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1. 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

2. An optimized procedure for direct access to 1H-indazole-3-carboxaldehyde derivatives by nitrosation of indoles

Author:
Chevalier, Arnaud; Ouahrouch, Abdelaaziz; Arnaud, Alexandre; Gallavardin, Thibault; Franck, Xavier
Source:
RSC advances 2018 v.8 no.24 pp. 13121-13128
ISSN:
2046-2069
Subject:
enzyme inhibitors,   etc   ; biochemistry; indoles;     Show all 3 Subjects
Abstract:
... Indazole derivatives are currently drawing more and more attention in medicinal chemistry as kinase inhibitors. 1H-indazole-3-carboxaldehydes are key intermediates to access to a variety of polyfunctionalized 3-substituted indazoles. We report here a general access to this motif, based on the nitrosation of indoles in a slightly acidic environment. These very mild conditions allow the conversion o ...
DOI:
10.1039/c8ra01546e

3. The discovery of shorter synthetic proteolytic peptides derived from Tob1 protein

Author:
Nakamura, Rina; Konishi, Motomi; Taniguchi, Masanari; Hatakawa, Yusuke; Akizawa, Toshifumi
Source:
Peptides 2019 v.116 pp. 71-77
ISSN:
0196-9781
Subject:
enzyme inhibitors,   etc   ; drugs; enzyme activity; proteolysis; synthetic peptides; trypsin;     Show all 6 Subjects
Abstract:
... We screened nearly 1000 synthetic peptides and found that JAL-AK22 (KYEGHWYPEKPYKGSGFRCIHI), which is derived from the BoxA domain in the Tob1 protein, activates both unfolded and folded proMMP-7. Interestingly, the smaller derivative of JAL-AK22, termed JAL-TA9 (YKGSGFRMI) possessed auto-proteolytic activity and cleaved three synthetic peptides fragment (MMP18-33, MMP18-40, and Aβ11-29) under phy ...
DOI:
10.1016/j.peptides.2019.03.005

4. Supramolecular azasugar clusters based on an amphiphilic fatty-acid-deoxynojirimycin derivative as multivalent glycosidase inhibitors

Author:
Li, Min; Wang, Ke-Rang; Yang, Jian-Xing; Peng, Ya-Tong; Liu, Yi-Xuan; Zhang, Hong-Xin; Li, Xiao-Liu
Source:
Journal of materials chemistry B 2019 v.7 no.9 pp. 1379-1383
ISSN:
2050-7518
Subject:
enzyme inhibitors,   etc   ; alpha-mannosidase; deoxynojirimycin; glycemic effect; mice; pH;     Show all 6 Subjects
Abstract:
... A novel supramolecular multivalent glycosidase inhibitor was constructed based on the amphiphilic deoxynojirimycin derivative FA-DNJ. FA-DNJ self-assembled into spherical assemblies with the diameters between 103 nm and 137 nm under different pH values (pH 2–7) and showed a potent glycosidase effect against α-mannosidase with a Kᵢ value of 0.11 μM, an effect that increased approximately 330-fold c ...
DOI:
10.1039/c8tb03249a

5. One-pot propagation of (Hetero)Arylamines: Modular synthesis of diverse Amino-di(hetero)arylamines

Author:
Liang, Xueting; Xu, Liang; Li, Cuihua; Jia, Xin; Wei, Yu
Source:
Tetrahedron 2019 v.75 no.6 pp. 721-731
ISSN:
0040-4020
Subject:
enzyme inhibitors,   etc   ; aniline; chemical structure; cross-coupling reactions; nitrobenzenes;     Show all 5 Subjects
Abstract:
... Formal propagation of (hetero)arylamine is achieved via a one-pot Buchwald–Hartwig C–N cross-coupling and nitro reduction sequence, enabling a rapid modular synthesis of diverse amino-di(hetero)arylamines from (hetero)arylamines and halogenated nitrobenzenes. Various functionalized aromatic amines with different electronic and steric environments can be efficiently prolongated to formally incorpor ...
DOI:
10.1016/j.tet.2018.12.035

6. Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

Author:
Krajcovicova, S.; Jorda, R.; Hendrychova, D.; Krystof, V.; Soural, M.
Source:
Chemical communications 2019 v.55 no.7 pp. 929-932
ISSN:
1364-548X
Subject:
enzyme inhibitors,   etc   ; chemical compounds; chemical reactions; chimerism; moieties; protein kinases;     Show all 6 Subjects
Abstract:
... A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment. ...
DOI:
10.1039/c8cc08716d

7. Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles

Author:
Wang, Dong; Li, Linna; Feng, Hairong; Sun, Hua; Almeida-Veloso, Fabrice; Charavin, Marine; Yu, Peng; Désaubry, Laurent
Source:
Green chemistry 2018 v.20 no.12 pp. 2775-2780
ISSN:
1463-9270
Subject:
enzyme inhibitors,   etc   ; aldehydes; amines; green chemistry; stereoselectivity;     Show all 5 Subjects
Abstract:
... An efficient synthesis of fully substituted 2,3-dihydropyrroles has been achieved in one step through the three-component reaction of amines, aromatic aldehydes and α-ketoamides. This atom-economical and catalyst-free reaction is highly stereoselective and generates underexplored heterocycles in a single step. These compounds were examined in an enzymatic assay that led to the identification of po ...
DOI:
10.1039/c8gc00987b

8. Toward a Slow-Release Borate Inhibitor To Control Mild Steel Corrosion in Simulated Recirculating Water

Author:
Cui, Jun; Yang, Yange; Li, Xiuqing; Yuan, Wenjiao; Pei, Yuansheng
Source:
ACS applied materials & interfaces 2018 v.10 no.4 pp. 4183-4197
ISSN:
1944-8252
Subject:
enzyme inhibitors,   etc   ; borates; corrosion; electrochemistry; models; steel;     Show all 6 Subjects
Abstract:
... On the basis of their potential passivating characteristics, in this study, borates have been used to synthesize a novel slow-release inhibitor to suppress long-term mild steel corrosion in simulated recirculating water. The passivating performance was characterized by various electrochemical measurements and the passivating mechanism was interpreted by the point defect model. The experimental res ...
DOI:
10.1021/acsami.7b15507

9. Genome-scale network model of metabolism and histone acetylation reveals metabolic dependencies of histone deacetylase inhibitors

Author:
Shen, Fangzhou; Boccuto, Luigi; Pauly, Rini; Srikanth, Sujata; Chandrasekaran, Sriram
Source:
Genome biology 2019 v.20 no.1 pp. 49
ISSN:
1474-760X
Subject:
enzyme inhibitors,   etc   ; acetylation; drugs; epigenetics; genes; histone deacetylase; histones; metabolism; metabolites; models; prediction;     Show all 11 Subjects
Abstract:
... Histone acetylation plays a central role in gene regulation and is sensitive to the levels of metabolic intermediates. However, predicting the impact of metabolic alterations on acetylation in pathological conditions is a significant challenge. Here, we present a genome-scale network model that predicts the impact of nutritional environment and genetic alterations on histone acetylation. It identi ...
DOI:
10.1186/s13059-019-1661-z

10. Detection of casein kinase II by aggregation-induced emission

Author:
Luan, Zhenzhu; Zhao, Li; Liu, Chao; Song, Weiling; He, Peng; Zhang, Xiaoru
Source:
Talanta 2019 v.201 pp. 450-454
ISSN:
0039-9140
Subject:
enzyme inhibitors,   etc   ; carboxypeptidase C; hydrophilicity; hydrophobicity; non-specific serine/threonine protein kinase; peptides; phosphorylation;     Show all 7 Subjects
Abstract:
... A novel aggregation-induced emission (AIE) probe comprised of a hydrophilic protein kinase specific peptide and a hydrophobic tetraphenylethene (TPE) unit was synthesized through click reaction. The prepared TPE-peptide probe could be completely degraded by carboxypeptidase Y (CPY) to release hydrophobic TPE part, which aggregated in buffer solution and showed strong TPE emission. In the presence ...
DOI:
10.1016/j.talanta.2019.04.036

11. Benzonitriles as tyrosinase inhibitors with hyperbolic inhibition manner

Author:
Nihei, Ken-ichi; Kubo, Isao
Source:
International journal of biological macromolecules 2019 v.133 pp. 929-932
ISSN:
0141-8130
Subject:
enzyme inhibitors,   etc   ; active sites; copper; enzyme inhibition; enzymes; inhibitory concentration 50; mushrooms; oxidation;     Show all 8 Subjects
Abstract:
... As a novel mushroom tyrosinase inhibitor, 4-methoxybenzonitrile (anisnitrile) was identified (IC50 = 111.1 μM) with hyperbolic inhibition manner. The calculated αKi (166.3 μM) was larger than Ki (66.5 μM) by Dixon plots, indicating that this nitrile acts as a competitive-noncompetitive mixed type inhibitor. Similarly, 4-isopropylbenzonitrile (cuminnitrile) partially inhibited the oxidation catalyz ...
DOI:
10.1016/j.ijbiomac.2019.04.156

