PubAg

Main content area

You searched for: Subject "enzyme inhibitors" Remove constraint Subject: "enzyme inhibitors"
Start Over

Search

6,669  Search Results

« Previous | 1 - 20 of 6,669 |
Number of results to display per page

Search Results

1. Correction: Suzuki coupling-based synthesis of VATPase inhibitor archazolid natural product derived fragments

Author:
Vincent, Cooper A.; Long, Evan T.; Jones, Holly C.; Young, Jeffrey C.; Spiegel, P. Clint; O’Neil, Gregory W.
Source:
RSC advances 2019 v.9 no.60 pp. 34963
ISSN:
2046-2069
Subject:
enzyme inhibitors
Abstract:
... Correction for ‘Suzuki coupling-based synthesis of VATPase inhibitor archazolid natural product derived fragments’ by Cooper T. Vincent et al., RSC Adv., 2019, 9, 32210–32218. ...
DOI:
10.1039/c9ra90080b

2. A Tumor-Agnostic NTRK (TRK) Inhibitor

Author:
Huang, Franklin W.; Feng, Felix Y.
Source:
Cell 2019 v.177 no.1 pp. 8
ISSN:
0092-8674
Subject:
enzyme inhibitors,   etc   ; genomics; neoplasms;     Show all 3 Subjects
Abstract:
... Larotrectinib is a small-molecule kinase inhibitor that targets NTRK fusions that occur in multiple types of cancer. Its FDA approval represents the first instance of a treatment indication being designated “tumor-agnostic” from the outset, being based on actionable genomic insights. To view this Bench to Bedside, open or download the PDF. ...
DOI:
10.1016/j.cell.2019.02.049

3. Characteristics of a XIP‐resistant xylanase from Neocallimastix sp. GMLF1 and its advantage in barley malt saccharification

Author:
Zhu, Dongdong; Liu, Xinyu; Xie, Xia; Yang, Sen; Lin, Hui; Chen, Hongge
Source:
International journal of food science & technology 2020 v.55 no.5 pp. 2152-2160
ISSN:
0950-5423
Subject:
enzyme inhibitors,   etc   ; Neocallimastix; malting barley; proteins; saccharification; xylanases;     Show all 6 Subjects
Abstract:
... The well‐studied xylanase inhibitor protein (XIP‐I) regularly inhibits fungi‐derived xylanases, yet some fungal xylanases are not inhibited by XIP‐I. Based on the sequence alignment with the known XIP‐I resistant NpXyn11A from Neocallimastix patriciarum, a new annotated xylanase from ruminal fungus Neocallimastix sp. GMLF1 was found, noted as Xyn1B, which shared 77.8% of sequence identity with NpX ...
DOI:
10.1111/ijfs.14341

4. Reductive sp³–sp² Coupling Reactions Enable Late-Stage Modification of Pharmaceuticals

Author:
Mennie, Katrina M.; Vara, Brandon A.; Levi, Samuel M.
Source:
Organic letters 2020 v.22 no.2 pp. 556-559
ISSN:
1523-7052
Subject:
enzyme inhibitors,   etc   ; derivatization; drugs; enzymes; moieties; organic halogen compounds;     Show all 6 Subjects
Abstract:
... Late-stage derivatization of pharmaceutically relevant scaffolds relies on the availability of highly functional-group tolerant reactions. Reactions that increase the sp³ character of molecules enable the pursuit of more selective and well-tolerated pharmaceuticals. Herein, we report the use of sp³–sp² cross-electrophile reductive couplings to modify a generic ATP-competitive kinase inhibitor with ...
DOI:
10.1021/acs.orglett.9b04320

5. Identification of fungal enzymes involving 3-phenoxybenzoic acid degradation by using enzymes inhibitors and inducers

Author:
Zhao, Jiayuan; Chen, Xiaofeng; Jia, Dongying; Yao, Kai
Source:
MethodsX 2020 v.7 pp. 100772
ISSN:
2215-0161
Subject:
enzyme inhibitors,   etc   ; benzoic acids; chemical structure; fungal enzymes;     Show all 4 Subjects
Abstract:
... Pyrethroid residues in food and the environment can be bio-transformed into 3-phenoxybenzoic acid (3-PBA); It is more toxic than the parent compounds, and has been detected in milk, soil, and human urine. In this study, when incubated at 30 °C and 180 rpm for 48 h, mycelial pellets during logarithmic growth phase were obtained and washed 2 times by phosphate buffer. The cell debris solutions and f ...
DOI:
10.1016/j.mex.2019.100772
PubMed:
32140437
PubMed Central:
PMC7046809

