Functionalization of cantilever tips with nucleotides by the phosphoramidite method.

abstract：:Better control of postprandial hyperglycemia can be achieved by delaying the absorption of glucose resulting from carbohydrate digestion. Because α-amylase initiates the hydrolysis of polysaccharides, the design of α-amylase inhibitors can lead to the development of new treatments for metabolic disorders such as type ...

journal_title：ChemMedChem

authors： Al-Asri J,Gyémánt G,Fazekas E,Lehoczki G,Melzig MF,Wolber G,Mortier J

更新日期：2016-11-07 00:00:00

abstract：:N-Myristoyltransferase (NMT) is a cytosolic monomeric enzyme present in eukaryotes such as fungi and protozoa, but is not found in prokaryotes. The attachment of a 14-carbon saturated fatty acid, myristate, from myristoyl-CoA (14:0 CoA) to the N-terminal glycine residue in a specific set of cellular proteins is common...

journal_title：ChemMedChem

authors： Zhao C,Ma S

更新日期：2014-11-01 00:00:00

abstract：:Protein-protein and protein-carbohydrate interactions as a means to target the cell surface for therapeutic applications have been extensively investigated. However, carbohydrate-carbohydrate interactions (CCIs) have largely been overlooked. Here, we investigate the concept of CCI-mediated drug delivery. Lactose-funct...

journal_title：ChemMedChem

authors： Murthy RV,Bavireddi H,Gade M,Kikkeri R

更新日期：2015-05-01 00:00:00

abstract：:A novel Ru(II) (arene) theranostic complex is presented. It is based on a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid macrocycle bearing a triarylphosphine and can be tracked in vivo by using the γ emission of (153) Sm atoms. Notably, the heteroditopic ligand can be selectively metalated with ruthenium at...

journal_title：ChemMedChem

authors： Adriaenssens L,Liu Q,Chaux-Picquet F,Tasan S,Picquet M,Denat F,Le Gendre P,Marques F,Fernandes C,Mendes F,Gano L,Campello MP,Bodio E

更新日期：2014-07-01 00:00:00

abstract：:Bromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes, thereby regulating epigenetically controlled processes including ge...

journal_title：ChemMedChem

authors： Mirguet O,Lamotte Y,Chung CW,Bamborough P,Delannée D,Bouillot A,Gellibert F,Krysa G,Lewis A,Witherington J,Huet P,Dudit Y,Trottet L,Nicodeme E

更新日期：2014-03-01 00:00:00

abstract：:Here we report the synthesis of a number of compounds structurally related to arginine methyltransferase inhibitor 1 (AMI-1). The structural alterations that we made included: 1) the substitution of the sulfonic groups with the bioisosteric carboxylic groups; 2) the replacement of the ureidic function with a bis-amidi...

journal_title：ChemMedChem

authors： Castellano S,Milite C,Ragno R,Simeoni S,Mai A,Limongelli V,Novellino E,Bauer I,Brosch G,Spannhoff A,Cheng D,Bedford MT,Sbardella G

更新日期：2010-03-01 00:00:00

abstract：:Seasonal influenza infections are associated with an estimated 250-500 000 deaths annually. Resistance to the antiviral M2 ion-channel inhibitors has largely invalidated their clinical utility. Resistance to neuraminidase inhibitors has also been observed in several influenza A virus (IAV) strains. These data have pro...

journal_title：ChemMedChem

authors： Sagong HY,Bauman JD,Nogales A,Martínez-Sobrido L,Arnold E,LaVoie EJ

更新日期：2019-06-18 00:00:00

abstract：:The tubulin-binding mode of C3- and C15-modified analogues of epothilone A (Epo A) was determined by NMR spectroscopy and computational methods and compared with the existing structural models of tubulin-bound natural Epo A. Only minor differences were observed in the conformation of the macrocycle between Epo A and t...

journal_title：ChemMedChem

authors： Erdélyi M,Navarro-Vázquez A,Pfeiffer B,Kuzniewski CN,Felser A,Widmer T,Gertsch J,Pera B,Díaz JF,Altmann KH,Carlomagno T

更新日期：2010-06-07 00:00:00

abstract：:The NLRP3 inflammasome is an important regulator of the sterile inflammatory response, and its activation by host-derived sterile molecules leads to the intracellular activation of caspase-1, processing of the pro-inflammatory cytokines interleukin-1β (IL-1β)/IL-18, and pyroptotic cell death. Inappropriate activation ...

journal_title：ChemMedChem

authors： Baldwin AG,Tapia VS,Swanton T,White CS,Beswick JA,Brough D,Freeman S

更新日期：2018-02-20 00:00:00

abstract：:Although the advantages of sp3 -rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp2 -rich components. Compounds that are sp3 -rich are difficult to synthesize, and thus we aimed to invent an efficient method to construct sp3 -rich lib...

journal_title：ChemMedChem

authors： Karaki F,Umemoto S,Ashizawa K,Oki T,Sato N,Ogino T,Ishibashi N,Someya R,Miyano K,Hirayama S,Uezono Y,Fujii H

