In vitro interaction of glutathione S-transferase-pi enzyme with glutathione-coated silver sulfide quantum dots: A novel method for biodetection of glutathione S-transferase enzyme.

abstract：:Structure-activity relationship (SAR) studies are essential in the generation of peptides with enhanced activity and efficacy as therapeutic agents. In this study, we report a Structure-activity relationship study for a family of mimetic peptides derived from type IV collagen with potent anti-angiogenic properties. Th...

journal_title：Chemical biology & drug design

authors： Rosca EV,Koskimaki JE,Pandey NB,Tamiz AP,Popel AS

更新日期：2012-07-01 00:00:00

abstract：:This work presents synthesis and antimicrobial evaluation of nineteen 6-alkylamino-N-phenylpyrazine-2-carboxamides. Antimycobacterial activity was determined against Mycobacterium tuberculosis H37Rv, M. kansasii and two strains of M. avium. Generally, the antimycobacterial activity increased with prolongation of simpl...

journal_title：Chemical biology & drug design

authors： Servusova-Vanaskova B,Paterova P,Garaj V,Mandikova J,Kunes J,Naesens L,Jílek P,Dolezal M,Zitko J

更新日期：2015-10-01 00:00:00

abstract：:Methionine aminopeptidase 1 (MetAP1) is a target for drug discovery against many adversaries and a potential antileishmanial target for its role in N-terminal methionine processing. As an effort towards new inhibitor discovery against methionine aminopeptidase 1 from Leishmania donovani (LdMetAP1), we have synthesized...

journal_title：Chemical biology & drug design

authors： Bhat SY,Bhandari S,Thacker PS,Arifuddin M,Qureshi IA

更新日期：2021-02-01 00:00:00

abstract：:Benzimidazole and their metal analogs that can act as multimodal agent and have non-peptidic CCK-B receptor antagonist were synthesized and characterized on the basis of spectroscopic techniques such as FT-IR, NMR, FAB-MS and also evaluated for biologic efficacy. The ligands showed binding to most of the organs, known...

journal_title：Chemical biology & drug design

authors： Agrawal S,Bhatnagar RR,Tiwari A,Srivastava R,Sharma U

更新日期：2013-11-01 00:00:00

abstract：:A cholesteryl-functionalized derivative of activity dependent neurotrophic factor-9 peptide (a nine amino acid core peptide of activity-dependent neurotrophic factor, acting against Alzheimer's disease) was synthesized aiming at the improvement of its bioavailability. Therefore, its uptake was comparatively investigat...

journal_title：Chemical biology & drug design

authors： Katsari E,Zikos C,Tziveleka LA,Paravatou-Petsotas M,Paleos CM

更新日期：2012-07-01 00:00:00

abstract：:Protein modification can have far-reaching effects. NEDDylation, a protein modification process with the protein NEDD8, stabilizes and modifies how the targeted protein interacts with other proteins. Its role in system regulation makes it a prime therapeutic target, and virtual high-throughput screening has already id...

journal_title：Chemical biology & drug design

authors： Chen JJ,Schmucker LN,Visco DP Jr

更新日期：2019-04-01 00:00:00

abstract：:Photodynamic therapy (PDT) uses non-toxic dyes called photosensitizers (PS) and harmless visible light that combine to form highly toxic reactive oxygen species that kill cells. Originally, a cancer therapy, PDT, now includes applications for infections. The most widely studied PS are tetrapyrrole macrocycles includin...

journal_title：Chemical biology & drug design

authors： Martinez De Pinillos Bayona A,Mroz P,Thunshelle C,Hamblin MR

更新日期：2017-02-01 00:00:00

abstract：:Specific assembly of ribonucleoprotein complexes is essential in controlling various cellular functions including gene regulation. Diverse scaffolds containing proteins or nucleic acids could play key roles in stabilizing specific ribonucleoprotein complexes by enhancing protein-protein or RNA-protein interactions. On...

journal_title：Chemical biology & drug design

authors： Chiu YL,Cao H,Rana TM

更新日期：2007-04-01 00:00:00

abstract：:Microsomal prostaglandin E synthase-1 (mPGES-1) is the key enzyme for prostaglandin E2 (PGE2) generation during inflammation and is a potential target for designing anti-inflammatory drugs. Potential inhibitors of m-PGES-1 were selected from traditional Chinese medicine (TCM Database@Taiwan) based on the pharmacophore...

journal_title：Chemical biology & drug design

authors： Chen KC,Sun MF,Yang SC,Chang SS,Chen HY,Tsai FJ,Chen CY

更新日期：2011-10-01 00:00:00

abstract：:Smooth muscle cell (SMC) proliferation has been accepted as a common event in the pathophysiology of vascular diseases, including atherogenesis and intimal hyperplasia. Delivery of the nitric oxide synthase (NOS) substrate l-arginine, pharmacological nitric oxide (NO) donors, NO gas or overexpression of NOS proteins c...

