当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > A novel cathepsin L inhibitor prevents the progression of idiopathic pulmonary fibrosis.

A novel cathepsin L inhibitor prevents the progression of idiopathic pulmonary fibrosis.

Abstract：

:In previous work, the target of asperphenamate as a natural product was successfully determined as cathepsin by the natural product consensus pharmacophore strategy. In order to develop accurate SAR (structure-activity relationship) of asperphenamate-type cathepsin inhibitor, we chose several novel analogs with heterocyclic moiety to perform further study. The molecular simulation showed that 4-pyridyl derivative 3 with the greatest cathepsin inhibitory activity presented new interaction modes with protein utilizing its B-ring moiety. And then molecular dynamics (MD) simulation further revealed that 3 and cathepsin kept stable interaction in the binding site, which validated the molecular docking results. In view that cathepsins play an important role in fibrosis and some cathepsin inhibitors display the therapeutic ability for fibrosis, we investigated the anti-fibrotic effect of 3in vitro and in vivo. The results indicated that 3 displayed the strongest inhibitory effect on the formation of α-SMA and collagen I as the protein markers of fibrosis among all tested derivatives. Further in vivo assay confirmed that 3 indeed showed significant inhibitory ability against pulmonary fibrosis by the method of H&E and Masson staining as well as immunohistochemical staining for characteristic α-SMA proteins.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Yuan L,Zou C,Ge W,Liu Y,Hu B,Wang J,Lin B,Li Y,Ma E

doi

10.1016/j.bioorg.2019.103417

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

103417

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)31246-5

journal_volume

94

pub_type

杂志文章

相关文献

BIOORGANIC CHEMISTRY文献大全
  • The effective molarity (EM) puzzle in proton transfer reactions.

    abstract：:The DFT and HF calculation results for the proton transfer reactions of three different systems reveal that the reaction mechanism (transfer of a proton to a nucleophile) is largely determined by the distance between the two reactive centers (r). Systems with relatively large r values tend to abstract a proton from a ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2009.04.003

    authors： Karaman R

    更新日期：2009-08-01 00:00:00

  • Characterization of inhibitory constituents of NO production from Catalpa ovata using LC-MS coupled with a cell-based assay.

    abstract：:An effective screening method for inhibitors of NO production in natural products using LC-QTOF MS/MS coupled with a cell-based assay was proposed. The ethyl acetate fraction of Catalpa ovata exhibited a strong inhibitory effect on NO production in lipopolysaccharide-induced BV2 microglia cells. We attempted to identi...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.05.023

    authors： Park S,Shin H,Park Y,Choi I,Park B,Lee KY

    更新日期：2018-10-01 00:00:00

  • Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.

    abstract：:Five novel 1H-pyrrolo[2,3-b]pyridine or 1H-pyrazolo[3,4-b]pyridine derivatives, with a methylene, sulfur, sulfoxide or cyclopropyl group as a linker, were designed, synthesized and biologically evaluated against c-Met and ALK. The development of these methods of compound synthesis may provide an important reference fo...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2016.02.009

    authors： Liu N,Wang Y,Huang G,Ji C,Fan W,Li H,Cheng Y,Tian H

    更新日期：2016-04-01 00:00:00

  • Synthesis, biological evaluation and molecular docking studies of novel 3,5-disubstituted 2,4-thiazolidinediones derivatives.

    abstract：:A series of thirteen novel 2,4-thiazolidinedione derivatives were synthesized through three step reaction procedure. The title compounds were synthesized by Knoevenagel condensation at the 5th position of the 2,4-thiazolidinedione ring. Various physicochemical and spectral studies were conducted to characterize the sy...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.102993

    authors： Ranjan Srivastava A,Bhatia R,Chawla P

    更新日期：2019-08-01 00:00:00

  • Quinoxalines as potent selective CRFRs ligands for monitoring and brain diagnostic.

