Abstract:
:This work presents the first use of yeast-displayed protein targets for screening mRNA-display libraries of cyclic and linear peptides. The WW domains of Yes-Associated Protein 1 (WW-YAP) and mitochondrial import receptor subunit TOM22 were adopted as protein targets. Yeast cells displaying WW-YAP or TOM22 were magnetized with iron oxide nanoparticles to enable the isolation of target-binding mRNA-peptide fusions. Equilibrium adsorption studies were conducted to estimate the binding affinity (KD) of select WW-YAP-binding peptides: KD values of 37 and 4 μM were obtained for cyclo[M-AFRLC-K] and its linear cognate, and 40 and 3 μM for cyclo[M-LDFVNHRSRG-K] and its linear cognate, respectively. TOM22-binding peptide cyclo[M-PELNRAI-K] was conjugated to magnetic beads and incubated with yeast cells expressing TOM22 and luciferase. A luciferase-based assay showed a 4.5-fold higher binding of TOM22+ yeast compared to control cells. This work demonstrates that integrating mRNA- and yeast-display accelerates the discovery of peptide ligands.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Bacon K,Bowen J,Reese H,Rao BM,Menegatti Sdoi
10.1021/acscombsci.0c00171subject
Has Abstractpub_date
2020-12-14 00:00:00pages
738-744issue
12eissn
2156-8952issn
2156-8944journal_volume
22pub_type
杂志文章abstract::The reactions of vinyl malononitriles with 3-phenacylideneoxindoles in ethanol in the presence of DBU as base resulted in the functionalized spirocyclic oxindoles through the domino Michael addition and intramolecular nucleophilic addition to cyano group. On the other hand, the similar reaction in the presence of pipe...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500006c
更新日期:2014-06-09 00:00:00
abstract::An efficient and straightforward synthetic protocol has been developed for the diversity-oriented synthesis of highly functionalized piperidines containing a Meldrum's acid moiety via pseudo five-component reaction between aromatic aldehydes, ammonium acetate, substituted β-nitrostyrenes and Meldrum's acid for the gen...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co4001502
更新日期:2014-03-10 00:00:00
abstract::A sequential single-flask multicomponent reactions is highly effective for the synthesis of 1,2-dihydroisoquinolines through amidealkylation from intermediate N-acylisoquinolinium salts under mild conditions. N-Acylisoquinolinium ions and trichloromethyl-1-(1H-indol-3-yl)isoquinoline-2(1H)-carboxylate have demonstrate...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00001
更新日期:2015-08-10 00:00:00
abstract::An expedient and metal-free synthetic protocol for construction of substituted quinolines has been developed from anilines and phenylacetaldehydes using imidazolium cation-based ionic liquids as the reaction medium. Mechanistic analysis indicated that the reaction occurs through C-C and C-N bond formation to produce i...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500047w
更新日期:2014-11-10 00:00:00
abstract::A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, while the same reaction afforded 3-cyano-benzopyrrolo-imidazoles ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00052
更新日期:2017-07-10 00:00:00
abstract::In this research, MgAl-CO32- nanolayered double hydroxide (NLDH) was synthesized through a facile coprecipitation method, followed by a hydrothermal treatment. The prepared NLDHs were used as a hydrophilic nanofiller for improving the performance of the PVDF-based ultrafiltration membranes. The main objective of this ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00046
更新日期:2017-07-10 00:00:00
abstract::A three-component reaction of a 2-aminoazine, a 2-oxoaldehyde, and a cyclic 1,3-dicarbonyl compound providing access toward a novel class of imidazo[1,2-a]azine derivatives was developed and studied. The scope of the process was thoroughly explored under three different reaction conditions resulting in the generation ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co5000695
更新日期:2014-10-13 00:00:00
abstract::Magnetization using cheap and minimally toxic materials, such as iron oxide nanoparticles can enable easy separation of cells from culture medium and is relevant to several industrial applications. Here, we show that cell surface expression of a mutant protein that binds iron oxide can enable efficient magnetization o...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.8b00084
更新日期:2018-10-08 00:00:00
abstract::A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazo...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co2001839
更新日期:2012-04-09 00:00:00
abstract::In view of the variety and complexity of thermoelectric (TE) material systems, combinatorial approaches to materials development come to the fore for identifying new promising compounds. The success of this approach is related to the availability and reliability of high-throughput characterization methods for identify...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00019
更新日期:2018-01-08 00:00:00
abstract::A microgradient-heater (MGH) was developed, and its feasibility as a tool for high-throughput materials science experimentation was tested. The MGH is derived from microhot plate (MHP) systems and allows combinatorial thermal processing on the micronano scale. The temperature gradient is adjustable by the substrate ma...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co3000488
更新日期:2012-10-08 00:00:00
abstract::A novel parallel medicinal chemistry (PMC)-enabled synthesis of 1H-pyrazolo[3,4-d]pyrimidines employing condensation of easily accessible N-pyrazolylamides and nitriles has been developed. The presented studies describe singleton and library enablements that allowed rapid generation of molecular diversity to examine C...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00116
更新日期:2017-11-13 00:00:00
abstract::High-throughput experimentation provides efficient mapping of composition-property relationships, and its implementation for the discovery of optical materials enables advancements in solar energy and other technologies. In a high throughput pipeline, automated data processing algorithms are often required to match ex...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00053
