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Themed collection Chemical Biology

28 items
Communication

A cationic ZnII porphyrazine induces a stable parallel G-quadruplex conformation in human telomeric DNA

A water soluble octacationic ZnII porhyrazine macrocycle drives the conformational equilibrium of the G-quadruplex of a human telomeric sequence exclusively towards a parallel conformation upon complexation.

Graphical abstract: A cationic ZnII porphyrazine induces a stable parallel G-quadruplex conformation in human telomeric DNA
From the themed collection: Chemical Biology
Communication

“Click-made” biaryl-linker improving efficiency in protein labelling for the membrane target protein of a bioactive compound

The design, synthesis and assessment of a novel biaryl-linked (BArL) molecular probe for the exploration of low-abundant target proteins for bioactive metabolites is reported

Graphical abstract: “Click-made” biaryl-linker improving efficiency in protein labelling for the membrane target protein of a bioactive compound
From the themed collection: Chemical Biology
Communication

Design and synthesis of nonpeptidic, small molecule inhibitors for the Mycobacterium tuberculosis protein tyrosine phosphatase PtpB

The design and synthesis of small molecules with low micromolar inhibition of Mycobacterium tuberculosis protein tyrosine phosphatase PtpB is described.

Graphical abstract: Design and synthesis of nonpeptidic, small molecule inhibitors for the Mycobacterium tuberculosis protein tyrosine phosphatase PtpB
From the themed collection: Chemical Biology
Paper

trans,trans-2,4-Hexadiene incorporation on enzymes for site-specific immobilization and fluorescent labeling

Chemical incorporation of a hexadiene moiety on an enzyme molecule permitted protein immobilization and site-specific labeling with NBD fluorophore by Diels–Alder reaction.

Graphical abstract: trans,trans-2,4-Hexadiene incorporation on enzymes for site-specific immobilization and fluorescent labeling
From the themed collection: Chemical Biology
Paper

Rapid synthesis and zebrafish evaluation of a phenanthridine-based small molecule library

A phenanthridine-based small molecule library was rapidly assembled using Heck methodology; library evaluation identified a novel inhibitor of early-stage zebrafish embryo development.

Graphical abstract: Rapid synthesis and zebrafish evaluation of a phenanthridine-based small molecule library
From the themed collection: Chemical Biology
Paper

Blue fluorescent dye-protein complexes based on fluorogenic cyanine dyes and single chain antibody fragments

Dye-protein complexes that emit intense blue fluorescence have been created from fluorogenic cyanine dyes and single chain antibody fragments.

Graphical abstract: Blue fluorescent dye-protein complexes based on fluorogenic cyanine dyes and single chain antibody fragments
From the themed collection: Chemical Biology
Paper

Alkyl sulfonyl derivatized PAMAM-G2 dendrimers as nonviral gene delivery vectors with improved transfection efficiencies

Amphiphilic PAMAM-G2 derivatives engineered with peripheral alkyl chains are nonviral gene delivery vectors that exhibit high transfection efficiencies and low toxicity, particularly in the case of functionalization with C18 tails.

Graphical abstract: Alkyl sulfonyl derivatized PAMAM-G2 dendrimers as nonviral gene delivery vectors with improved transfection efficiencies
From the themed collection: Chemical Biology
Paper

Cell permeable ITAM constructs for the modulation of mediator release in mast cells

A synthetic cell permeable ITAM construct can enhance mast cell degranulation up to 140%.

Graphical abstract: Cell permeable ITAM constructs for the modulation of mediator release in mast cells
From the themed collection: Chemical Biology
Paper

Antimicrobial phenalenone derivatives from the marine-derived fungus Coniothyrium cereale

The marine algae-derived fungus Coniothyrium cereale produces phenalenone derivatives with a variety of significant biological activities.

Graphical abstract: Antimicrobial phenalenone derivatives from the marine-derived fungus Coniothyrium cereale
From the themed collection: Chemical Biology
Paper

Structural basis for the potential antitumour activity of DNA-interacting benzo[kl]xanthene lignans

The investigation of benzo[kl]xanthene as DNA ligands suggests they are suitable lead compounds for the design of new binders with potential antitumour properties.