    abstract：:The paper highlighted quinoxalines as potent ligands to corticotropin-releasing factor receptor types 1 and 2. The content includes design and structure-activity relationship of 50 model substances to CRFR1, CRFR2α and CRF2β, respectively. It is important to bear in mind, that our concept has based on challenging rese...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2014.10.008

    authors： Ivanova B,Spiteller M

    更新日期：2015-02-01 00:00:00

  • Chemical characterization of cytotoxic indole acetic acid derivative from mulberry fruit (Morus alba L.) against human cervical cancer.

    abstract：:The fruit of the white mulberry tree (Morus alba L.) is a multiple fruit with a sweet flavor commonly consumed around the world. Chemical investigation of the fruits led to the isolation of two indole acetic acid derivatives (1 -2) including a new compound, which turned out to be an isolation artifact, 3S-(β-D-glucopy...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2017.10.015

    authors： Yu JS,Lee D,Lee SR,Lee JW,Choi CI,Jang TS,Kang KS,Kim KH

    更新日期：2018-02-01 00:00:00

  • Design, synthesis and biological evaluation of some novel benzothiazole/benzoxazole and/or benzimidazole derivatives incorporating a pyrazole scaffold as antiproliferative agents.

    abstract：:In an aim at developing new antiproliferative agents, new series of benzothiazole/benzoxazole and/or benzimidazole substituted pyrazole derivatives 11a-c, 12a-c and 13a-c were prepared and evaluated for their antiproliferative activity against breast carcinoma (MCF-7) and non-small cell lung cancer (A549) cell lines. ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2017.07.007

    authors： Abdelgawad MA,Bakr RB,Omar HA

    更新日期：2017-10-01 00:00:00

  • Synthesis of Mitomycin C and decarbamoylmitomycin C N6 deoxyadenosine-adducts.

    abstract：:Mitomycin C (MC), an anti-cancer drug, and its analog, decarbamoylmitomycin C (DMC), are DNA-alkylating agents. MC is currently used in the clinics and its cytotoxicity is mainly due to its ability to form Interstrand Crosslinks (ICLs) which impede DNA replication and, thereby, block cancer cells proliferation. Howeve...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103280

    authors： Zheng M,Hwang S,Snyder T,Aquilina J,Proni G,Paz MM,Pradhan P,Cheng SY,Champeil E

    更新日期：2019-11-01 00:00:00

  • Synthesis of pyrimidine-2,4,6-trione derivatives: Anti-oxidant, anti-cancer, α-glucosidase, β-glucuronidase inhibition and their molecular docking studies.

    abstract：:This paper describes a facile protocol, efficient, and environmentally benign for the synthesis a series of barbiturate acid substituted at C5 position 3a-o. The desired compounds subjected in vitro for different set of bioassays including against anti-oxidant (DPPH and super oxide scavenger assays), anti-cancer, α-gl...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2016.07.009

    authors： Barakat A,Islam MS,Al-Majid AM,Ghabbour HA,Yousuf S,Ashraf M,Shaikh NN,Iqbal Choudhary M,Khalil R,Ul-Haq Z

    更新日期：2016-10-01 00:00:00

  • Design and synthesis of novel 4-thiazolidinone derivatives with promising anti-breast cancer activity: Synthesis, characterization, in vitro and in vivo results.

    abstract：:Novel lead compounds as anticancer agents with the ability to circumvent emerging drug resistance have recently gained a great deal of interest. Thiazolidinones are among such compounds with well-established biological activity in the field of oncology. Here, we designed, synthesized and characterized a series of thia...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104276

    authors： Tahmasvand R,Bayat P,Vahdaniparast SM,Dehghani S,Kooshafar Z,Khaleghi S,Almasirad A,Salimi M

    更新日期：2020-11-01 00:00:00

  • Acetylenic fatty acids from Porcelia macrocarpa (Annonaceae) against trypomastigotes of Trypanosoma cruzi: Effect of octadec-9-ynoic acid in plasma membrane electric potential.

    abstract：:Porcelia macrocarpa (Warm.) R. E. Fries (Annonaceae) is an endemic plant in Brazil where its tasty pulp has been eaten fresh. The hexane extract from its flowers was subjected to chromatographic procedures to afford four acetylene derivatives identified as octadec-9-ynoic (stearolic acid - 1), (11E)-octadec-11-en-9-yn...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.03.025

    authors： Londero VS,da Costa-Silva TA,Gomes KS,Ferreira DD,Mesquita JT,Tempone AG,Young MCM,Jerz G,Lago JHG