6. Contribution of calpain to protein degradation, variation in myowater properties and the water-holding capacity of pork during postmortem ageing

Author:
Qian, Shuyi; Li, Xia; Wang, Hang; Wei, Xiuli; Mehmood, Waris; Zhang, Chunhui; Blecker, Christophe
Source:
Food chemistry 2020 v.324 pp. 126892
ISSN:
0308-8146
Subject:
enzyme inhibitors,   etc   ; calpain; desmin; integrins; muscles; pork; protein degradation; proteolysis; swine; water holding capacity;     Show all 10 Subjects
Abstract:
... To investigate calpain’s effect on protein degradation, myowater properties, and the water-holding capacity (WHC), porcine longissimus muscles were incubated with control buffer, PD₁₅₀,₆₀₆ (calpain-specific inhibitor) and MG-262 (multiple-protease inhibitor) and assigned to an ageing period of 1, 4 or 7 d. Over 7 d of storage, no significant differences (P > 0.05) were observed in desmin or integr ...
DOI:
10.1016/j.foodchem.2020.126892

7. Detection of organophosphorus pesticides with liquid crystals supported on the surface deposited with polyoxometalate-based acetylcholinesterase-responsive supramolecular spheres

Author:
Qi, Lubin; Wu, Wenli; Kang, Qi; Hu, Qiongzheng; Yu, Li
Source:
Food chemistry 2020 v.320 pp. 126683
ISSN:
0308-8146
Subject:
enzyme inhibitors,   etc   ; acetylcholinesterase; aqueous solutions; detection limit; dimethoate; enzymatic hydrolysis; glass; liquid crystals; surfactants;     Show all 9 Subjects
Abstract:
... Here, we demonstrate use of acetylcholinesterase (AChE)-responsive polyoxometalate (POM)/surfactant supramolecular spheres to build a liquid crystal (LC)-based sensing platform for detection of organophosphorus pesticides. The self-assembled spheres are composed of hybrid materials of a POM, sodium dodecatungstophosphate (PW₁₂), and a surfactant, myristoylcholine (Myr). It displays dark appearance ...
DOI:
10.1016/j.foodchem.2020.126683

8. 5-HT2A receptor-mediated PKCδ phosphorylation is critical for serotonergic impairments induced by p-chloroamphetamine in mice

Author:
Phan, Dieu Hien; Shin, Eun-Joo; Sharma, Naveen; Hoang Yen, Tran Phi; Dang, Duy-Khanh; Lee, Yong Sup; Lee, Yu Jeung; Nah, Seung-Yeol; Cheong, Jae Hoon; Jeong, Ji Hoon; Kim, Hyoung-Chun
Source:
Food and chemical toxicology 2020 v.141 pp. 111395
ISSN:
0278-6915
Subject:
enzyme inhibitors,   etc   ; amphetamine; antagonists; gene expression; genes; mice; neurotoxicity; phosphorylation; protein kinase C; toxicology;     Show all 10 Subjects
Abstract:
... p-Chloroamphetamine (PCA), an amphetamine derivative, has been shown to induce serotonergic toxicity. However, the precise mechanism of serotonergic toxicity induced by PCA remains unclear. In this study, PCA treatment (20 mg/kg, i.p.) did not significantly change 5-HT₁A receptor gene expression, but significantly increased 5-HT₂A receptor gene expression. Furthermore, 5-HT₂A receptor antagonist M ...
DOI:
10.1016/j.fct.2020.111395

9. Synopsis of recent synthetic methods and biological applications of phosphinic acid derivatives

Author:
Abdou, Moaz M.
Source:
Tetrahedron 2020 v.76 no.25 pp. 131251
ISSN:
0040-4020
Subject:
enzyme inhibitors,   etc   ; acids; aldehydes; alkenes; allylation; benzylation; cross-coupling reactions; drugs; enantiomers; enzymes; heterocyclic compounds; phosphorylation;     Show all 12 Subjects
Abstract:
... The chemistry of phosphinic acid derivatives has attracted increasing attention in both synthetic organic and biological fields, and great progress in the application of such compounds has been achieved in recent years. This review aims to document a systematic account of the prevailing methods for the synthesis of acyclic/cyclic phosphinic acids either in enantiopure or in racemic form. The most ...
DOI:
10.1016/j.tet.2020.131251

10. Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned

Author:
Choi, Ryan; Hulverson, Matthew A.; Huang, Wenlin; Vidadala, Rama S.R.; Whitman, Grant R.; Barrett, Lynn K.; Schaefer, Deborah A.; Betzer, Dana P.; Riggs, Michael W.; Doggett, J. Stone; Hemphill, Andrew; Ortega-Mora, Luis Miguel; McCloskey, Molly C.; Arnold, Samuel L.M.; Hackman, Robert C.; Marsh, Kennan C.; Lynch, James J.; Freiberg, Gail M.; Leroy, Bruce E.; Kempf, Dale J.; Choy, Robert K.M.; de Hostos, Eugenio L.; Maly, Dustin J.; Fan, Erkang; Ojo, Kayode K.; Van Voorhis, Wesley C.
Source:
International journal for parasitology 2020 v.50 no.5 pp. 413-422
ISSN:
0020-7519
Subject:
enzyme inhibitors,   etc   ; Miozoa; glycine (amino acid); parasitoses; pharmacology; protein kinases; therapeutics;     Show all 7 Subjects
Abstract:
... Bumped Kinase Inhibitors, targeting Calcium-dependent Protein Kinase 1 in apicomplexan parasites with a glycine gatekeeper, are promising new therapeutics for apicomplexan diseases. Here we will review advances, as well as challenges and lessons learned regarding efficacy, safety, and pharmacology that have shaped our selection of pre-clinical candidates. ...
DOI:
10.1016/j.ijpara.2020.01.006

11. Preparation of ACE-inhibitory peptides from milk protein in continuous enzyme membrane reactor with gradient dilution feeding substrate

Author:
Huang, Shanfen; Gong, Yang; Li, Yunliang; Ruan, Siyu; Roknul Azam, S M; Duan, Yuqing; Ye, Xiaofei; Ma, Haile
Source:
Process biochemistry 2020 v.92 pp. 130-137
ISSN:
1359-5113
Subject:
angiotensin-converting enzyme inhibitors,   etc   ; hydrolysis; inhibitory concentration 50; kinetics; milk proteins; peptides; peptidyl-dipeptidase A;     Show all 7 Subjects
Abstract:
... In this study, a novel method of gradient dilution feeding substrate (GDFS) was established to improve the yield of angiotensin-converting enzyme (ACE) inhibitory peptides from milk protein. The hydrolysis process stability, enzymatic efficiency and kinetics of the method were studied and compared with traditional feeding modes, viz., adding water after feeding substrate or constant concentration ...
DOI:
10.1016/j.procbio.2020.02.030

12. Epigenetic Therapy for Epithelioid Sarcoma

Author:
Rothbart, Scott B.; Baylin, Stephen B.
Source:
Cell 2020 v.181 no.2 pp. 211
ISSN:
0092-8674
Subject:
enzyme inhibitors,   etc   ; chromatin; epigenetics; lysine; methyltransferases; mutation; sarcoma; therapeutics; transcription (genetics);     Show all 9 Subjects
Abstract:
... Tazemetostat is the first epigenetic therapy to gain FDA approval in a solid tumor. This lysine methyltransferase inhibitor targets EZH2, the enzymatic subunit of the PRC2 transcriptional silencing complex. Tumors with mutations in subunits of the SWI/SNF chromatin remodeling complex, inclusive of most epithelioid sarcomas, are sensitive to EZH2 inhibition. ...
DOI:
10.1016/j.cell.2020.03.042

13. Adverse Outcome Pathway Network–Based Assessment of the Interactive Effects of an Androgen Receptor Agonist and an Aromatase Inhibitor on Fish Endocrine Function

