Highly selective cyclic peptide ligands for NeutrAvidin and avidin identified by phage display.

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：:Chemotherapy against human African trypanosomiasis relies on four drugs that cause frequent and occasionally severe side-effects. Because human African trypanosomiasis is a disease of poor people in Africa, the traditional market-driven pathways to drug development are not available. One potentially rapid and cost-eff...

journal_title：Chemical biology & drug design

authors： Mackey ZB,Baca AM,Mallari JP,Apsel B,Shelat A,Hansell EJ,Chiang PK,Wolff B,Guy KR,Williams J,McKerrow JH

更新日期：2006-05-01 00:00:00

abstract：:Alyteserin-2a (ILGKLLSTAAGLLSNL.NH2 ) stimulated the rate of insulin release from BRIN-BD11 clonalβ cells at a concentration of 30 nm (p < 0.05) with a response of 296 ± 26% of basal release at 3 μm (p < 0.001). The insulinotropic actions of analogs containing substitutions by l-lysine, d-lysine, or l-tryptophan at si...

journal_title：Chemical biology & drug design

authors： Ojo OO,Abdel-Wahab YH,Flatt PR,Conlon JM

更新日期：2013-08-01 00:00:00

abstract：:The screening of an in-house quinolones library against Mycobacterium tuberculosis (Mtb) H(37) Rv, followed by a first cycle of optimization, yielded 6-hydrogen-8-methyl derivatives endowed with good potency. The antitubercular activity also encompassed the bacteria in a non-replicating state (NRP-TB) with minimum inh...

journal_title：Chemical biology & drug design

authors： Tabarrini O,Sabatini S,Massari S,Pieroni M,Franzblau SG,Cecchetti V

更新日期：2012-11-01 00:00:00

abstract：:Based on the N-(phenethyl)azole backbone of azole antifungals, we designed 1-[(2-benzyloxy)phenyl]-2-(azol-1-yl)ethanone derivatives 2 and 3, containing benzyloxyphenyl scaffold of croconazole. Also these compounds can be considered as flexible analogs, resulted from C2-C3 disconnection of 3'-chloro-3-imidazolylflavan...

journal_title：Chemical biology & drug design

authors： Emami S,Kazemi-Najafabadi M,Pashangzadeh S,Foroumadi A,Faramarzi MA,Samadi N,Falahati M,Fateh R,Ashrafi-Khozani M

更新日期：2011-12-01 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：: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：:Transient receptor potential melastatin-2 (TRPM2) channel critical for monitoring internal body temperature is implicated in the pathological processes such as neurodegeneration. However, lacking selective and potent TRPM2 inhibitors impedes investigation and validation of the channel as a drug target. To discover nov...

journal_title：Chemical biology & drug design

authors： Luo X,Li M,Zhan K,Yang W,Zhang L,Wang K,Yu P,Zhang L

更新日期：2018-02-01 00:00:00

abstract：:Kinases are key targets for many of the pathological conditions. Inverse screening of ligands serves as an essential mode to identify potential kinase targets in modern drug discovery research. Hence, we intend to develop KinomeRun, a robust pipeline for inverse screening and kinome tree visualization through the seam...

journal_title：Chemical biology & drug design

authors： Ansar S,Vetrivel U

更新日期：2020-10-01 00:00:00

abstract：:A novel series of thiophene-containing biaryl amide glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, 14f and 14h, exhibited good GCGR binding (IC50  = 6.1 and 4.4 μm, respectively) and cAMP functional activities (IC50  = 4.4 and 14.4 μm, respectively). The possible bind...

journal_title：Chemical biology & drug design

authors： Li J,Feng Y,Li H,Shu S,Dai A,Cai X,Wang J,Yang D,Ma D,Wang MW,Liu H

更新日期：2018-07-01 00:00:00

abstract：:The facile synthesis of core-shell magnetic mesoporous silica nanoparticles (Fe3 O4 @mSiO2 NPs) was reported in aqueous phase using cetyltrimethylammonium bromide as a template under alcohol-free conditions. Compared to the conventional synthesis method for core-shell Fe3 O4 @mSiO2 NPs, the approach in this study is r...

journal_title：Chemical biology & drug design

authors： Shao D,Wang Z,Dong WF,Zhang X,Zheng X,Xiao XA,Wang YS,Zhao X,Zhang M,Li J,Huo QS,Chen L

更新日期：2015-12-01 00:00:00

abstract：:π-π interactions are common and important noncovalent interactions that contribute to biochemical molecular interactions, but the tools for the convenient 3D visualization of π-π interactions are lacking. We have developed an open-source and easy-to-use tool for the automated identification and display of π-π stacking...