    更新日期：2018-08-01 00:00:00

  • Photoactivable analogs for labeling 25-hydroxyvitamin D3 serum binding protein and for 1,25-dihydroxyvitamin D3 intestinal receptor protein.

    abstract：:3-Azidobenzoates and 3-azidonitrobenzoates of 25-hydroxyvitamin D3 as well as 3-deoxy-3-azido-25-hydroxyvitamin D3 and 3-deoxy-3-azido-1,25-dihydroxyvitamin D3 were prepared as photoaffinity labels for vitamin D serum binding protein and 1,25-dihydroxyvitamin D3 intestinal receptor protein. The compounds prepared wer...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/0045-2068(86)90023-4

    authors： Kutner A,Link RP,Schnoes HK,DeLuca HF

    更新日期：1986-01-01 00:00:00

  • Synthesis, anticancer effect and molecular modeling of new thiazolylpyrazolyl coumarin derivatives targeting VEGFR-2 kinase and inducing cell cycle arrest and apoptosis.

    abstract：:New thiazolylpyrazolyl coumarin derivatives were synthesized and tested for their anticancer potential in vitro against five different human cell lines, including breast MCF-7, lung A549, prostate PC3, liver HepG2 and normal melanocyte HFB4. Breast carcinoma revealed higher sensitivity towards compounds 7a, 8c, 9b, 9c...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.12.040

    authors： Mohamed TK,Batran RZ,Elseginy SA,Ali MM,Mahmoud AE

    更新日期：2019-04-01 00:00:00

  • Separation and configurational assignment of stereoisomeric phenalenones from the marine mangrove-derived fungus Penicillium herquei MA-370.

    abstract：:Eight phenalenone derivatives, including four new compounds, aceneoherqueinones A and B (1 and 2), (+)-aceatrovenetinone A (3a), and (+)-aceatrovenetinone B (3d), along with four known congeners, (-)-aceatrovenetinone A (3b), (-)-aceatrovenetinone B (3c), (-)-scleroderolide (4a), and (+)-scleroderolide (4b), were char...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104477

    authors： Yang SQ,Mándi A,Li XM,Liu H,Li X,Balázs Király S,Kurtán T,Wang BG

    更新日期：2021-01-01 00:00:00

  • Synthesis and evaluation of redox-sensitive gonadotropin-releasing hormone receptor-targeting peptide conjugates.

    abstract：:Lytic peptides have been demonstrated to exhibit obvious advantages in cancer therapy with binding ability toward tumor cells via electrostatic attractions, which are lack of active targeting and aggregation to tumor tissue. In the present study, five conjugated lytic peptides were redesigned and constructed to target...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.102945

    authors： Dai Y,Yue N,Liu C,Cai X,Su X,Bi X,Li Q,Li C,Huang W,Qian H

    更新日期：2019-07-01 00:00:00

  • QM/MM study of the reaction mechanism of Cl-cis,cis-muconate with muconate lactonizing enzyme.

    abstract：:The lactonization process of Cl-cis,cis-muconate catalyzed by anti-muconate lactonizing enzyme (anti-MLE) was studied theoretically with the aid of a combined quantum mechanics/molecular mechanics (QM/MM) approach. Two elementary processes steps involved in the lactanization process were investigated. The calculated e...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.05.007

    authors： Zhu L,Tang X,Li Y,Zhang R,Wang J,Zhang Q,Wang W

    更新日期：2018-10-01 00:00:00

  • Pesimquinolones I-S, eleven new quinolone alkaloids produced by Penicillium simplicissimum and their inhibitory activity on NO production.

    abstract：:Eleven undescribed quinolone alkaloids, pesimquinolones I-S (1-4 and 6-12), as well as eleven known congeners (5 and 13-22), were isolated from the solid culture broth of the fungus Penicillium simplicissimum. Their chemical structures with absolute configurations were established by a combination of NMR spectroscopy,...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2021.104635

    authors： Dai C,Li X,Zhang K,Li XN,Wang W,Zang Y,Chen X,Li Q,Wei M,Chen C,Zhu H,Zhang Y