Author:
Ankley, Gerald T.; Blackwell, Brett R.; Cavallin, Jenna E.; Doering, Jon A.; Feifarek, David J.; Jensen, Kathleen M.; Kahl, Michael D.; LaLone, Carlie A.; Poole, Shane T.; Randolph, Eric C.; Saari, Travis W.; Villeneuve, Daniel L.
Source:
Environmental toxicology and chemistry 2020 v.39 no.4 pp. 913-922
ISSN:
0730-7268
Subject:
enzyme inhibitors,   etc   ; adverse outcome pathways; agonists; androgen receptors; aromatase; estradiol; fadrozole; females; minnows; prediction; toxicity; vitellogenin;     Show all 12 Subjects
Abstract:
... Predictive approaches to assessing the toxicity of contaminant mixtures have been largely limited to chemicals that exert effects through the same biological molecular initiating event. However, by understanding specific pathways through which chemicals exert effects, it may be possible to identify shared “downstream” nodes as the basis for forecasting interactive effects of chemicals with differe ...
DOI:
10.1002/etc.4668

14. Synthesis of a protected 2-aminocyclobutanone as a modular transition state synthon for medicinal chemistry

Author:
Habeeb Mohammad, Thahani S.; Reidl, Cory T.; Zeller, Matthias; Becker, Daniel P.
Source:
Tetrahedron letters 2020 v.61 no.12 pp. 151632
ISSN:
0040-4039
Subject:
enzyme inhibitors,   etc   ; chemical reactions; chlorides; crystal structure; isothiocyanates; lead; metalloproteinases; serine proteinases; urea;     Show all 9 Subjects
Abstract:
... The hydrochloride salt of ɑ-aminocyclobutanone protected as its dimethyl acetal 2,2-dimethoxycyclobutan-1-aminium chloride (3) has been prepared as a modular synthon for convenient access to cyclobutanone-containing lead inhibitors of hydrolase enzymes including serine proteases and metalloproteases. Protected ɑ-aminocyclobutanone 3 was converted to representative amide and sulfonamide-functionali ...
DOI:
10.1016/j.tetlet.2020.151632

15. Inhibition of streptococcal biofilm formation by Aronia by extracellular RNA degradation

Author:
Lee, Heon‐Jin; Oh, Su Young; Hong, Su‐Hyung
Source:
Journal of the science of food and agriculture 2020 v.100 no.4 pp. 1806-1811
ISSN:
0022-5142
Subject:
enzyme inhibitors,   etc   ; Aronia melanocarpa; RNA; antimicrobial properties; biofilm; etiology; juices; mouth diseases; ribonucleases; tap water;     Show all 10 Subjects
Abstract:
... BACKGROUND: The accumulation of oral bacterial biofilms is one of the primary etiological factors for oral diseases. Aronia melanocarpa extracts display general health benefits, including antimicrobial activities. This study evaluates the inhibitory effect of Aronia juice on oral streptococcal biofilm formation. RESULTS: Exposure to 1/10‐diluted Aronia juice for 1 min significantly decreased in vi ...
DOI:
10.1002/jsfa.10223

16. Dynasore potentiates c-Met inhibitors against hepatocellular carcinoma through destabilizing c-Met

Author:
Zaky, Mohamed Y.; Liu, Xiuxiu; Wang, Taishu; Wang, Shanshan; Liu, Fang; Wang, Duchuang; Wu, Yueguang; Zhang, Yang; Guo, Dong; Sun, Qianhui; Li, Qiong; Zhang, Jinrui; Zhang, Yingqiu; Dong, Weijie; Liu, Zhenhua; Liu, Shuyan; Liu, Han
Source:
Archives of biochemistry and biophysics 2020 v.680 pp. 108239
ISSN:
0003-9861
Subject:
enzyme inhibitors,   etc   ; apoptosis; cell cycle checkpoints; cell proliferation; dynamins; hepatoma; patients; phosphorylation; therapeutics; tyrosine;     Show all 10 Subjects
Abstract:
... c-Met receptor is frequently overexpressed in hepatocellular carcinoma and thus considered as an attractive target for pharmacological intervention with small molecule tyrosine kinase inhibitors. Albeit with the development of multiple c-Met inhibitors, none reached clinical application in the treatment of hepatoma so far. To improve the efficacy of c-Met inhibitors towards hepatocellular carcinom ...
DOI:
10.1016/j.abb.2019.108239

