- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Clinical, Journal: Global analysis of protein stability by temperature and chemical denaturation. (Pubmed Central) - Feb 5, 2021
Here we have determined the stability of acyl-coenzyme A binding protein at pH 5.3 and chymotrypsin inhibitor 2 at pH 3 and pH 6.25 by combined temperature and denaturant unfolding...For assessment of stability of protein purified in small scale e.g. in micro plate format, our method will be highly applicable. The routine for fitting the experimental data is made available as a python notebook.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Effect of mild α-chymotrypsin treatment of highly viscous semen samples on fertilization rates. (Pubmed Central) - Feb 4, 2021
There was no significant difference in the fertilization rates of α-chymotrypsin treated semen samples compared to the control group; pregnancy rates were unaffected. The use of mild α-chymotrypsin treatment of semen samples in case of hyperviscosity does not appear to impact negatively on the fertilization rates after ART and could be regarded as an additional method to induce liquefaction of highly viscous semen samples in IVF.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Review, Journal: Potential compounds from several Indonesian plants to prevent SARS-CoV-2 infection: A mini-review of SARS-CoV-2 therapeutic targets. (Pubmed Central) - Feb 4, 2021
This mini-review briefly reports the number of potential plants widely distributed in Indonesia for further research and development as anti-SARS-CoV-2 agents and the critical targets for SARS-CoV-2 therapy, such as angiotensin-converting enzyme 2 (ACE-2) receptor, spike protein, 3-chymotrypsin-like protease (3CL), papain-like protease (PL), RNA-dependent RNA polymerase (RdRp), helicase, and serine protease...However, since SARS-CoV-2 is a new disease, it has no history of plant-based treatment anywhere in the world. This mini-review describes natural products from several Indonesian plants that contain compounds that could potentially prevent or reduce SARS-CoV-2 infection, act as potential targeted therapy, and provide new therapeutic strategies to develop SARS-CoV-2 countermeasures.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Review, Journal: A Review on Plant Bioactive Compounds and Their Modes of Action Against Coronavirus Infection. (Pubmed Central) - Feb 2, 2021
This includes inhibition of viral attachment and penetration, inhibition of viral RNA and protein synthesis, inhibition of viral key proteins such as 3-chymotrypsin-like cysteine protease (3CL) and papain-like protease 2 (PL), as well as other mechanisms including inhibition of the viral release and enhanced host immunity. We hope this compilation will help researchers and clinicians to identify the source of appropriate anti-viral drugs from plants in combating COVID-19 and, ultimately, save millions of affected human lives.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Review, Journal: Biflavonoid as potential 3-chymotrypsin-like protease (3CLpro) inhibitor of SARS-Coronavirus. (Pubmed Central) - Feb 2, 2021
Lastly, the pharmacophores of biflavonoid have been identified as a protease inhibitor, was also discussed. This review hopefully will help researchers to obtain packed information about biflavonoid which could lead to the study in designing and discovering a novel SARS-Coronavirus-2 drug by targetting the 3CLpro enzyme.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents. (Pubmed Central) - Jan 29, 2021
The 100 ns molecular dynamics simulation studies showed that ivermectin may require homodimeric form of 3CLpro enzyme for its inhibitory activity. In summary, these molecules could be useful to develop highly specific therapeutically viable drugs to inhibit the SARS-CoV-2 replication either alone or in combination with drugs specific for other SARS-CoV-2 viral targets.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Clinical, Journal: Probing CAS database as prospective antiviral agents against SARS-CoV-2 main protease. (Pubmed Central) - Jan 28, 2021
Virus main protease or chymotrypsin-like protease plays a pivotal role in virus replication and transcription; thus, it is considered as an attractive drug target to combat the COVID-19...Insight binding modes demonstrated that the selected hits stabilized inside the binding pocket of the target protein and exhibit complementarity with the active site residues. Our study provides compounds for further in vitro and in vivo studies against SARS-CoV-2.
