29, 2021
Utilizing a chromophore/warhead strategy, PIs of the protease α-chymotrypsin were synthesized, which led to the discovery of inhibitors with large differences in inhibition constants (K) for the different photoisomers...Upon irradiation of the continuously stirred tank reactor with different light pulse sequences, i.e., varying the pulse duration or frequency of UV and blue light irradiation, reversible switching between photoisomers resulted in ultrasensitive responses in enzymatic activity as well as frequency filtering of input signals. This general and modular strategy enables reversible and tunable control over the kinetic rates of individual enzyme-catalyzed reactions and makes a programmable linkage of enzymes to a wide range of network topologies feasible.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Decoding the Papain Inhibitor from Streptomyces mobaraensis as Being Hydroxylated Chymostatin Derivatives: Purification, Structure Analysis, and Putative Biosynthetic Pathway. (Pubmed Central) - Sep 22, 2021
Chymotrypsin and papain were both inhibited by the SPI compounds in the low nanomolar range...The crystal structure of one of these chymostatin variants confirmed its molecular structure and revealed a S-configured hemithioacetal bond with the catalytic Cys25 thiolate as well as close interactions with hydrophobic S1 and S2 subsite amino acids. A model for chymostatin biosynthesis is provided based on the discovery of clustered genes encoding several putative nonribosomal peptide synthetases; among them, there is the unusual CstF enzyme that accommodates two canonical amino acid activation domains as well as three peptide carrier protein domains.
- |||||||||| chymotrypsin / Generic mfg.
Clinical, Journal: Clinical interpretation of SPINK1 and CTRC variants in pancreatitis. (Pubmed Central) - Sep 19, 2021
Since the description of the SPINK1 gene encoding the serine protease inhibitor Kazal type 1 and the CTRC gene encoding the Chymotrypsin C as being involved in chronic pancreatitis, more than 56 SPINK1 and 87 CTRC variants have been reported...This classification was based on the results of in vitro experiments, in silico analysis using different prediction tools, and on population data, in comparing the allelic frequency of each variant in patients with pancreatitis and in unaffected control individuals. This review should help geneticists and clinicians in charge of patient's care and genetic counseling to interpret the results of genetic studies.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Role of Thrombin in Central Nervous System Injury and Disease. (Pubmed Central) - Sep 19, 2021
Thrombin is a Na-activated allosteric serine protease of the chymotrypsin family involved in coagulation, inflammation, cell protection, and apoptosis...In this review, we explore the mechanisms of thrombin action, localization, and functions in the central nervous system and describe the involvement of thrombin in stroke and intracerebral hemorrhage, neurodegenerative diseases, epilepsy, traumatic brain injury, and primary central nervous system tumors. We aim to comprehensively characterize the role of thrombin in neurological disease and injury.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Molecular Dynamics-Guided Design of a Functional Protein-ATRP Conjugate That Eliminates Protein-Protein Interactions. (Pubmed Central) - Sep 16, 2021
Using chymotrypsin, an important enzyme that is used to treat pancreatic insufficiency, we have designed a series of molecular chimeras with varied grafting densities and shapes...Atomistic molecular dynamic simulations predicted that a dense nanoarmor with long-armed comb-shaped polymer would act as an almost perfect molecular sieve to filter large ligands from substrates. Surprisingly, a conjugate that was composed of 99% polymer was needed before the elimination of protein-protein interactions.
- |||||||||| Psoralen / EMD Serono
Journal: Synthesis and Biochemical Evaluation of Warhead-Decorated Psoralens as (Immuno)Proteasome Inhibitors. (Pubmed Central) - Sep 11, 2021
Despite mapping the chemical space with different warheads, all compounds showed decreased inhibition of the β5i subunit of immunoproteasome in comparison to the parent oxathiazolone-based compound. Although suboptimal, these results provide crucial information about structure-activity relationships that will serve as guidance for the further design of (immuno)proteasome inhibitors.
