- |||||||||| chymotrypsin / Generic mfg.
Journal: RNA-seq analysis of the differential response to low-temperature stress in two morphs of mud crabs (Scylla paramamosain). (Pubmed Central) - Aug 22, 2022
The gene expressions of acid phosphatase (ACP), chymotrypsin (CHY), serine carboxypeptidase (SCP), and trypsin (TRY) under low-temperature stress were detected...The ACP, CHY, SCP, and TRY gene expression of the Sp1 morph was lower than that of the Sp2 morph; however, the ACP gene expression of the Sp1 morph was higher than that of the Sp2 morph at several time points. In conclusion, adaptability differences between the morphs to low-temperature stress were confirmed, which will enable the selection of cold-tolerant, high-quality varieties of mud crabs for breeding.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Structure of silk I (Bombyx mori silk fibroin before spinning) in the dry and hydrated states studied using C solid-state NMR spectroscopy. (Pubmed Central) - Aug 22, 2022
Three kinds of C INEPT, CP/MAS and DD/MAS NMR spectra were observed for SF, [3-C] Ser- and [3-C] Tyr-SF, the crystalline fraction obtained by chymotrypsin treatment of SF and their model peptide with silk I structures in the dry and hydrated states. Especially, the presence of the sequences containing Tyr, (((GX)GY) where X = A or V) with random coil conformations adjacent to (GAGAGS) is an essence to get water-soluble SF and the formation of silk I* structure of (GAGAGS).
- |||||||||| bortezomib / Generic mfg., carfilzomib / Generic mfg.
Journal: Bortezomib- and carfilzomib-resistant myeloma cells show increased activity of all three arms of the unfolded protein response. (Pubmed Central) - Aug 16, 2022
Both baseline and drug-induced activity of the unfolded protein response were higher in resistant cells than in MM1S WT cells and included all three arms of this pathway: IRE1α/XBP1s, ATF6 and EIF2α/ATF4 (downstream effectors of PERK). In conclusion, contrary to some previous reports, resistant MM1S cells show upregulation of unfolded protein response activity, reflecting the heterogeneity of multiple myeloma and prompting further studies on the role of this pathway in resistance to proteasome inhibitors.
- |||||||||| chymotrypsin / Generic mfg.
A comparative analysis of CPA1, bcl10 and chymotrypsin for the distinction of pancreatic acinar cell carcinomas (Osaka/Samarkand) - Aug 16, 2022 - Abstract #ECP2022ECP_820;
CPA1 and chymotrypsin are both highly specific and sensitive for ACC while bcl10 is sensitive but has markedly lower specificity. Because all "false positive" cases identified by CPA1 were CRCs that only showed a positive staining in goblet cells and an identical staining pattern was observed in all these cases for chymotrypsin and bcl10, a pancreatic origin of the mucus in these goblet cells is concluded.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Native metabolomics identifies the rivulariapeptolide family of protease inhibitors. (Pubmed Central) - Aug 11, 2022
Guided by the native metabolomics results, we select and purify five of these compounds for full structure elucidation via tandem mass spectrometry, chemical derivatization, and nuclear magnetic resonance spectroscopy as well as evaluation of their biological activities. These results identify rivulariapeptolides as a family of serine protease inhibitors with nanomolar potency, highlighting native metabolomics as a promising approach for drug discovery, chemical ecology, and chemical biology studies.
- |||||||||| chymotrypsin / Generic mfg.
Bifunctional molecules as prodrugs for the immunoproteasome (Great Lakes F (Marriott Marquis Chicago)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_362;
Once the hybrid molecule binds to the chymotrypsin-like active site of the iCP, the biologically-relevant molecule will be released from the peptide...The sequence of the peptide can also be modified depending on the desire to also inhibit excessive iCP function. Further medicinal chemistry optimization and biochemical characterization has further allowed us to better understand what functional groups are favored by the iCP’s substrate channel for more efficient cleavage and therefore, activation of our prodrug-like scaffold.