Graphical abstract: Structural basis for the potential antitumour activity of DNA-interacting benzo[kl]xanthene lignans
From the themed collection: Chemical Biology
Paper

Comparable stabilisation, structural changes and activities can be induced in FGF by a variety of HS and non-GAG analogues: implications for sequence-activity relationships

Appropriate characteristics for FGF binding and activity are provided by various HS structures and non-GAG analogues

Graphical abstract: Comparable stabilisation, structural changes and activities can be induced in FGF by a variety of HS and non-GAG analogues: implications for sequence-activity relationships
From the themed collection: Chemical Biology
Paper

Discovery of a quorum sensing modulator pharmacophore by 3D small-molecule microarray screening

A 3D microarray platform was used to discover the biologically active chloro-pyridine pharmacophore, which was found to be able to inhibit N acyl-homoserine-lactone (AHL) mediated quorum sensing phenotypes in Serratia and Pseudomonas aeruginosa.

Graphical abstract: Discovery of a quorum sensing modulator pharmacophore by 3D small-molecule microarray screening
From the themed collection: Chemical Biology
Paper

Chemical genetics approach to identify new small molecule modulators of cell growth by phenotypic screening of Saccharomyces cerevisiae strains with a library of morpholine-derived compounds

The screening of yeast deletants strains with a pool of morpholine-derived compounds towards cell growth rate identified two small molecules able to produce phenotypic effects on yeast cells.

Graphical abstract: Chemical genetics approach to identify new small molecule modulators of cell growth by phenotypic screening of Saccharomyces cerevisiae strains with a library of morpholine-derived compounds
From the themed collection: Chemical Biology
Paper

Understanding the DNA binding of novel non-symmetrical guanidinium/2-aminoimidazolinium derivatives

The DNA binding of asymmetric guanidinium/2-aminoimidazolinium has been explored using different biophysical techniques such as SPR, UV-titrations, CD, LD and ITC.

Graphical abstract: Understanding the DNA binding of novel non-symmetrical guanidinium/2-aminoimidazolinium derivatives
From the themed collection: Chemical Biology
Paper

Tubulin-binding dibenz[c,e]oxepines as colchinol analogues for targeting tumour vasculature

Of various dibenz[c,e]oxepines prepared as colchinol analogues, 5,7-dihydro-3,9,10,11-tetramethoxydibenz[c,e]oxepin-4-ol is a potent inhibitor of microtubule assembly and cytotoxic agent.

Graphical abstract: Tubulin-binding dibenz[c,e]oxepines as colchinol analogues for targeting tumour vasculature
From the themed collection: Chemical Biology
Paper

Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates

Structure-based design, microwave-assisted synthesis and biochemical evaluation of 3-substituted pyridine dicarboxylates as JMJD2 histone demethylase inhibitors with selectivity over the PHD2 prolyl hydroxylase.

Graphical abstract: Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates
From the themed collection: Chemical Biology
Paper

Guanidiniocarbonyl-pyrrole-aryl conjugates as nucleic acid sensors: switch of binding mode and spectroscopic responses by introducing additional binding sites into the linker

Compounds 3 and 4 are specific spectroscopic probes for ds-polynucleotides interacting strongly with ds-DNAs (but only weakly with ds-RNA) being able to distinguish different forms of DNA minor grooves due to different positioning of the pyrene probe in the groove.

Graphical abstract: Guanidiniocarbonyl-pyrrole-aryl conjugates as nucleic acid sensors: switch of binding mode and spectroscopic responses by introducing additional binding sites into the linker
From the themed collection: Chemical Biology
Paper

Amino acids attached to 2′-amino-LNA: synthesis and excellent duplex stability

2′-Amino-LNA-derived monomers with positive charges improve thermal stability of duplexes.

Graphical abstract: Amino acids attached to 2′-amino-LNA: synthesis and excellent duplex stability
From the themed collection: Chemical Biology
Paper

Cationic nucleolipids as efficient siRNA carriers

Five novel uridine-based cationic nucleolipids, synthesized by introducing basic amino acid residues at the 5′ position of uridine, through 1,3-dipolar cycloaddition, and hydrophobic alkyl moieties at the 2′ and 3′ positions, through carbamate linkages, delivered siRNAs efficiently to cells without any severe toxicity.