- |||||||||| ceftriaxone / Generic mfg.
Whipple’s Disease Diagnosed by Enteroscopy: A Rare Case of a Young Male in the United States (Shoreline Exhibit Hall) - Sep 8, 2021 - Abstract #ACG2021ACG_2043;
Fecal elastase and chymotrypsin were within normal range...The patient was treated with 2g IV Ceftriaxone...Whipple’s disease should be considered in patients with chronic diarrhea and weight loss of unknown origins after extensive initial workup, even in the absence of classic symptoms or risk factors for transmission. Clinicians must always remain vigilant of this infectious etiology under these circumstances as a delay in diagnosis leads to considerable morbidity and possible mortality.
- |||||||||| chymotrypsin / Generic mfg.
Journal: A Molecular Probe with Both Chromogenic and Fluorescent Units for Detecting Serine Proteases. (Pubmed Central) - Sep 5, 2021
In the case of nattokinase, both the fluorescence emission and UV absorbance slowly increased. In contrast, the increasing UV absorbance was saturated at the early stage of the reaction of the present probe with chymotrypsin, whereas the fluorescence emission continuously increased in the following stages.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Peracetic Acid-Ethanol Processed Human Tendon Allograft: A Morphological, Biochemical, and Biomechanical Study In Vitro. (Pubmed Central) - Sep 4, 2021
In contrast, the increasing UV absorbance was saturated at the early stage of the reaction of the present probe with chymotrypsin, whereas the fluorescence emission continuously increased in the following stages. PES treatment for 30 min has no adverse effect on the properties of human hamstring tendon allografts, longer processing time could not promise better properties preservation.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Serpins in Fasciola hepatica: insights into host-parasite interactions. (Pubmed Central) - Sep 2, 2021
Biochemical characterisation revealed that recombinant FhS-2 (rFhS) inhibits the activity of human neutrophil cathepsin G, while rFhS-4 inhibits the activity of bovine pancreatic chymotrypsin and cathepsin G. Consistent with inhibitor function profiling data, rFhS-4 inhibited cathepsin G-activated platelet aggregation in a dose-responsive manner.Similar to other serpins, rFhS2 and rFhS-4 bind to heparin with high affinity...These findings provide the basis for study of functional roles of these proteins as part of an immune evasion mechanism in the adult fluke, and in protection of eggs to ensure parasite life cycle continuity. Further understanding of serpins from the liver fluke may lead to the discovery of novel anti-parasitic interventions.
- |||||||||| chymotrypsin / Generic mfg.
Journal: The dataset of predicted trypsin serine peptidases and their inactive homologs in Tenebrio molitor transcriptomes. (Pubmed Central) - Aug 31, 2021
We used RNA-Seq transcriptome data from T. molitor to annotate trypsin-like sequences from the chymotrypsin S1 family of serine peptidases, including sequences of active serine peptidases (SerP) and their inactive homologs (SerPH) in T. molitor transcriptomes...The length of preproenzyme and mature form of the predicted enzyme, position of signal peptide and proenzyme cleavage sites, molecular mass, active site and S1 substrate binding subsite residues, and transmembrane and regulatory domains were analyzed using bioinformatic tools. The data can be used for further physiological, biochemical, and phylogenetic study of tenebrionid pests and other animal systems.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Intestinal Exposure to Food-Derived Protease Inhibitors: Digestion Physiology- and Gut Health-Related Effects. (Pubmed Central) - Aug 28, 2021
Plant-derived protease inhibitors (PI), such as Bowman-Birk inhibitors and Kunitz-type inhibitors, have been suggested to negatively affect dietary protein digestion by blocking the activity of trypsin and chymotrypsin in the human gastrointestinal system...The aim of this review was to evaluate the relevance of PIs in protein digestion in humans and to discuss the potential of PIs from whole foods and as purified compounds in decreasing symptoms of bowel-related conditions. Based on the reviewed literature, we concluded that while the complex interactions affecting plant protein digestibility and bioavailability remain unclear, PI supplements could be considered for targeted purposes to mitigate inflammation and gastric pain.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Purification and Biological Function of Caldecrin. (Pubmed Central) - Aug 27, 2021