- |||||||||| CM-AT / Curemark
Trial completion date, Trial primary completion date: An Open Label Study of CM-AT for the Treatment of Children With Autism (clinicaltrials.gov) - Aug 3, 2022
P3, N=405, Active, not recruiting,
To the best of our knowledge, this is the first report on the structure of trypsin in-complex with LBTI. Trial completion date: Jun 2022 --> Jun 2023 | Trial primary completion date: Dec 2021 --> Jan 2023
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Review: Mast Cell and Basophil Granule Proteases - In Vivo Targets and Function. (Pubmed Central) - Jul 30, 2022
The absolute majority of these proteases belong to the large family of chymotrypsin related serine proteases...The chymase also appear to have a protective role against ectoparasites such as ticks, mosquitos and leeches by the cleavage of their anticoagulant proteins. We here review the data that has accumulated concerning the potential in vivo functions of these enzymes and we discuss how this information sheds new light on the role of MCs and basophils in health and disease.
- |||||||||| chymotrypsin / Generic mfg.
Journal: A novel 8-hydroxyquinoline derivative induces breast cancer cell death through paraptosis and apoptosis. (Pubmed Central) - Jul 28, 2022
Molecular docking analysis revealed a favorable binding mode of HQ-11 in the active site of the chymotrypsin-like β5 subunit of the proteasome, indicative of proteasome dysfunction under HQ-11 treatment, which might result in further aggravated ER stress...In addition, exposure to HQ-11 also caused apoptosis in breast cancer cells partially through activation of ERK pathway. All these results conclusively indicate that HQ-11 triggers two distinct cell death modes via inhibition of proteasome and activation of ERK pathway in breast cancer cells, providing a promising candidate in future anti-breast cancer therapy.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Structure of Senecavirus A 3C Protease Revealed the Cleavage Pattern of 3C Protease in Picornaviruses. (Pubmed Central) - Jul 27, 2022
The structure revealed that SVA 3C adopted a typical chymotrypsin-like fold with the S1 subsite as the most conservative site among picornavirus 3C...Here, we showed the 1.9 Å crystal structure of SVA 3C. The structure revealed similarities and differences in the substrate-binding groove among picornaviruses, providing new insights into the development of inhibitors and VLP.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Circular Dichroism Spectra of α-Chymotrypsin-SDS Solutions Depend on the Procedure of Their Preparation. (Pubmed Central) - Jul 20, 2022
For quantitative analysis of far-UV CD spectra in terms of populations of protein secondary structure elements, we used four well-established software packages. All programs consistently indicate that the observed differences in the far-UV CD spectra can be explained by the differences in the increase in the population of helical forms in chymotrypsin under the influence of SDS.
- |||||||||| selisistat (SEN-196) / AOP Orphan Pharma
Journal: Microglial polarization differentially affects neuronal vulnerability to the β-amyloid protein: modulation by melatonin. (Pubmed Central) - Jul 16, 2022
These effects were prevented by CM from anti-inflammatory microglia (Aβ42 for 6 h), or from MELco and MELpost microglia, but the reduction of neuritic length was not rescued when the SIRT1 inhibitor EX527 was added. In conclusion, our data add to the concept that melatonin shows a promising anti-inflammatory action on microglia that is retained even after pro-inflammatory activation, involves modulation of proteasome function and translates into neuroprotective microglial effects.
- |||||||||| chymotrypsin / Generic mfg.
Journal: TNKPVI, a Putative Bioaccessible Pharmacophore of Anti-Inflammatory Potato Patatin-Derived Decapeptide DIKTNKPVIF. (Pubmed Central) - Jul 1, 2022
The peptides lacked the cleavage sites of chymotrypsin...This highlights the important role of the C-terminal phenylalanine residue of the parent peptide in the bioactivity. Furthermore, given its activity and the absence of cleavage sites of major digestive proteases, TNKPVI could be the biostable and bioaccessible pharmacophore of potato patatin-derived anti-inflammatory decapeptide DIKTNKPVIF.
- |||||||||| chymotrypsin / Generic mfg.