更新日期：2019-11-06 00:00:00

abstract：:Herbal medicines (HMs) are an important source of drugs. In this study, an efficient strategy integrating ultrafiltration LC-MS, microplate bioassays, and molecular docking was proposed to screen high-potency enzyme inhibitors from HMs. Using this strategy, the structure-activity relationships (SARs) including binding...

journal_title：ChemMedChem

authors： Song HP,Wang H,Liang JX,Qian C,Wu SQ,Xu WJ,Wu B,Liu XG,Li P,Yang H

更新日期：2016-12-06 00:00:00

abstract：:Targeting protein-protein interactions, such as the HIV-1 gp120-CD4 interface, has become a cutting-edge approach in the current drug discovery scenario. Many small molecules have been developed so far as inhibitors of the interaction between CD4 and HIV-1 gp120. However, due to a variety of reasons such as solubility...

journal_title：ChemMedChem

authors： Tintori C,Selvaraj M,Badia R,Clotet B,Esté JA,Botta M

更新日期：2013-03-01 00:00:00

abstract：:The histamine H1 G protein-coupled receptor (GPCR) plays an important role in allergy and inflammation. Existing drugs that address the H1 receptor differ in their chemical structure, pharmacology, and side effects. Light-controllable spatial and temporal activity regulation of photochromic H1 ligands may contribute t...

journal_title：ChemMedChem

authors： Rustler K,Pockes S,König B

更新日期：2019-03-22 00:00:00

abstract：:Plasmodium parasites kill 435 000 people around the world every year due to unavailable vaccines, a limited arsenal of antimalarial drugs, delayed treatment, and the reduced clinical effectiveness of current practices caused by drug resistance. Therefore, there is an urgent need to discover and develop new antiplasmod...

journal_title：ChemMedChem

authors： de Souza Pereira C,Costa Quadros H,Magalhaes Moreira DR,Castro W,Santos De Deus Da Silva RI,Botelho Pereira Soares M,Fontinha D,Prudêncio M,Schmitz V,Dos Santos HF,Gendrot M,Fonta I,Mosnier J,Pradines B,Navarro M

更新日期：2020-11-24 00:00:00

abstract：:A series of new dibenzoxepines were synthesized in a straightforward and efficient manner through diastereoselective biaryl Suzuki-Miyaura coupling and Brønsted-acid-mediated cyclodehydration as key steps. The vascular-disrupting potential of these molecules was evaluated with various in vitro assays: inhibition of mi...

journal_title：ChemMedChem

authors： Joncour A,Liu JM,Décor A,Thoret S,Wdzieczak-Bakala J,Bignon J,Baudoin O

更新日期：2008-11-01 00:00:00

abstract：:A novel class of isochroman dopamine analogues, originally reported by Abbott Laboratories, have >100-fold selectivity for D₁-like over D₂-like receptors. We synthesized a parallel series of chroman compounds and showed that repositioning the oxygen atom in the heterocyclic ring decreases potency and confers D₂-like r...

journal_title：ChemMedChem

authors： Bonner LA,Laban U,Chemel BR,Juncosa JI,Lill MA,Watts VJ,Nichols DE

更新日期：2011-06-06 00:00:00

abstract：:Members of the Eph receptor tyrosine kinase family play essential roles in the pathogenesis of cancer and are therefore promising candidates for molecular imaging by positron emission tomography (PET), for example. In this regard, radiochemical access to novel PET radiotracers derived from potent inhibitors that targe...

journal_title：ChemMedChem

authors： Mamat C,Mosch B,Neuber C,Köckerling M,Bergmann R,Pietzsch J

更新日期：2012-11-01 00:00:00

abstract：:β-Lactamases (BLs) are important antibiotic-resistance determinants that significantly compromise the efficacy of valuable β-lactam antibacterial drugs. Thus, combinations with BL inhibitor were developed. Avibactam is the first non-β-lactam BL inhibitor introduced into clinical practice. Ceftazidime-avibactam represe...

journal_title：ChemMedChem

authors： Pozzi C,Di Pisa F,De Luca F,Benvenuti M,Docquier JD,Mangani S

更新日期：2018-07-18 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin-4-one derivatives 8-22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5-(Furan-2-ylmethylene)-2-(4-nitrophen...

journal_title：ChemMedChem

authors： Patel AD,Pasha TY,Lunagariya P,Shah U,Bhambharoliya T,Tripathi RKP

更新日期：2020-07-03 00:00:00

abstract：:Over the years, a number of dimensionality reduction techniques have been proposed and used in chemoinformatics to perform nonlinear mappings. In this study, four representatives of nonlinear dimensionality reduction methods related to two different families were analyzed: distance-based approaches (Isomap and Diffusi...

journal_title：ChemMedChem

authors： Kireeva NV,Ovchinnikova SI,Tetko IV,Asiri AM,Balakin KV,Tsivadze AY

更新日期：2014-05-01 00:00:00

abstract：:Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series of twenty chalcones containing electron-donating and electron-wi...