Caldecrin, or chymotrypsin-like elastase, was originally identified in the pancreas as a serum calcium-decreasing factor...The ectopic intramuscular expression of caldecrin cDNA prevents bone resorption in ovariectomized mice, and the administration of caldecrin protein also prevents skeletal muscle destruction in dystrophic mice. In vivo and in vitro studies have indicated that caldecrin is a unique multifunctional protease and a possible therapeutic target for skeletal and inflammatory diseases.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Changes in digestive enzyme activities during the early ontogeny of the South American cichlid (Cichlasoma dimerus). (Pubmed Central) - Aug 27, 2021
Chymotrypsin, L-aminopeptidase, and carboxypeptidase A activities increased at 6 dah, while trypsin activity was first detected on 13 dah and reached its maximum activity on 17 dah...The enzymatic activity analyzes indicate the digestive system shows the low activity of some enzymes in the first days after hatching, registering significant increases on 6 dah and the maximum peaks of activities around at 17 dah. Therefore, we recommend replacing live food with dry feed and only providing dry feed after day 17 dah.
- |||||||||| chymotrypsin / Generic mfg.
Journal: EGCG inhibits pressure overload-induced cardiac hypertrophy via the PSMB5/Nmnat2/SIRT6-dependent signaling pathways. (Pubmed Central) - Aug 20, 2021
Therefore, we recommend replacing live food with dry feed and only providing dry feed after day 17 dah. These findings serve as the first evidence that the effect of EGCG against cardiac hypertrophy may be, at least partially, attributed to the modulation of the PSMB5/Nmnat2-dependent signaling pathway, suggesting the therapeutic potential of EGCG in the prevention and treatment of cardiac hypertrophy.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Perchlorate salts confer psychrophilic characteristics in α-chymotrypsin. (Pubmed Central) - Aug 18, 2021
We have also shown that α-chymotrypsin activity appears to exhibit an altered pressure response at low temperatures while also maintaining stability at high pressures and sub-zero temperatures. As the effects of perchlorate salts on the thermodynamics of α-chymotrypsin's activity closely resemble those of psychrophilic adaptations, it suggests that the presence of chaotropic molecules may be beneficial to life operating in low temperature environments.
- |||||||||| chymotrypsin / Generic mfg.
Journal, PARP Biomarker: Proteasomal dysfunction and ER stress triggers 2'-hydroxy-retrochalcone induced paraptosis in cancer cells. (Pubmed Central) - Aug 13, 2021
Docking studies revealed that HRC could bind to the Thr1 residue on the active site of the chymotrypsin-like subunit of the proteasome...Pretreatment with thiol antioxidants and cycloheximide were able to inhibit this programmed cell death. Thus our data suggest that HRC can effectively kill cancer cells via paraptosis, an alternative death pathway and can be a potential lead molecule for anti-cancer therapy.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Discovery of selective fragment-sized immunoproteasome inhibitors. (Pubmed Central) - Aug 13, 2021
The screening of an in-house library of structurally diverse fragments resulted in the identification of benzo[d]oxazole-2(3H)-thiones, benzo[d]thiazole-2(3H)-thiones, benzo[d]imidazole-2(3H)-thiones, and 1-methylbenzo[d]imidazole-2(3H)-thiones (with a general term benzoXazole-2(3H)-thiones) as inhibitors of the chymotrypsin-like (β5i) subunit of the immunoproteasome...Thorough characterization of these compounds suggested that they inhibit the immunoproteasome by forming a disulfide bond with the Cys48 available specifically in the β5i active site. To obtain fragments with biologically more tractable covalent interactions, we performed a warhead scan, which yielded benzoXazole-2-carbonitriles as promising starting points for the development of selective immunoproteasome inhibitors with non-peptidic scaffolds.