Biomarker, Journal: Socioeconomic disparity in cardiovascular disease: Possible biological pathways based on a proteomic approach. (Pubmed Central) - Jun 29, 2022
Furthermore, given its activity and the absence of cleavage sites of major digestive proteases, TNKPVI could be the biostable and bioaccessible pharmacophore of potato patatin-derived anti-inflammatory decapeptide DIKTNKPVIF. SEP was associated with multiple biomarkers, indicating pathways involving inflammation (IL-6, RARRES2), platelet-activation (vWF, IL-6), blood pressure (REN, LEP) and Mitogen-activated protein kinase cascade (GDF-15, EGFR) may contribute to the socioeconomic differences in CVD.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Interactions between unfolding/disassembling behaviors, proteolytic subfragments and reversible aggregation of oxidized skeletal myosin isoforms at different salt contents. (Pubmed Central) - Jun 29, 2022
Thus, this study investigated the impact of different salt content (0%, 1%, 2%, 3%, 4%, 5% NaCl) and oxidation in vitro (10 mM HO/ascorbate-based hydroxyl radical (OH)-generating system) on the oxidative stability, solubility/dispersion capacity, chymotrypsin digestibility, aggregation site and the microrheological properties of isolated porcine myosin...The results of micro-rheology proved that oxidized myosin formed a tighter heat-set network following rehydration at high ion strength (≥4% salt), suggesting an increased inter-droplet resistance and macroscopic viscosity. This work is expected to give some useful insights into improved texture and functionality of engineered muscle foods.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Acetylcholinesterase and butyrylcholinesterase inhibitory activities of antioxidant peptides obtained from enzymatic pea protein hydrolysates and their ultrafiltration peptide fractions. (Pubmed Central) - Jun 28, 2022
This study optimized the enzymatic hydrolysis of yellow field pea proteins using alcalase (ACH), chymotrypsin (CHH), flavourzyme (FZH), pancreatin (PCH), pepsin (PEH), and trypsin (TPH) to obtain hydrolysates and ultrafiltered fractions (<1, 1-3, 3-5 and 5-10 kDa) that possess antioxidant plus acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities...Peptides derived from food proteins consist of ester bonds with structural similarity to ACh and theoretically possess the ability to interact with AChE and BuChE. Results from the present study imply that pea protein-derived peptides are potential candidates for use as inhibitors of AChE and BuChE activities, with application in the prevention and management of AD.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Semi-Quantitative Evaluation of Asymmetricity of Dialysis Membrane Using Forward and Backward Ultrafiltration. (Pubmed Central) - Jun 24, 2022
Forward and backward ultrafiltration experiments were performed separately with aqueous vitamin B (MW 1355), α-chymotrypsin (MW 25,000), albumin (MW 66,000) and dextran solutions, introducing the test solution inside or outside the hollow fiber (HF), respectively...This fact was verified in continuous basis by employing dextran solution before and after being fouled with albumin. These findings may contribute to the development of a novel membrane for improved success of dialysis therapy.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Chymotrypsin attenuates adjuvant-induced arthritis by downregulating TLR4, NF-κB, MMP-1, TNF-α, IL-1β and IL-6 expression in Sprague- Dawley rats. (Pubmed Central) - Jun 24, 2022
Likewise, the rats treated with chymotrypsin and piroxicam had a substantial decline in the mRNA expression of TLR4, NF-κB, TNF-α, IL-1β and IL-6 in synovial tissue. Chymotrypsin alleviates the joint damage of AIA rats, probably by reducing the expression of MMP-1, TNF-α, IL-1β and IL-6 through TLR4/NF-κB signaling pathway.
- |||||||||| chymotrypsin / Generic mfg.
Journal: KPI5 Is Involved in the Regulation of the Expression of Antibacterial Peptide Genes and Hemolymph Melanization in the Silkworm, Bombyx mori. (Pubmed Central) - Jun 14, 2022
Inhibitory activity and stability analyses indicated that recombinant KPI5 protein significantly inhibited the activity of chymotrypsin and was highly tolerant to temperature and pH...These findings suggested that KPI5 plays a dual regulatory role in innate immunity by promoting the expression of antimicrobial peptides in the fat body and inhibiting hemolymph melanization. Our study furthers the understanding of the function of insect KPIs and provides new insights into the regulatory mechanism of insect immune homeostasis.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Sustained endocrine and exocrine function in the pancreas of the Pacific spiny dogfish post-feeding. (Pubmed Central) - Jun 4, 2022
Previous studies have identified that the exocrine pancreas produces (co)lipases, chymotrypsin, carboxypeptidase, and low levels of chitinases; however, investigations into other digestive enzymes are limited...Yet, a significant and transient decrease in glut4 and sodium glucose-linked transporter mRNA abundance was found at 48 h post-feeding. We propose that the constant enzyme activity across this relatively large organ, in combination with a relatively slow rate of digestion leads to an evenly distributed, sustained release of digestive enzymes regardless of digestive state.