- |||||||||| 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) - Jan 26, 2021
P3, N=405, Active, not recruiting,
Largely, our results supported that this novel compound 16 binds with domains I and II, and the domain II-III linker of the 3CL protein, suggesting its suitability as a strong candidate for therapeutic discovery against COVID-19. Trial completion date: Dec 2019 --> Jun 2022 | Trial primary completion date: Dec 2019 --> Dec 2021
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Improving Enzyme Catalytic Efficiency by Co-operative Vibrational Strong Coupling of Water. (Pubmed Central) - Jan 23, 2021
Here, we report enhancement of catalytic efficiency of an enzymatic reaction by co-operative vibrational strong coupling (VSC) of water and the enzyme α-chymotrypsin...This is specifically achieved by controlling the rate-determining proton-transfer process through a co-operative mechanism. Here, VSC is also used as a spectroscopic tool to understand the mechanism of the enzymatic reaction, suggesting its potential applications in chemistry.
- |||||||||| oprozomib (ONX 0912) / Amgen
Journal: The active second-generation proteasome inhibitor oprozomib reverts the oxaliplatin-induced neuropathy symptoms. (Pubmed Central) - Jan 23, 2021
This preclinical study reveals the involvement of the proteasome in the oxaliplatin-induced neuropathy and adds useful information to better understand the molecular mechanism underlying this pain condition. Moreover, although further evidence is required, these findings suggest that oprozomib could be a therapeutic option to counteract chemotherapy-induced neuropathy.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Potential Antioxidant Properties of Enzymatic Hydrolysates from Stichopusjaponicus against Hydrogen Peroxide-Induced Oxidative Stress. (Pubmed Central) - Jan 22, 2021
japonicus was hydrolyzed with food-grade enzymes (alcalase, α-chymotrypsin, flavourzyme, kojizyme, neutrase, papain, pepsin, protamex, and trypsin), and the free radical scavenging activities were screened via electron spin resonance (ESR) spectroscopy...Furthermore, α-chy-III remarkably attenuated the cell death, intracellular ROS and lipid peroxidation in HO exposed zebrafish embryos. Altogether, our findings demonstrated that α-chy and its α-chy-III from S. japonicus possess strong antioxidant activities that could be utilized as a bioactive ingredient for functional food industries.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Preclinical, Journal: N-Terminomics for the Identification of in vitro Substrates and Cleavage Site Specificity of the SARS-CoV-2 Main Protease. (Pubmed Central) - Jan 21, 2021
The genome of coronaviruses, including SARS-CoV-2, encodes for two proteases, a papain like (PL ) protease and the so-called main protease (M ), a chymotrypsin-like cysteine protease, also named 3CL or non-structural protein 5 (nsp5)...These data enable to better understand the cleavage site specificity of the viral proteases and will help to identify novel substrates in vivo. All data are available via ProteomeXchange with identifier PXD021406.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Clinical, Journal: Existing antiviral options against SARS-CoV-2 replication in COVID-19 patients. (Pubmed Central) - Jan 21, 2021
Developing the new treatment is usually time consuming, therefore using the repurposing broad-spectrum antiviral drugs could be an effective strategy to respond immediately. In this review, a number of broad-spectrum antivirals with potential efficacy to inhibit the virus replication via targeting the virus spike protein (S protein), RNA-dependent RNA polymerase (RdRp), 3-chymotrypsin-like protease (3CLpro) and papain-like protease (PLpro) that are critical in the pathogenesis and life cycle of coronavirus, have been evaluated as possible treatment options against SARS-CoV-2 in COVID-19 patients.