    更新日期：2021-01-08 00:00:00

  • A novel bi-functional chalcone inhibits multi-drug resistant Staphylococcus aureus and potentiates the activity of fluoroquinolones.

    abstract：:Staphylococcus aureus is the leading cause of bacteraemia and the dwindling supply of effective antibacterials has exacerbated the problem of managing infections caused by this bacterium. Isoliquiritigenin (ISL) is a plant flavonoid that displays therapeutic potential against S. aureus. The present study identified a ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.10.024

    authors： Gupta VK,Gaur R,Sharma A,Akther J,Saini M,Bhakuni RS,Pathania R

    更新日期：2019-03-01 00:00:00

  • Synthesis of N-2(5H)-furanonyl sulfonyl hydrazone derivatives and their biological evaluation in vitro and in vivo activity against MCF-7 breast cancer cells.

    abstract：:A series of (E)-N-2(5H)-furanonyl sulfonyl hydrazone derivatives have been rationally designed and efficiently synthesized by one-pot reaction with good yields for the first time. This green approach with wide substrate range and good selectivity can be achieved at room temperature in a short time in the presence of m...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104518

    authors： Yang K,Yang JQ,Luo SH,Mei WJ,Lin JY,Zhan JQ,Wang ZY

    更新日期：2020-11-27 00:00:00

  • Bioactive secondary metabolites from the marine-associated fungus Aspergillus terreus.

    abstract：:Three new compounds, including a prenylated tryptophan derivative, luteoride E (1), a butenolide derivative, versicolactone G (2), and a linear aliphatic alcohol, (3E,7E)-4,8-dimethyl-undecane-3,7-diene-1,11-diol (3), together with nine known compounds (4-12), were isolated and identified from a coral-associated fungu...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.06.029

    authors： Liu M,Sun W,Wang J,He Y,Zhang J,Li F,Qi C,Zhu H,Xue Y,Hu Z,Zhang Y

    更新日期：2018-10-01 00:00:00

  • Ugi efficient synthesis, biological evaluation and molecular docking of coumarin-quinoline hybrids as apoptotic agents through mitochondria-related pathways.

    abstract：:Ugi reaction was a reliable procedure for the synthesis of new coumarin-quinoline frameworks. Excellent yields, mild reaction conditions and easily available and inexpensive starting materials are advantages of this protocol. Cytotoxic effects of fourteen products were investigated in A2780 human ovarian cancer cells....

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103147

    authors： Taheri S,Nazifi M,Mansourian M,Hosseinzadeh L,Shokoohinia Y

    更新日期：2019-10-01 00:00:00

  • Reaction of epichlorohydrin with adenosine, 2'-deoxyadenosine and calf thymus DNA: identification of adducts.

    abstract：:Epichlorohydrin (a probable human carcinogen) was allowed to react with adenosine and the adducts were characterized by NMR and UV spectroscopy, and mass spectrometry. The adduct initially formed was 1-(3-chloro-2-hydroxypropyl)-adenosine, which subsequently ring closures to 1,N(6)-(2-hydroxypropyl)-adenosine at neutr...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2006.01.005

    authors： Sund P,Kronberg L

    更新日期：2006-06-01 00:00:00

  • Probing 2-acetylbenzofuran hydrazones and their metal complexes as α-glucosidase inhibitors.

    abstract：:Inhibition of α-glucosidase is one of the important approaches in designing antidiabetic drugs for its role in decrease of the carbohydrates digestion to avoid post-prandial increase in blood sugar levels in diabetic patients. In the present study we designed a novel series of 2-acetylbenzofuran hydrazones (L1-L7) and...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104082

    authors： Khan S,Tariq M,Ashraf M,Abdullah S,Al-Rashida M,Khalid M,Taslimi P,Fatima M,Zafar R,Shafiq Z