journal_title：Chemical biology & drug design

authors： Yu H,Payne TJ,Mohanty DK

更新日期：2011-10-01 00:00:00

abstract：:Currently, a popular strategy for designing novel radioprobes as bone-imaging agents is based on the concept of bifunctional radiopharmaceuticals. Considering the dithiocarbamate ligand can act as a suitable bifunctional linking agent to attach technetium-99m (99m Tc) to corresponding target molecules, in this study, ...

journal_title：Chemical biology & drug design

authors： Song X,Wang Y,Zhang J,Jin Z,Zhang W,Zhang Y

更新日期：2018-02-01 00:00:00

abstract：:Two series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted benzylpiperazine moieties have been synthesized and evaluated for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. The majority of the derivativ...

journal_title：Chemical biology & drug design

authors： Wu Y,Sun LP,Ma LX,Che J,Song MX,Cui X,Piao HR

更新日期：2013-05-01 00:00:00

abstract：:The ability of Archaea to adapt their membrane lipid compositions to extreme environments has brought in archaeosomes into consideration for the development of drug delivery systems overcoming the physical, biological blockades that the body exhibits against drug therapies. In this study, we prepared unilamellar archa...

journal_title：Chemical biology & drug design

authors： Attar A,Bakir C,Yuce-Dursun B,Demir S,Cakmakci E,Danis O,Birbir M,Ogan A

更新日期：2018-01-01 00:00:00

abstract：:Electron transport and respiratory pathways are active in both latent and rapidly growing mycobacteria and remain conserved in all mycobacterial species. In mycobacteria, menaquinone is the sole electron carrier responsible for electron transport. Menaquinone biosynthesis pathway is found to be essential for the growt...

journal_title：Chemical biology & drug design

authors： Mathew R,Kruthiventi AK,Prasad JV,Kumar SP,Srinu G,Chatterji D

更新日期：2010-07-01 00:00:00

abstract：:Human DNA methyltransferase1 (hDNMT1) is responsible for preserving DNA methylation patterns that play important regulatory roles in differentiation and development. Misregulation of DNA methylation has thus been linked to many syndromes, life style diseases, and cancers. Developing specific inhibitors of hDNMT1 is an...

journal_title：Chemical biology & drug design

authors： Joshi M,Rajpathak SN,Narwade SC,Deobagkar D

更新日期：2016-07-01 00:00:00

abstract：:A new series of fluoroquinolone-based benzothiazolyl-4-thiazolidinone hybrids has been yielded via sulfated tungstate-promoted highly accelerated N-formylation at a piperazine residue of ciprofloxacin and norfloxacin entities. The formylated fluoroquinolone moieties were then coupled with substituted 2-aminobenzothiaz...

journal_title：Chemical biology & drug design

authors： Patel RV,Park SW

更新日期：2014-07-01 00:00:00

abstract：:Malaria, mainly caused by Plasmodium falciparum and Plasmodium vivax, has been a growing cause of morbidity and mortality. P. falciparum is more lethal than is P. vivax, but there is a vital need for effective drugs against both species. Geranylgeranyl diphosphate synthase (GGPPS) is an enzyme involved in the biosynth...

journal_title：Chemical biology & drug design

authors： Venkatramani A,Gravina Ricci C,Oldfield E,McCammon JA

更新日期：2018-06-01 00:00:00

abstract：:In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)acetamides were synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit heart p...

journal_title：Chemical biology & drug design

authors： Ye BJ,Liu XK,Jiang SM,Cui X,Piao HR

更新日期：2011-01-01 00:00:00

abstract：:The cytochrome P450 isozyme CYP2D6 binds a large variety of drugs, oxidizing many of them, and plays a crucial role in establishing in vivo drug levels, especially in multidrug regimens. The current study aimed to develop reliable predictive models for estimating the CYP2D6 inhibition properties of drug candidates. Qu...

journal_title：Chemical biology & drug design

authors： Saraceno M,Massarelli I,Imbriani M,James TL,Bianucci AM

更新日期：2011-08-01 00:00:00

abstract：:PCSK9, a member of the proprotein convertase family, is a key negative regulator of hepatic low-density lipoprotein receptor (LDLR) concentrations in the blood plasma and is associated with the risk of coronary artery disease (CAD). Peptide inhibitors designed to block PCSK9-LDLR interactions could reduce the risk of ...

journal_title：Chemical biology & drug design

authors： Pasam B,Medicherla KM,Rathore RS,Upadhyayula RS

更新日期：2019-12-01 00:00:00

abstract：:The design, synthesis and utility of fluorescence probes that bind to the DFG-out conformation of p38alpha kinase are described. Probes that demonstrate good affinity for p38alpha, have been identified and one of the probes, PF-04438255, has been successfully used in an high throughput screening (HTS) assay to identif...