journal_title：Chemical biology & drug design

authors： Liu Y,Ao X,Wang Q,Wang J,Ge H

更新日期：2018-10-01 00:00:00

abstract：:Ten new xanthone derivatives have been designed and synthesized for their potential antibacterial activity. All compounds have been screened against Staphylococcus epidermidis strains ATCC 12228 and clinical K/12/8915. The highest antibacterial activity was observed for compound 3: 5-chloro-2-((4-(2-hydroxyethyl)piper...

journal_title：Chemical biology & drug design

authors： Mazur G,Skiba-Kurek I,Karczewska E,Pańczyk-Straszak K,Jaworska J,Waszkielewicz AM

更新日期：2020-10-08 00:00:00

abstract：:Magnetic albumin nanospheres that incorporate doxorubicin (M-DOX-BSA-NPs) were prepared previously by our research group to develop magnetically responsive drug carrier system. This nanocarrier was synthesized as a drug delivery system for targeted chemotherapy. In this work, cytotoxic effects of doxorubicin (DOX)-loa...

journal_title：Chemical biology & drug design

authors： Zeybek A,Şanlı-Mohamed G,Ak G,Yılmaz H,Şanlıer ŞH

更新日期：2014-07-01 00:00:00

abstract：:The present paper is an attempt for unifying two different quinoxaline data sets with a wide range of substituents in 2, 3, 7, and 8 positions having excellent antitubercular activities with a view to developing robust and reliable structure-activity relationships. The merging has been performed for these two sets of ...

journal_title：Chemical biology & drug design

authors： Ghosh P,Vracko M,Chattopadhyay AK,Bagchi MC

更新日期：2008-08-01 00:00:00

abstract：:A diversity of novel 2-aryl-3-heteroaryl-2-ylmethyl-1,3-thiazolidin-4-ones were designed and synthesized by reacting heteroaryl-2-ylmethyl amine with various 2,6-dihalosubstituted benzaldehydes and mercaptoacetic acid. The title compounds were evaluated for human immunodeficiency virus type-1 (HIV-1) reverse transcrip...

journal_title：Chemical biology & drug design

authors： Rawal RK,Tripathi R,Kulkarni S,Paranjape R,Katti SB,Pannecouque C,De Clercq E

更新日期：2008-08-01 00:00:00

abstract：:For decades, biomedical and pharmaceutical researchers have worked to devise new and more effective therapeutics to treat diseases affecting the central nervous system. The blood-brain barrier effectively protects the brain, but poses a profound challenge to drug delivery across this barrier. Many traditional drugs ca...

journal_title：Chemical biology & drug design

authors： Stockwell J,Abdi N,Lu X,Maheshwari O,Taghibiglou C

更新日期：2014-05-01 00:00:00

abstract：:Zinc containing peptidases are widely distributed in nature and have important roles in many physiological processes. M4 family comprises numerous zinc-dependent metallopeptidases that hydrolyze peptide bonds. A large number of these enzymes are implicated as virulence factors of the microorganisms that produce them a...

journal_title：Chemical biology & drug design

authors： Adekoya OA,Sylte I

更新日期：2009-01-01 00:00:00

abstract：:The novel naphthoquinone adduct 12,13-Dihydro-N-methyl-6,11,13-trioxo-5H-benzo[4,5]cyclohepta[1,2-b]naphthalen-5,12-imine (hereafter called TU100) was synthesized as a potential chemotherapeutic agent. TU100 arrests tissue culture cells in S and G2/M phases of the cell cycle, followed by rapid induction of apoptosis. ...

journal_title：Chemical biology & drug design

authors： Carvajal D,Kennedy S,Boustani A,Lazar M,Nguyen S,DiCesare JC,Sheaff RJ

更新日期：2011-11-01 00:00:00

abstract：:EGFR is a well-established therapeutic target of clinical relevance in cancer. However, acquisition of secondary mutation (T790M) makes first-generation inhibitors ineffective. Therefore, to circumvent the problem of resistance, new T790M/L858R (TMLR) double mutant inhibitors are required. In this study, fragment-base...

journal_title：Chemical biology & drug design

authors： Fatima S,Pal D,Agarwal SM

更新日期：2019-07-01 00:00:00

abstract：:As the most common primary malignant brain tumors, gliomas cause more years of life lost than do any other tumors. Recently, abnormalities of the eukaryotic initiation factors (EIFs) have been reported in gliomas. Yet the role of EIF3D, which encodes a subunit of EIF3 multiprotein complex, remains poorly understood. I...