Graphical abstract: Cationic nucleolipids as efficient siRNA carriers
From the themed collection: Chemical Biology
Paper

3-Phosphono-L-alanine as pyrophosphate mimic for DNA synthesis using HIV-1 reverse transcriptase

The synthesis and evaluation of a series of sulf(on)ate and phosph(on)ate amino acid phosphoramidate analogues of deoxynucleotides as potential substrates for HIV-1 reverse transcriptase are described.

Graphical abstract: 3-Phosphono-l-alanine as pyrophosphate mimic for DNA synthesis using HIV-1 reverse transcriptase
From the themed collection: Chemical Biology
Open Access Paper

Synthesis of cyclic adenosine 5′-diphosphate ribose analogues: a C2′ endo/syn “southern” ribose conformation underlies activity at the sea urchin cADPR receptor

Conformational analysis of cyclic ADP-ribose analogues reveals a correlation between a C2′ endo/syn “southern” ribose conformation and activity in sea urchin egg homogenates.

Graphical abstract: Synthesis of cyclic adenosine 5′-diphosphate ribose analogues: a C2′ endo/syn “southern” ribose conformation underlies activity at the sea urchin cADPR receptor
From the themed collection: Chemical Biology
Paper

Rapid chemical ligation of oligonucleotides by the Diels–Alder reaction

Simultaneous templated Diels–Alder chemical ligation of multiple furan and maleimide oligonucleotides proceeds within 1 min at room temperature.

Graphical abstract: Rapid chemical ligation of oligonucleotides by the Diels–Alder reaction
From the themed collection: Chemical Biology
Paper

Crystal structure of the insect neuropeptide proctolin.

The crystal structure of the neuropeptide proctolin (Arg-Tyr-Leu-Pro-Thr) is reported revealing the solid-state conformation of its molecules and their association in the crystal.

Graphical abstract: Crystal structure of the insect neuropeptide proctolin.
From the themed collection: Chemical Biology
Paper

Access to phosphoproteins and glycoproteins through semi-synthesis, Native Chemical Ligation and NS acyl transfer

Phosphoproteins and glycoproteins can be assembled through Native Chemical Ligation using thioesters prepared by NS acyl transfer.

Graphical abstract: Access to phosphoproteins and glycoproteins through semi-synthesis, Native Chemical Ligation and N→S acyl transfer
From the themed collection: Chemical Biology
Paper

Preparation of FRET reporters to support chemical probe development

We describe economical routes for the preparation of rhodamine maleimide and non-emitting quencher probes to enable a high throughput screening campaign that seeks to identify inhibitors of phosphopantetheinyl transferase.

Graphical abstract: Preparation of FRET reporters to support chemical probe development
From the themed collection: Chemical Biology
Paper

Highly efficient and enantioselective biotransformations of β-lactam carbonitriles and carboxamides and their synthetic applications

Biotransformations of nitriles and amides provide a highly efficient and enantioselective approach to enantioenriched β-lactam compounds, which are useful intermediates in the synthesis of fused heterocycles

Graphical abstract: Highly efficient and enantioselective biotransformations of β-lactam carbonitriles and carboxamides and their synthetic applications
From the themed collection: Chemical Biology
Paper

Quantum chemical dissection of the classic terpinyl/pinyl/bornyl/camphyl cation conundrum—the role of pyrophosphate in manipulating pathways to monoterpenes

Quantum chemical methods are used to reveal details of the conversion of farnesyl diphosphate to bornyl diphosphate and several monoterpenes.

Graphical abstract: Quantum chemical dissection of the classic terpinyl/pinyl/bornyl/camphyl cation conundrum—the role of pyrophosphate in manipulating pathways to monoterpenes
From the themed collection: Chemical Biology
Paper

N-Terminal peptidic boronic acids selectively inhibit human ClpXP

We report the synthesis and development of N-terminal peptidic boronic acids as novel protease inhibitors. These boronic acids harvest the unique selectivity inherent on the P′-site of peptide substrates. Our effort provides the first selective inhibitor of hClpXP over hLon; both are ATP-dependent serine proteases present in mitochondrial matrix.

Graphical abstract: N-Terminal peptidic boronic acids selectively inhibit human ClpXP
From the themed collection: Chemical Biology
28 items

About this collection

Organic and Biomolecular Chemistry has collated some of the latest exciting research from across the breadth of chemical biology published in our journal. You can read about it in this web themed issue guest edited by Nick Westwood (School of Chemistry and BSRC, University of St Andrews).

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