journal_title：Chemical biology & drug design

authors： Tecle H,Feru F,Liu H,Kuhn C,Rennie G,Morris M,Shao J,Cheng AC,Gikunju D,Miret J,Coli R,Xi SH,Clugston SL,Low S,Kazmirski S,Ding YH,Cao Q,Johnson TL,Deshmukh GD,DiNitto JP,Wu JC,English JM

更新日期：2009-12-01 00:00:00

abstract：:The non-receptor Src tyrosine kinase is known to cooperate with the epidermal growth factor receptor in a mechanism leading to invasion and metastasis of solid tumours. With the purpose of developing agents targeted to both epidermal growth factor receptor and Src or related kinases, we embarked on the design of chime...

journal_title：Chemical biology & drug design

authors： Barchéchath S,Williams C,Saade K,Lauwagie S,Jean-Claude B

更新日期：2009-04-01 00:00:00

abstract：:Alzheimer's disease onset and progression are associated with the dysregulation of multiple and complex physiological processes, and a successful therapeutic approach should therefore address more than one target. In line with this modern paradigm, a series of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene analogs (4a-q) w...

journal_title：Chemical biology & drug design

authors： Shaik JB,Palaka BK,Penumala M,Eadlapalli S,Darla Mark M,Ampasala DR,Vadde R,Amooru Gangaiah D

更新日期：2016-07-01 00:00:00

abstract：:Synthesis of new series of 1,2,4-triazole with 1,2,3-triazole and piperidine ring using ZrOCl(2) ·8H(2) O as a catalyst in ethanol has been described. The yields obtained are in the range of 80-85%. All the synthesized compounds (3a-3o) are novel and were evaluated for their in vitro antifungal activities using standa...

journal_title：Chemical biology & drug design

authors： Sangshetti JN,Lokwani DK,Sarkate AP,Shinde DB

更新日期：2011-11-01 00:00:00

abstract：:Dimethoxycurcumin (Dimc), a synthetic analogue of curcumin, that has been reported to exhibit better in vivo stability and anti-tumour activity, was investigated for its interaction with DNA, employing spectroscopic methods based on absorption, fluorescence, circular dichroism (CD), ethidium bromide (EtBr) competitive...

journal_title：Chemical biology & drug design

authors： Kunwar A,Simon E,Singh U,Chittela RK,Sharma D,Sandur SK,Priyadarsini IK

更新日期：2011-04-01 00:00:00

abstract：:Phosphodiesterase 11 (PDE11) is the latest isoform of the PDEs family to be identified, acting on both cyclic adenosine monophosphate and cyclic guanosine monophosphate. The initial reports of PDE11 found evidence for PDE11 expression in skeletal muscle, prostate, testis, and salivary glands; however, the tissue distr...

journal_title：Chemical biology & drug design

authors： Cichero E,D'Ursi P,Moscatelli M,Bruno O,Orro A,Rotolo C,Milanesi L,Fossa P

更新日期：2013-12-01 00:00:00

abstract：:The present study describes ligand-based pharmacophore modeling of a series of structurally diverse acyl coenzyme A cholesterol acyltransferase inhibitors. Quantitative pharmacophore models were generated using HypoGen module of Discovery Studio 2.1, whereby the best pharmacophore model possessing two hydrophobic, one...

journal_title：Chemical biology & drug design

authors： Chhabria MT,Brahmkshatriya PS,Mahajan BM,Darji UB,Shah GB

更新日期：2012-07-01 00:00:00

abstract：:Follicle-stimulating hormone is important for mammalian reproduction. It acts through specific receptors located on the plasma membrane of granulosa cells in ovaries and Sertoli cells in testes. The binding of follicle-stimulating hormone to its receptor activates intracytoplasmic signaling pathways leading to steroid...

journal_title：Chemical biology & drug design

authors： Navalakhe RM,Jagtap DD,Nayak SU,Nandedkar TD,Mahale SD

更新日期：2013-08-01 00:00:00

abstract：:Spiropyrans have been extensively investigated because of their thermo- and photochromic characteristics, but their biotherapeutic properties have not been explored much. We report anti-proliferative properties of a novel 3,3'-azadimethylene dinaphthospiropyran 11. Dibenzospiropyrans and dinaphthospiropyrans were synt...

journal_title：Chemical biology & drug design

authors： Lagisetty P,Eeda V,Yadav VR,Nimmo SL,Subramaniam D,Powell DR,Awasthi V

更新日期：2021-02-01 00:00:00

abstract：:STAT3 is attractive target for development of anti-cancer therapeutics as it is implicated in nearly all forms of human tumors. To identify novel leads, we screened a combinatorial peptide library displayed on the surface of M13 bacteriophage. After three rounds of biopanning, a dodecapeptide with the YYVSWPPDMMHY seq...

journal_title：Chemical biology & drug design

authors： Ambaye ND,Yu HE

更新日期：2021-01-01 00:00:00