12. MMP targeting in the battle for vision: Recent developments and future prospects in the treatment of diabetic retinopathy

Author:
Drankowska, Justyna; Kos, Michał; Kościuk, Andrzej; Marzęda, Paweł; Boguszewska-Czubara, Anna; Tylus, Magdalena; Święch-Zubilewicz, Anna
Source:
Life sciences 2019 v.229 pp. 149-156
ISSN:
0024-3205
Subject:
enzyme inhibitors,   etc   ; Alzheimer disease; atherosclerosis; blindness; diabetic retinopathy; disease course; extracellular matrix; metalloproteinases; neoplasms; therapeutics; vision;     Show all 11 Subjects
Abstract:
... Matrix metalloproteinases (MMPs) are enzymes capable of degrading nearly all types of extracellular matrix. They perform a wide range of roles in physiological processes, which is the reason for their strict regulation by numerous mechanisms including natural tissue inhibitors of metalloproteinases (TIMP). Research only started to shed light on more troublesome aspects of MMPs function, like cance ...
DOI:
10.1016/j.lfs.2019.05.038

13. Total synthesis of (±)-fumimycin and analogues for biological evaluation as peptide deformylase inhibitors

Author:
Zaghouani, Mehdi; Bögeholz, Lena A.K.; Mercier, Evan; Wintermeyer, Wolfgang; Roche, Stéphane P.
Source:
Tetrahedron 2019 v.75 no.24 pp. 3216-3230
ISSN:
0040-4020
Subject:
enzyme inhibitors,   etc   ; Suzuki reaction; amino acids; antibacterial properties; chlorination; enzymes; moieties; organic compounds; peptides; regioselectivity;     Show all 10 Subjects
Abstract:
... A concise 7-step total synthesis of (±)-fumimycin in 11.6% overall yield is reported. An acid-catalyzed intramolecular aza-Friedel–Crafts cyclization was developed to construct the benzofuranone skeleton of the natural product bearing an α,α-disubstituted amino acid moiety in a single step. Regioselective chlorination followed by a Suzuki–Miyaura cross-coupling rapidly enabled the preparation of a ...
DOI:
10.1016/j.tet.2019.03.037

14. Novel inhibitors against wild-type and mutated HCV NS3 serine protease: an in silico study

Author:
Ezat, Ahmed A.; Elfiky, Abdo A.; Elshemey, Wael M.; Saleh, Noha A.
Source:
Virusdisease 2019 v.30 no.2 pp. 207-213
ISSN:
2347-3584
Subject:
enzyme inhibitors,   etc   ; Hepatitis C virus; computer simulation; patients; serine proteinases; therapeutics;     Show all 6 Subjects
Abstract:
... In 2011, the FDA approved boceprevir as a hepatitis C virus (HCV) NS3 serine protease inhibitor. The sustained virological response rate for treatment with this approved compound is considerably low. Patients have not responded as much as expected to boceprevir therapy. In this in silico study, modified boceprevir compounds are suggested and tested on wild-type HCV NS3 protease and 19 mutated HCV ...
DOI:
10.1007/s13337-019-00516-7

15. Relationships of dietary flavonoid structure with its tyrosinase inhibitory activity and affinity

Author:
Fan, Meihui; Ding, Huafang; Zhang, Guowen; Hu, Xing; Gong, Deming
Source:
Lebensmittel-Wissenschaft + [i.e. und] Technologie 2019 v.107 pp. 25-34
ISSN:
0023-6438
Subject:
enzyme inhibitors,   etc   ; amino acids; binding capacity; enzyme inhibition; enzymes; flavonols; glycosylation; hydrogen bonding; hydrogenation; hydroxylation; methylation;     Show all 11 Subjects
Abstract:
... Flavonoids possess the inhibition ability against tyrosinase. Here, the effects of flavonoids structure on inhibitory activity and binding affinity of tyrosinase were investigated. The results showed that the hydroxy groups of 5C−OH, 4′C−OH and 5′C−OH of flavonoids were in favor of forming hydrogen bond with the amino acid residues of tyrosinase, which played a crucial role in the binding and inte ...
DOI:
10.1016/j.lwt.2019.02.076