- |||||||||| remdesivir / Generic mfg., lenvatinib / Generic mfg.
Preclinical, Journal: Combined computational and cellular screening identifies synergistic inhibition of SARS-CoV-2 by lenvatinib and remdesivir. (Pubmed Central) - Aug 13, 2021
Here, we used high-throughput docking to screen 6000 compounds within the DrugBank library for their potential to bind and inhibit the SARS-CoV-2 3 CL main protease, a chymotrypsin-like enzyme that is essential for viral replication...Lenvatinib is a broadly-acting host receptor tyrosine kinase (RTK) inhibitor, but the synergistic effect with remdesivir was not observed with other approved RTK inhibitors (such as pazopanib or sunitinib), suggesting that the mechanism-of-action is independent of host RTKs...Our work shows that combining computational and cellular screening is a means to identify existing drugs with repurposing potential as antiviral compounds. Future studies could be aimed at understanding and optimizing the lenvatinib/remdesivir synergistic mechanism as a therapeutic option.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Daily rhythms of intestinal cholecystokinin and pancreatic proteases activity in Senegalese sole juveniles with diurnal and nocturnal feeding. (Pubmed Central) - Aug 12, 2021
The influence of diurnal and nocturnal feeding on daily rhythms of gut levels of cholecystokinin (CCK) and the activity of two key pancreatic proteases, trypsin and chymotrypsin, were examined in juveniles of Senegalese sole (Solea senegalensis), a species with nocturnal habits...The daily pattern of the gut CCK content in our study is in agreement with the anorexigenic function of this hormone. Our results support the existence of a negative feedback regulatory loop between CCK and pancreatic proteolytic enzymes in Senegalese sole juveniles.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Proteases, Protease Inhibitors and Radiation Carcinogenesis. (Pubmed Central) - Jul 31, 2021
2) Within the category of APIs, those that inhibited the activity of chymotrypsin were effective at far lower molar concentrations than other APIs...6) Several human trials were performed using BBIC and they indicated many potentially beneficial health effects produced by BBIC administration to people in various forms (e.g., tablets). 7) It is hypothesized that BBI takes the place of α-1-antichymotrypsin, an important regulatory compound in the human body, and helps to maintain homeostasis.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Bromo-spiroisoxazoline Alkaloids, Including an Isoserine Peptide, from the Caribbean Marine Sponge Aplysina lacunosa. (Pubmed Central) - Jul 31, 2021
Three new bromotyrosine spiroisoxazoline alkaloids, lacunosins A and B (1 and 2) and desaminopurealin (3), were isolated from a MeOH extract of the marine sponge Aplysina lacunosa that showed modest α-chymotrypsin inhibitory activity...Allylic O-naphthoylation of the SIO subunit enhances the ECD spectrum of SIOs and improves discrimination of enantiomorphs. A unifying hypothesis is proposed that links the biosynthesis of several of the new compounds with previously reported analogues.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Glass-like protein condensate for the long-term storage of proteins. (Pubmed Central) - Jul 23, 2021
Various protein types, including immunoglobulin G, gamma globulin, albumin, and chymotrypsin, formed a glassy state during ultracentrifugation and natural drying, while proteins that tend to crystalize, such as hen egg-white lysozyme, did not...The GLPCs preserved their native structures even after 1 year of incubation at ambient temperature. These results provide a framework for the development of protein preservation methods at ambient temperature other than lyophilization.
- |||||||||| chymotrypsin / Generic mfg.
Journal: A Deadly Cargo: Gene Repertoire of Cytotoxic Effector Proteins in the Camelidae. (Pubmed Central) - Jul 22, 2021
High protein sequence similarities with other camelid and ungulate species were observed for GZMK and GZMM. The protein variability in dromedaries and Bactrian camels was rather low, except for GNLY and chymotrypsin-like granzymes (GZMB, GZMH).