更新日期:2016-11-14 00:00:00
abstract::Applications of silica-ROMP reagents in a one-pot, sequential protocol have been developed for the synthesis of a variety of diverse benzoxathiazepine 1,1-dioxides. This protocol includes sulfonylation, intramolecular SNAr, alkylation with silica-supported oligomeric benzyl (Si-OBPn) and triazole (Si-OTPn) phosphates,...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00041
更新日期:2016-07-11 00:00:00
abstract::In this article, an original one-pot method is utilized to synthesize a variety of derivatives of naphtho[2,1-b]furan-2(1H)-one via a pseudo-four-component domino reaction of aryl aldehydes, acetic anhydride, hippuric acids, and 2-naphthols catalyzed by HSW@SPIONs. This reaction illustrates an array of attractive feat...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00018
更新日期:2015-08-10 00:00:00
abstract::Fourteen (hetero-)(arylidene)arylhydrazide derivatives (ABH1-ABH14) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound ABH5 most potently inhibited MAO-B with an IC50 value of 0.025 ± 0.0019 μM; ABH2 and ABH3 exhibited high IC50 ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.0c00136
更新日期:2020-11-09 00:00:00
abstract::For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co200090p
更新日期:2011-09-12 00:00:00
abstract::A combinatorial library having 66 different ternary compositions of Pd-Ir-Ce was prepared via the impregnation method to find the optimum ternary composition with the highest performance toward oxygen reduction reaction (ORR) in acid media. Its performance in ORR activity of the combinatorial array was evaluated throu...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co400008v
更新日期:2013-11-11 00:00:00
abstract::The possibility of band gap engineering in graphene opens countless new opportunities for application in nanoelectronics. In this work, the energy gaps of 622 computationally optimized graphene nanoflakes were mapped to topological autocorrelation vectors using machine learning techniques. Machine learning modeling re...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00094
更新日期:2016-11-14 00:00:00
abstract::Ultrasound-assisted synthesis of benzimidazo[2,1-b]quinazolin-1(1H)-ones was achieved via piperidine-catalyzed three-component reaction of 2-aminobenzimidazoles, an aromatic aldehyde, and 1,3-dione in aqueous isopropanol. This mechanism was first suspected following our identification of unusual reaction intermediates...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00186
更新日期:2016-03-14 00:00:00
abstract::Combinatorial synthesis of Li-ion batteries has proven extremely powerful in screening complex compositional spaces for next-generation materials. To date, no Na-ion counterpart exists wherein Na-ion cathodes can be synthesized in such a way to be comparable to that obtained in bulk synthesis. Herein, we develop a syn...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.9b00181
更新日期:2020-06-08 00:00:00
abstract::Under the acidic conditions, substituted furans were constructed from γ-alkynyl ketones through corresponding allene intermediates in one-pot. The methodology was also tailored to a series of the Ugi reaction products for the synthesis of 6-methylpyrazin-2(1 H)-one derivatives. The current method offered significant a...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.8b00005
更新日期:2018-05-14 00:00:00
abstract::A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, α-hydroxy aldehydes, and boronic acids, which undergo Petasis 3-component reactions (coup...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500091f
更新日期:2015-01-12 00:00:00
abstract::We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional β-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of soph...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co400003d
更新日期:2013-04-08 00:00:00
abstract::Individually, benzoxazole and triazole moieties are of significant biological interest owing to their importance in drugs and pharmaceuticals. To assess their combined biological impact when woven into one molecule, we designed a novel, regioselective, multicomponent, one-pot (MCOP) approach for the construction of be...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500135z
更新日期:2015-01-12 00:00:00
abstract::A one-pot parallel synthesis of N(1)-aryl-N(2)-alkyl-substituted oxamides with 2,2,2-trifluoroethyl chlorooxoacetate was developed. The synthesis of a library of 45 oxamides revealed higher efficiency of this reagent over the known ethyl chlorooxoacetate. The reagent was successfully used to prepare the known oxamide-...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00091
更新日期:2015-10-12 00:00:00
abstract::An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 μ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00010
更新日期:2016-05-09 00:00:00
abstract::Dispiro-pyrrolidino/pyrrolizidino fused oxindoles/acenaphthoquinones have been derived from andrographolide via azomethine ylide cycloaddition to the conjugated double-bond under microwave (MW) irradiation. The reactions are chemo-, stereo-, and regioselective in nature. Change in amino acid from sarcosine/N-benzyl gl...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co3001154
更新日期:2013-01-14 00:00:00
abstract::A potentiometric Pb(II)-selective sensor was fabricated by a combinatorial screening of electrically conducting polysulfoaminoanthraquinone (PSA) nanoparticles as a solid ionophore, ion exchangers (oleic acid (OA) and NaTPB), plasticizers in a polyvinyl chloride (PVC) matrix, membrane thickness, inner filling ion spec...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co400140g
更新日期:2014-03-10 00:00:00
abstract::This is a report on the early years of combinatorial materials science and technology. High-throughput technologies (HTTs) are found in life- and materials-science laboratories. Although HTTs have long been the standard in life sciences in academia as well as in industry, HTTs in materials science have become the stan...
journal_title:ACS combinatorial science
pub_type: 历史文章,杂志文章,评审
doi:10.1021/acscombsci.8b00189
更新日期:2019-06-10 00:00:00