16. Divalent oseltamivir analogues as potent influenza neuraminidase inhibitors

Author:
Yan, Zhong-Li; Liu, Ao-Yun; Wei, Xia-Xia; Zhang, Zhuang; Qin, Long; Yu, Qun; Yu, Peng; Lu, Kui; Yang, Yang
Source:
Carbohydrate research 2019 v.477 pp. 32-38
ISSN:
0008-6215
Subject:
enzyme inhibitors,   etc   ; Orthomyxoviridae; carbohydrates; esterification; influenza; oseltamivir; sialidase; structure-activity relationships; virion; viruses;     Show all 10 Subjects
Abstract:
... A panel of divalent oseltamivir and guanidino oseltamivir analogues with esterification on the carboxyl acid group as potent inhibitors of influenza virus neuraminidase was prepared via click reaction. The primary structure activity relationship study demonstrated that appropriate distance between two oseltamivir monomers around 30 Å can crosslink two adjacent neuraminidase tetramers on the virion ...
DOI:
10.1016/j.carres.2019.03.012

17. Highly potent bacterial neuraminidase inhibitors, chromenone derivatives from Flemingia philippinensis

Author:
Wang, Yan; Kim, Jeong Yoon; Song, Yeong Hun; Li, Zuo Peng; Yoon, Sang Hwa; Uddin, Zia; Ban, Yeong Jun; Lee, Keun Woo; Park, Ki Hun
Source:
International journal of biological macromolecules 2019 v.128 pp. 149-157
ISSN:
0141-8130
Subject:
enzyme inhibitors,   etc   ; Flemingia; bacterial infections; binding capacity; computer simulation; inflammation; inhibitory concentration 50; pathogenesis; sialidase;     Show all 9 Subjects
Abstract:
... The chromenone derivatives (1–4) from the root part of Flemingia philippinensis showed a significant inhibition against bacterial neuraminidase (NA) which plays a pivotal role in a cellular interaction including pathogenesis of bacterial infection and subsequent inflammation. The compounds 1 and 2 were the new compounds, philippin D (1) and philippin E (2). In particular, compounds (1–3) exhibited ...
DOI:
10.1016/j.ijbiomac.2019.01.105

18. A laser-induced TiO₂-decorated graphene photoelectrode for sensitive photoelectrochemical biosensing

Author:
Ge, Lei; Hong, Qing; Li, Hui; Li, Feng
Source:
Chemical communications 2019 v.55 no.34 pp. 4945-4948
ISSN:
1364-548X
Subject:
enzyme inhibitors,   etc   ; acetylcholinesterase; biosensors; chemical reactions; glass; graphene; indium tin oxide; light;     Show all 8 Subjects
Abstract:
... Herein, direct-laser-writing of TiO₂-decorated graphene on indium-tin oxide glass was demonstrated to fabricate a unique photoelectrode with a rapid and stable photoelectrochemical response under visible light; this photoelectrode was then applied in a photoelectrochemical enzymatic biosensor for the sensitive detection of an acetylcholinesterase inhibitor. ...
DOI:
10.1039/c9cc00889f

19. Simultaneous identification and determination of eleven tyrosine kinase inhibitors by supercritical fluid chromatography-mass spectrometry

Author:
Zhang, Shaomin; Jin, Wei; Yang, Yongjian
Source:
Analytical methods 2019 v.11 no.16 pp. 2211-2222
ISSN:
1759-9679
Subject:
enzyme inhibitors,   etc   ; additives; markets; mass spectrometry; supercritical fluid chromatography; temperature; tyrosine;     Show all 7 Subjects
Abstract:
... A rapid analytical method using supercritical fluid chromatography (SFC) coupled to mass spectrometry for the simultaneous identification and determination of eleven tyrosine kinase inhibitors (TKIs) was developed and validated. For quantitative assay, a tested solution with a high concentration of 0.4 mg mL⁻¹ was applied for SFC determination. For identification purposes, a diluted solution with ...
DOI:
10.1039/c9ay00332k

20. Autophagy and mitochondrial metabolism: insights into their role and therapeutic potential in chronic myeloid leukaemia

Author:
Baquero, Pablo; Dawson, Amy; Helgason, Gudmundur Vignir
Source:
TheFEBS journal 2019 v.286 no.7 pp. 1271-1283
ISSN:
1742-464X
Subject:
enzyme inhibitors,   etc   ; autophagy; metabolism; mitochondria; myeloid leukemia; patients; stem cells; therapeutics; tyrosine;     Show all 9 Subjects
Abstract:
... Despite the development of selective BCR‐ABL‐targeting tyrosine kinase inhibitors (TKIs) transforming the management of chronic myeloid leukaemia (CML), therapy‐resistant leukaemic stem cells (LSCs) persist after TKI treatment and present an obstacle to a CML cure. Recently, we and others have made significant contributions to the field by unravelling survival dependencies in LSCs to work towards ...
DOI:
10.1111/febs.14659