- |||||||||| chymotrypsin / Generic mfg.
Journal: Contribution of cysteine and serine proteases to proteolytic digestion in an allergy-eliciting house dust mite. (Pubmed Central) - Jul 21, 2021
Further incubation of these extracts with exogenous Der p 1, but not with other commercial cysteine proteases, restored trypsin (Der p 3) and chymotrypsin (Der p 6) activities, indicating that Der p 1 is responsible for their activation in vivo. Finally, the role of serine proteases on the mités digestive physiology is discussed based on their remarkable activity in fecal extracts and the autocoprophagic behavior reported in mites in this study.
- |||||||||| chymotrypsin / Generic mfg.
[VIRTUAL] CHYMOTRYPSIN IN THE GUT: MORE THAN JUST A FOOD DIGESTION ENZYME (Hall 2) - Jul 20, 2021 - Abstract #UEGW2021UEGW_3307;
Our results highlight the ability of chymotrypsin to induce signalling on intestinal epithelial cells via PAR2 and modifies the expression of genes involved in the promotion of intestinal barrier function. These results suggest that chymotrypsin could have protective functions in the gut.
- |||||||||| chymotrypsin / Generic mfg.
Review, Journal: Proteolytic Enzyme Therapy in Complementary Oncology: A Systematic Review. (Pubmed Central) - Jul 15, 2021
These results suggest that chymotrypsin could have protective functions in the gut. On the basis of existing evidence, there is no clear therapeutic benefit of enzymes neither as supportive therapy nor as part of antineoplastic therapy.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Antioxidant and enzymes inhibitory properties of Amaranth leaf protein hydrolyzates and ultrafiltration peptide fractions. (Pubmed Central) - Jul 10, 2021
Amaranth leaf protein isolate (ALI) was hydrolyzed using four different proteases (alcalase, trypsin, pepsin, and chymotrypsin) followed by fractionation of the pepsin hydrolyzate (PH) into different sizes using ultrafiltration membrane...The results of the analyses showed that the hydrolyzates and the fractions showed good antioxidant and enzyme inhibitory activities such as the inhibition of ACE, α-amylase, and glucosidase enzymes. The results suggest that the enzymatic hydrolyzates and peptide fractions could be used as ingredients in the nutraceutical and functional food industries to scavenge free radicals and inhibit angiotensin-converting enzyme activity.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Modulatory effect of ursolic acid on neurodegenerative activities in oxidative brain injury: An ex vivo study. (Pubmed Central) - Jul 10, 2021
Induction of oxidative injury in isolated rat brains with 0.1 mM FeSO led to depleted levels of glutathione, superoxide dismutase, catalase, and ENTPDase activities, with concomitant exacerbation of malondialdehyde and nitric oxide levels, α-chymotrypsin, ATPase, and acetylcholinesterase activities...The present study describes the possible therapeutic mechanism of ursolic acid in the amelioration of complications linked to neurodegeneration in oxidative-mediated brain injury. These findings thus give insights into the use of natural products of plant origin in treating and managing neurodegenerative diseases, which may have little or no side effects.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Powerful Chemiluminescence Probe for Rapid Detection of Prostate Specific Antigen Proteolytic Activity: Forensic Identification of Human Semen. (Pubmed Central) - Jul 9, 2021
The prostate specific antigen (PSA), a serine protease with chymotrypsin-like activity, is predominantly expressed in the prostate and is considered as the most common marker in use to identify and follow the progress of prostate cancer...The advantageous sensitivity and simplicity of a chemiluminescence assay to detect seminal fluid was effectively demonstrated by on-site measurements using a small portable luminometer. It is expected that the new chemiluminescence probe would be broadly useful for numerous applications in which PSA detection or imaging is required.
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