- |||||||||| Invirase (saquinavir) / Roche
Preclinical, Journal: Repurposing existing drugs: identification of SARS-CoV-2 3C-like protease inhibitors. (Pubmed Central) - Jan 21, 2021
Ethacrynic acid, naproxen, allopurinol, butenafine hydrochloride, raloxifene hydrochloride, tranylcypromine hydrochloride, and saquinavir mesylate have been found to block the proteolytic activity of SARS-CoV-2 3CLpro. The inhibitory activity of these repurposing drugs against SARS-CoV-2 3CLpro highlights their therapeutic potential for treating COVID-19 and other Betacoronavirus infections.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Safety evaluation of a food enzyme containing trypsin, chymotrypsin, elastase and carboxypeptidase from porcine pancreas. (Pubmed Central) - Jan 20, 2021
The Panel considered that a risk of allergic sensitisation to these peptides after consumption of products prepared by hydrolysis of milk, cannot be excluded in infants, but the likelihood to occur is considered to be low. Based on the origin of the food enzyme from edible parts of animals, the data provided by the applicant, supported by the evaluation of clinical studies with pharmaceutical preparations based on pancreatic enzymes, the Panel concluded that the porcine pancreatic enzymes do not give rise to safety concern under the intended conditions of use.
- |||||||||| Olysio (simeprevir) / J&J, Medivir, Xofluza (baloxavir marboxil) / Roche, Shionogi
Journal, Combination therapy: Combination and tricombination therapy to destabilize the structural integrity of COVID-19 by some bioactive compounds with antiviral drugs: insights from molecular docking study. (Pubmed Central) - Jan 14, 2021
In this study, we aim to find antagonists that may inhibit the activity of the three major viral targets: SARS-CoV-2 3-chymotrypsin-like protease (6LU7), SARS-CoV-2 spike protein (6VYB), and a host target human angiotensin-converting enzyme 2 (ACE2) receptor (1R42), which is the entry point for the viral encounter, were studied with the prospects of identifying significant drug candidate(s) against COVID-19 infection...Hence, we studied the combination and tricombination therapy between bioactive compounds which have the best binding affinity and some antiviral drugs like chloroquine, hydroxychloroquine, azithromycin, simeprevir, baloxavir, lopinavir, and favipiravir to show the effect of combination and tricombination therapy to disrupt the stability of the three major viral targets that are mentioned previously...All results confirmed that caulerpin can be utilized as a combination and tricombination therapy along with the studied antiviral drugs for disrupting the stability of the three major viral receptors (6LU7, 6VYB, and 1R42). The online version contains supplementary material available at 10.1007/s11224-020-01723-5.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Safety evaluation of a food enzyme containing trypsin and chymotrypsin from porcine pancreas. (Pubmed Central) - Jan 14, 2021
The Panel considered that a risk of allergic sensitisation to this food enzyme after consumption of products prepared by hydrolysis of milk cannot be excluded in infants, but considers the likelihood to be low. Based on the origin of the food enzyme from edible parts of animals, the data provided by the applicant, supported by the evaluation of clinical studies with pharmaceutical preparations based on pancreatic enzymes, the Panel concluded that the porcine pancreatic enzymes do not give rise to safety concern under the intended conditions of use.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: The effect of fruit on the extracellular enzyme profiles of fungi. (Pubmed Central) - Jan 12, 2021
Individual fruits can increase or decrease the activity of the enzymes. Fungi present in fruit have pathogenic properties and can be possible risk factors for fungal infections.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: The polyphenol quercetin protects from glucotoxicity depending on the aggresome in Caenorhabditis elegans. (Pubmed Central) - Jan 8, 2021
These findings also suggest that inactivation of serpin B1 by oxidation may have a physiological role to play during inflammation. The study provides evidence that quercetin protects C. elegans from glucotoxicity through the activation of the aggresome, thereby, quercetin prevents the aggregation and functional loss of proteins, which is typically caused by enhanced glucose concentrations.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Inhibition of α-chymotrypsin by pristine single-wall carbon nanotubes: Clogging up the active site. (Pubmed Central) - Jan 6, 2021
An important role in the bonding appears also for purely hydrophobic residues and with residues able to establish surfactant-like interactions. The secondary structure of α-CT and the catalytic triad structure are not perturbed by the complex formation, on the contrary the volume of the substrate binding pocket is strongly reduced by SWCNT binding because SWCNT occupies the α-CT substrate binding site, clogging the active site.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Journal: Ultra-rapid glutathionylation of chymotrypsinogen in its molten globule-like conformation: A comparison to archaeal proteins. (Pubmed Central) - Jan 6, 2021
The extraordinary reactivity toward GSSG is absent in two proteins of the thermophilic archaeon Sulfolobus solfataricus, an organism lacking glutathione: the Protein Disulphide Oxidoreductase (SsPDO) and the Bacterioferritin Comigratory Protein 1 (Bcp1) that displays Cys residues with an even lower pK value (7.5 ± 0.1) compared to chymotrypsinogen. This study, which also uses single mutants in Cys residues for Bcp1, proposes that this hyper-reactivity of a single cysteine, similar to that found in serum albumin, lysozyme, ribonuclease, may have relevance to drive the "incipit" of the oxidative folding of proteins from organisms where the glutathione/oxidized glutathione (GSH/GSSG) system is present.