    更新日期：2020-09-01 00:00:00

  • Building fluorescent sensors for carbohydrates using template-directed polymerizations.

    abstract：:The ability to custom-make fluorescent sensors for different analytes could have a tremendous impact in a variety of areas. Template-directed polymerization or molecular imprinting seems to be a promising approach for the preparation of high-affinity and specific binding sites for different template molecules. However...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1006/bioo.2001.1219

    authors： Gao S,Wang W,Wang B

    更新日期：2001-10-01 00:00:00

  • Design, synthesis, biological evaluation and molecular modeling of novel 1H-pyrrolo[2,3-b]pyridine derivatives as potential anti-tumor agents.

    abstract：:A class of 3-substituted 1H-pyrrolo[2,3-b]pyridine derivatives were designed, synthesized and evaluated for their in vitro biological activities against maternal embryonic leucine zipper kinase (MELK). Among these derivatives, the optimized compound 16h exhibited potent enzyme inhibition (IC50 = 32 nM) and excellent a...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103474

    authors： Wang R,Chen Y,Yang B,Yu S,Zhao X,Zhang C,Hao C,Zhao D,Cheng M

    更新日期：2020-01-01 00:00:00

  • Evaluation of thioamides, thiolactams and thioureas as hydrogen sulfide (H2S) donors for lowering blood pressure.

    abstract：:Hydrogen sulfide (H2S) is a biologically important gaseous molecule that exhibits promising protective effects against a variety of pathological processes. For example, it was recognized as a blood pressure lowering agent. Aligned with the need for easily modifiable platforms for the H2S supply, we report here the pre...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.102941

    authors： Zaorska E,Hutsch T,Gawryś-Kopczyńska M,Ostaszewski R,Ufnal M,Koszelewski D

    更新日期：2019-07-01 00:00:00

  • Facile synthesis and antimicrobial activity of CdS-Ag2S nanocomposites.

    abstract：:In this study CdS-Ag2S nanocomposites for antibacterial activity were synthesized via facile co-precipitation method using PVP as capping agent. The prepared nanocomposites have particle sizes in the range of 50-100 nm (SEM) and PVP addition has good influence on the morphology of nanocomposites. The antimicrobial act...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103064

    authors： Iqbal T,Ali F,Khalid NR,Tahir MB,Ijaz M

    更新日期：2019-09-01 00:00:00

  • Synthesis and in vitro antitumor activity of novel acylspermidine derivative N-(4-aminobutyl)-N-(3-aminopropyl)-8-hydroxy-dodecanamide (AAHD) against HepG2 cells.

    abstract：:Naturally occurring polyamines like Putrescine, Spermidine, and Spermine are polycations which bind to the DNA, hence stabilizing it and promoting the essential cellular processes. Many synthetic polyamine analogues have been synthesized in the past few years, which have shown cytotoxic effects on different tumours. I...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.102937

    authors： Al-Malki AL,Razvi SS,Mohammed FA,Zamzami MA,Choudhry H,Kumosani TA,Balamash KS,Alshubaily FA,ALGhamdi SA,Abualnaja KO,Abdulaal WH,Zeyadi MA,Al-Zahrani MH,Alhosin M,Asami T,Moselhy SS

    更新日期：2019-07-01 00:00:00

  • Synthesis and biological evaluation of new bis-indolone-N-oxides.

    abstract：:A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They d...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2013.03.001

    authors： Najahi E,Valentin A,Téné N,Treilhou M,Nepveu F

    更新日期：2013-06-01 00:00:00

  • Design, efficient synthesis, docking studies, and anticancer evaluation of new quinoxalines as potential intercalative Topo II inhibitors and apoptosis inducers.

    abstract：:As an extension for our earlier effort in the field of discovery of anticancer agents acting on DNA and Topo II, eighteen quinoxaline derivatives were designed and synthesized. Such members were designed to possess the main essential pharmacophoric features of DNA intercalators. The cytotoxic potential of the synthesi...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104255

    authors： Abbass EM,Khalil AK,Mohamed MM,Eissa IH,El-Naggar AM

    更新日期：2020-11-01 00:00:00