journal_title：Chemical biology & drug design

authors： Ren M,Zhou C,Liang H,Wang X,Xu L

更新日期：2015-10-01 00:00:00

abstract：:The unfolded protein response (UPR) is a coordinated program that promotes cell survival under conditions of endoplasmic reticulum stress and is required in tumor progression as well. To date, no specific small molecule inhibitor targeting this pathway has been identified. Pancreatic endoplasmic reticulum kinase (PERK...

journal_title：Chemical biology & drug design

authors： Wang H,Blais J,Ron D,Cardozo T

更新日期：2010-12-01 00:00:00

abstract：:A new series of 3-benzoylamino-5-(1H-imidazol-4-yl)methylaminobenzo[b]furans were synthesized and screened as antitumor agents. As a general trend, tested compounds showed concentration-dependent antiproliferative activity against HeLa and MCF-7 cancer cell lines, exhibiting GI50 values in the low micromolar range. In...

journal_title：Chemical biology & drug design

authors： Lauria A,Gentile C,Mingoia F,Palumbo Piccionello A,Bartolotta R,Delisi R,Buscemi S,Martorana A

更新日期：2018-01-01 00:00:00

abstract：:New imines, derived from aromatic aldehyde, chalcones and 5-amino-1,3,4-thiadiazole-2-thiol exhibited promising anti-convulsant activity which is explained through chemo-biological interactions at receptor site producing the inhibition of human Carbonic Anhydrase-II enzyme (hCA-II) through the proposed pharmacophore m...

journal_title：Chemical biology & drug design

authors： Yusuf M,Khan RA,Khan M,Ahmed B

更新日期：2013-05-01 00:00:00

abstract：:The activation mechanism of G-protein-coupled receptors triggered upon binding of a ligand represents a very important 'conformational switch' in the biological array of signal transduction. However, the molecular and functional details for this activation switch remain unknown. Random saturation mutagenesis data on t...

journal_title：Chemical biology & drug design

authors： Sen S,Baranski TJ,Nikiforovich GV

更新日期：2008-03-01 00:00:00

abstract：:Utilizing atypical wake-promoting agent modafinil (inactive in both rH(3) and hH(3) binding assays) as a launching pad, a series of sulfinyl- and sulfone-derived H(3) receptor inverse agonists were developed. Brain-permeable compound 27, a potent member of the series displayed excellent selectivity against related fam...

journal_title：Chemical biology & drug design

authors： Dunn D,Raddatz R,Ator MA,Bacon ER,Chatterjee S

更新日期：2013-03-01 00:00:00

abstract：:The cationic glycolipid IAXO-102, a potent TLR4 antagonist targeting both MD-2 and CD14 co-receptors, has been used as scaffold to design new potential TLR4 modulators and fluorescent labels for the TLR4 receptor complex (membrane TLR4.MD-2 dimer and CD14). The primary amino group of IAXO-102, not involved in direct i...

journal_title：Chemical biology & drug design

authors： Ciaramelli C,Calabrese V,Sestito SE,Pérez-Regidor L,Klett J,Oblak A,Jerala R,Piazza M,Martín-Santamaría S,Peri F

更新日期：2016-08-01 00:00:00

abstract：:Tuberculosis is the second leading infectious killer with 9 million new cases in 2009. Extensive use of pathogen's lipid metabolism especially in utilizing the host lipids and virulence highlights the importance of exported lipid-catabolizing enzymes. Current study aims to emphasize the importance of Rv0183, an export...

journal_title：Chemical biology & drug design

authors： Saravanan P,Dubey VK,Patra S

更新日期：2012-06-01 00:00:00

abstract：:The new series of asymmetrical pyrazole curcumin analogues 4a-g were synthesized by using polyethylene glycol (PEG-400) as a green reaction medium and evaluated for their in vivo analgesic and in vitro antioxidant (H2 O2 , DPPH, Ferrous reducing power and Nitric oxide scavenging activity) and anti-inflammatory activit...

journal_title：Chemical biology & drug design

authors： Jadhav SY,Bhosale RB,Shirame SP,Patil SB,Kulkarni SD

更新日期：2015-03-01 00:00:00

abstract：:Hydrophobization of proteins, such as chemical acylation, has been recognized as an efficient method for improving their membrane permeability. In this research, chicken cystatin, a model protein inhibitor of cysteine proteinases, was acylated with fatty acyl residues of 6-18 carbon atoms. The chemical modification wa...

journal_title：Chemical biology & drug design

authors： Kocevar N,Obermajer N,Kreft S

更新日期：2008-09-01 00:00:00