- |||||||||| Journal: Flavonols as potential antiviral drugs targeting SARS-CoV-2 proteases (3CL and PL), spike protein, RNA-dependent RNA polymerase (RdRp) and angiotensin-converting enzyme II receptor (ACE2). (Pubmed Central) - Jan 6, 2021
In this context, the present study reviews the efficacy of many dietary flavonols as potential antiviral drugs targeting the SARS-CoV-2 enzymes and proteins including Chymotrypsin-Like Protease (3CL), Papain Like protease (PL), Spike protein (S protein) and RNA-dependent RNA polymerase (RdRp), and also their ability to interact with the angiotensin-converting enzyme II (ACE2) receptor...On the other hand, the immunomodulatory, the anti-inflammatory and the antiviral effects of secondary metabolites from this class of flavonoids were reported. Also, their bioavailability limitations and toxicity were predicted.
- |||||||||| Chymoral Forte-DS (chymotrypsin) / Generic mfg.
Review, Journal: Naringenin, a flavanone with antiviral and anti-inflammatory effects: A promising treatment strategy against COVID-19. (Pubmed Central) - Jan 5, 2021
The evidence reviewed here indicates that naringenin might exert therapeutic effects against COVID-19 through the inhibition of COVID-19 main protease, 3-chymotrypsin-like protease (3CLpro), and reduction of angiotensin converting enzyme receptors activity...The antiviral activity of the flavanone naringenin against some viruses has also been reported. On the whole, the favorable effects of naringenin lead to a conclusion that naringenin may be a promising treatment strategy against COVID-19.
- |||||||||| chymotrypsin / Generic mfg.
Journal: Protective effect of overexpression of PrxII on H2O2-induced cardiomyocyte injury. (Pubmed Central) - Sep 25, 2020
Among the complexes assayed in cultured cells, complex Ru3 was able to diminish the proteasomal chymotrypsin-like activity to a greater extent. Overexpression of PrxII can activate the AMPK/Sirt1 pathway, thereby inhibiting H2O2-induced oxidative stress and slowing apoptosis.
- |||||||||| CM-AT / Curemark
Trial primary completion date: An Open Label Study of CM-AT for the Treatment of Children With Autism (clinicaltrials.gov) - Jul 26, 2019
P3, N=405, Active, not recruiting,
Overexpression of PrxII can activate the AMPK/Sirt1 pathway, thereby inhibiting H2O2-induced oxidative stress and slowing apoptosis. Trial primary completion date: Jun 2019 --> Dec 2019
- |||||||||| 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) - Dec 14, 2018
P3, N=405, Active, not recruiting,
Trial primary completion date: Jun 2019 --> Dec 2019 Trial completion date: Dec 2018 --> Dec 2019 | Trial primary completion date: Oct 2018 --> Jun 2019
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