- |||||||||| chymotrypsin / Generic mfg.
Retrospective data, Journal: Risk of chronic pancreatitis in carriers of loss-of-function CTRC variants: A meta-analysis. (Pubmed Central) - May 29, 2022
The digestive protease chymotrypsin C (CTRC) protects the pancreas against pancreatitis by degrading potentially harmful trypsinogen...Taken together, the results indicate that heterozygous loss-of-function CTRC variants increase the risk for CP approximately 3-7-fold. This meta-analysis confirms the clinical significance of CTRC variants and provides further justification for the genetic screening of CP patients.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Treponema denticola Promotes OSCC Development via the TGF-β Signaling Pathway. (Pubmed Central) - May 25, 2022
Previous studies have mainly focused on T. denticola surface proteins-for example, chymotrypsin-like proteinase, which was detected in the majority of orodigestive tumor tissues.T...Regarding the mechanism, T. denticola could promote the development of OSCC by activating the TGF-β pathway. In conclusion, T. denticola could promote OSCC cell proliferation directly, and the mechanism was associated with intracellular TGF-β pathway activation.
- |||||||||| rivaroxaban / Generic mfg.
Journal: Unexpected Dynamic Binding May Rescue the Binding Affinity of Rivaroxaban in a Mutant of Coagulation Factor X. (Pubmed Central) - May 24, 2022
This case again emphasizes that binding of ligands may not only be a dynamic process but also a dynamic state, which is often neglected in drug design and screening based on static X-ray structures. In addition, the computational results somewhat confirmed our hypothesis on the activated Tyr319Cys FX (Y99C FXa) with an impaired procoagulant function to bind inhibitors of FXa and to be developed into a potential reversal agent for novel oral anticoagulants (NOAC).
- |||||||||| chymotrypsin / Generic mfg.
Journal: The role of the transmembrane domain of silicanin-1: Reconstitution of the full-length protein in artificial membranes. (Pubmed Central) - May 18, 2022
By using a chymotrypsin digest, the orientation of Sin1 in unilamellar vesicles was analyzed indicating a positioning of the large N-terminal domain to the outside of the vesicles...Successful Sin1 reconstitution into these planar membranes was shown by means of immunostaining with purified primary anti-Sin1 and secondary fluorescent antibodies. The established planar model membrane system, amenable for surface sensitive and microscopy techniques, will pave the way to investigate SDV-membrane interactions with other SDV associated biomolecules and its role in silica biogenesis.
- |||||||||| methoxyamine (TRC102) / Tracon Pharma
Journal: Application of a Novel Pancreas Perfusion Technique to Characterize Exocrine Pancreas Metabolism. (Pubmed Central) - May 14, 2022
The exocrine tissue produces digestive enzymes such as chymotrypsin and is connected through the ductal system...The extracts were derivatized using methoxyamine and MTBSTFA before gas chromatography-mass spectrometry (GC-MS) analysis...This research will use the T1D mouse model NOD. Rag1-/-.AI4α/β and compare the results to the NOD.Rag1-/- control mouse model to examine how exocrine pancreas central carbon metabolism is altered in T1D models in a more physiologically relevant manner than previously possible.
- |||||||||| chymotrypsin / Generic mfg.
Preclinical, Journal: Utility of the DHFR-based destabilizing domain across mouse models of retinal degeneration and aging. (Pubmed Central) - May 7, 2022
Moreover, trimethoprim (TMP) administration stabilized the DHFR DD in all mouse models. Thus, the DHFR DD-based approach allows for control of protein abundance in a variety of mouse models, laying the foundation to use this strategy for the conditional control of gene therapies to potentially treat multiple eye diseases.
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