journal_title：ChemMedChem

authors： Mathew B,Uçar G,Mathew GE,Mathew S,Kalatharakkal Purapurath P,Moolayil F,Mohan S,Varghese Gupta S

更新日期：2016-12-16 00:00:00

abstract：:Following the discovery of a type III allosteric modulator of cyclin-dependent kinase 2 (CDK2) characterized by a hexahydrocyclopenta[c]quinolone scaffold, three different series of its derivatives were synthesized and biologically evaluated. Docking of the synthesized compounds into the allosteric pocket of CDK2 allo...

journal_title：ChemMedChem

authors： Carlino L,Christodoulou MS,Restelli V,Caporuscio F,Foschi F,Semrau MS,Costanzi E,Tinivella A,Pinzi L,Lo Presti L,Battistutta R,Storici P,Broggini M,Passarella D,Rastelli G

更新日期：2018-12-20 00:00:00

abstract：:A screen of a focused kinase inhibitor library against Trypanosoma brucei rhodesiense led to the identification of seven series, totaling 121 compounds, which showed >50 % inhibition at 5 μm. Screening of these hits in a T. b. brucei proliferation assay highlighted three compounds with a 1H-imidazo[4,5-b]pyrazin-2(3H)...

journal_title：ChemMedChem

authors： Woodland A,Thompson S,Cleghorn LA,Norcross N,De Rycker M,Grimaldi R,Hallyburton I,Rao B,Norval S,Stojanovski L,Brun R,Kaiser M,Frearson JA,Gray DW,Wyatt PG,Read KD,Gilbert IH

更新日期：2015-11-01 00:00:00

abstract：:A small library of 17 organoruthenium compounds with the general formula [RuII (fcl)(chel)(L)]n+ (in which fcl=face capping ligand, chel=chelating bidentate ligand, and L=monodentate ligand) were screened for inhibitory activity against cholinesterases and glutathione-S-transferases of human and animal origins. Compou...

journal_title：ChemMedChem

authors： Ristovski S,Uzelac M,Kljun J,Lipec T,Uršič M,Zemljič Jokhadar Š,Žužek MC,Trobec T,Frangež R,Sepčić K,Turel I

更新日期：2018-10-22 00:00:00

abstract：:First reported in the late 1930s and partly explained in 1970, the antibacterial activity of pectin remained almost ignored until the late 1990s. The concomitant emergence of research on natural antibacterials and new usages of pectin polysaccharides, including those in medicine widely researched in Russia, has led to...

journal_title：ChemMedChem

authors： Ciriminna R,Fidalgo A,Meneguzzo F,Presentato A,Scurria A,Nuzzo D,Alduina R,Ilharco LM,Pagliaro M

更新日期：2020-08-28 00:00:00

abstract：:The in silico design, synthesis, and biological evaluation of ten potent type II dehydroquinase inhibitors are described. These compounds contain an anhydroquinate core, incorporated as a mimic of the enolate reaction intermediate. This substructure is attached by a variety of linking units to a terminal phenyl group ...

journal_title：ChemMedChem

authors： Payne RJ,Peyrot F,Kerbarh O,Abell AD,Abell C

更新日期：2007-07-01 00:00:00

abstract：:Metalloproteinases of the astacin family are drawing ever increasing attention as potential drug targets. However, knowledge regarding inhibitors thereof is limited in most cases. Crucial for the development of metalloprotease inhibitors is high selectivity, to avoid side effects brought about by inhibition of off-tar...

journal_title：ChemMedChem

authors： Tan K,Jäger C,Schlenzig D,Schilling S,Buchholz M,Ramsbeck D

更新日期：2018-08-20 00:00:00

abstract：:Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies an...

journal_title：ChemMedChem

authors： La Pensée L,Sabbani S,Sharma R,Bhamra I,Shore E,Chadwick AE,Berry NG,Firman J,Araujo NC,Cabral L,Cristiano ML,Bateman C,Janneh O,Gavrila A,Wu YH,Hussain A,Ward SA,Stocks PA,Cosstick R,O'Neill PM

更新日期：2013-05-01 00:00:00

abstract：:The protozoan parasite Plasmodium falciparum causes the most severe and prevailing form of malaria in sub-Saharan Africa. Previously, we identified the plasmodial lactate transporter, PfFNT, a member of the microbial formate-nitrite transporter family, as a novel antimalarial drug target. With the pentafluoro-3-hydrox...

journal_title：ChemMedChem

authors： Walloch P,Hansen C,Priegann T,Schade D,Beitz E

更新日期：2020-12-18 00:00:00

abstract：:The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to ...

journal_title：ChemMedChem

authors： Pellicciari R,Filosa R,Fulco MC,Marinozzi M,Macchiarulo A,Novak C,Natalini B,Hermit MB,Nielsen S,Sager TN,Stensbøl TB,Thomsen C

更新日期：2006-03-01 00:00:00