17. Role of protein S-nitrosylation in regulating beef tenderness

Author:
Hou, Qin; Zhang, Chao-yang; Zhang, Wan-gang; Liu, Rui; Tang, Hanqi; Zhou, Guang-hong
Source:
Food chemistry 2020 v.306 pp. 125616
ISSN:
0308-8146
Subject:
enzyme inhibitors,   etc   ; autolysis; beef; cattle; desmin; muscles; myofibrillar proteins; nitric oxide; nitric oxide synthase; proteolysis; tenderizing;     Show all 11 Subjects
Abstract:
... This research aimed to explore the role of protein S-nitrosylation in regulating the tenderness of postmortem beef, from the perspective of μ-calpain autolysis and protein proteolysis. Five bovine semimembranosus muscles were incubated with three treatments including S-nitrosoglutathione (GSNO, nitric oxide donor), normal saline and Nω-nitro-L-arginine methyl ester hydrochloride (L-NAME, nitric ox ...
DOI:
10.1016/j.foodchem.2019.125616

18. Cu-Mediated Expeditious Annulation of Alkyl 3-Aminoacrylates with Aryldiazonium Salts: Access to Alkyl N²-Aryl 1,2,3-Triazole-carboxylates for Druglike Molecular Synthesis

Author:
Liu, Hao-Nan; Cao, Hao-Qiang; Cheung, Chi Wai; Ma, Jun-An
Source:
Organic letters 2020 v.22 no.4 pp. 1396-1401
ISSN:
1523-7052
Subject:
enzyme inhibitors,   etc   ; carbonate dehydratase; chemical reactions; chemical structure; organic compounds; salts;     Show all 6 Subjects
Abstract:
... Alkyl N-aryl 1,2,3-triazole-carboxylates are important molecules or intermediates in medicinal chemistry, but the synthesis of N²-aryl counterparts remains elusive. Herein, we describe a Cu-mediated annulation reaction of alkyl 3-aminoacrylates with aryldiazonium salts, both of which are readily available substrates. Furthermore, alkyl 2-aminoacrylates are also viable substrates. Diverse alkyl N²- ...
DOI:
10.1021/acs.orglett.0c00006

19. Effects of aminoguanidine on γ‐aminobutyric acid accumulation pathways in fresh tea leaves under hypoxic conditions

Author:
Wu, Qinyan; Guo, Rui; Zhang, Wenwen; Li, Dongdong; Rao, Bing; Ma, Shengzhou; Zhao, Fei; Yao, Kebing; Zhuang, Yiqing
Source:
International journal of food science & technology 2020 v.55 no.2 pp. 899-907
ISSN:
0950-5423
Subject:
enzyme inhibitors,   etc   ; anaerobic conditions; diamine oxidase; gamma-aminobutyric acid; leaves; polyamines; tea;     Show all 7 Subjects
Abstract:
... Aminoguanidine (AG), a specific inhibitor of diamine oxidase (DAO), can be used to investigate the γ‐aminobutyric acid (GABA) accumulation pathways. The effect of AG on GABA accumulation pathways of tea fresh leaves remains to be explored. Our results indicated AG concentration did not significantly affect GAD activity, but high concentration solution made GABA‐T activity increase. AG (1 mm) maxim ...
DOI:
10.1111/ijfs.14360

20. The effect of acetylation on the protein stability of BmApoLp‐III in the silkworm, Bombyx mori

Author:
Yang, F.; Zhu, B.; Liu, J.; Liu, Y.; Jiang, C.; Sheng, Q.; Qiu, J.; Nie, Z.
Source:
Insect molecular biology 2020 v.29 no.1 pp. 104-111
ISSN:
0962-1075
Subject:
enzyme inhibitors,   etc   ; Bombyx mori; acetylation; cycloheximide; enzymes; hemolymph; protein degradation; silkworms; storage proteins; ubiquitin; ubiquitination;     Show all 11 Subjects
Abstract:
... Acetylation is an important, reversible posttranslational modification to a protein. In a previous study, we found that there were a large number of acetylated sites in various nutrient storage proteins of the silkworm haemolymph. In this study, we confirmed that acetylation can affect the stability of nutrient storage protein Bombyx mori apolipophorin‐III (BmApoLp‐III). First, the expression of B ...
DOI:
10.1111/imb.12613