(Q34626302)

3 August 2017

title

In situ click chemistry: a powerful means for lead discovery (English)

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3 August 2017

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1

K Barry Sharpless

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3 August 2017

Roman Manetsch

2

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3 August 2017

language of work or name

English

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publication date

1 November 2006

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Expert Opinion on Drug Discovery

3 August 2017

published in

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3 August 2017

volume

1

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3 August 2017

issue

6

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3 August 2017

page(s)

525-538

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Lead compounds discovered from libraries

3 August 2017

cites work

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Lead compounds discovered from libraries: part 2.

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Fragment-Based Drug Discovery

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Making drugs on proteins: site-directed ligand discovery for fragment-based lead assembly

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Fragment-based lead discovery: leads by design

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Library design for fragment based screening

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Fragment-based lead discovery using X-ray crystallography.

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Discovering high-affinity ligands for proteins: SAR by NMR

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Utility of NMR in lead optimization: fragment-based approaches

21 January 2018

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Receptor-assisted combinatorial chemistry: thermodynamics and kinetics in drug discovery

21 January 2018

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Dynamic Combinatorial Chemistry: The Unexpected Choice of Receptors by Guest Molecules

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Drug discovery by dynamic combinatorial libraries

21 January 2018

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Target-assisted selection of galactosyltransferase binders from dynamic combinatorial libraries. An unexpected solution with restricted amounts of the enzyme

21 January 2018

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Discovery of glutathione S-transferase inhibitors using dynamic combinatorial chemistry

21 January 2018

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Fragment-based drug discovery of carbonic anhydrase II inhibitors by dynamic combinatorial chemistry utilizing alkene cross metathesis

21 January 2018

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Amplification of bifunctional ligands for calmodulin from a dynamic combinatorial library

21 January 2018

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Dynamic combinatorial carbohydrate libraries: probing the binding site of the concanavalin A lectin

21 January 2018

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In situ generation and screening of a dynamic combinatorial carbohydrate library against concanavalin A.

21 January 2018

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Virtual combinatorial libraries: dynamic generation of molecular and supramolecular diversity by self-assembly

21 January 2018

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Tethering: fragment-based drug discovery

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Discovery of a New Phosphotyrosine Mimetic for PTP1B Using Breakaway Tethering

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

In situ assembly of enzyme inhibitors using extended tethering

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Site-directed ligand discovery

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

On the attribution and additivity of binding energies

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Multisubstrate adduct inhibitors of glycinamide ribonucleotide transformylase: Synthetic and enzyme-assembled

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Unexpected formation of an epoxide-derived multisubstrate adduct inhibitor on the active site of GAR transformylase

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Self-assembling cytotoxins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Synergism through direct covalent bonding between agents: a strategy for rational design of chemotherapeutic combinations

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

1.3-Dipolare Cycloadditionen, XXXII. Kinetik der Additionen organischer Azide an CC-Mehrfachbindungen

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Mechanism-based profiling of enzyme families

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Assembly of ultrathin polymer multilayer films by click chemistry.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Efficient templated synthesis of donor-acceptor rotaxanes using click chemistry.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Efficiency and Fidelity in a Click-Chemistry Route to Triazole Dendrimers by the Copper(I)-Catalyzed Ligation of Azides and Alkynes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Presentation and detection of azide functionality in bacterial cell surface proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

A strain-promoted [3 + 2] azide-alkyne cycloaddition for covalent modification of biomolecules in living systems

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Bioconjugation by copper(I)-catalyzed azide-alkyne [3 + 2] cycloaddition

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

The growing impact of click chemistry on drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Peptidotriazoles on solid phase: [1,2,3]-triazoles by regiospecific copper(i)-catalyzed 1,3-dipolar cycloadditions of terminal alkynes to azides

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Ruthenium-catalyzed cycloaddition of alkynes and organic azides

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Cell surface engineering by a modified Staudinger reaction

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

A "traceless" Staudinger ligation for the chemoselective synthesis of amide bonds

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

In situ click chemistry: enzyme inhibitors made to their own specifications

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

In situ selection of lead compounds by click chemistry: target-guided optimization of acetylcholinesterase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

The cholinesterases: from genes to proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Acetylcholinesterase: 'classical' and 'non-classical' functions and pharmacology

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Acetylcholinesterase: a multifaceted target for structure-based drug design of anticholinesterase agents for the treatment of Alzheimer's disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Interaction kinetics of reversible inhibitors and substrates with acetylcholinesterase and its fasciculin 2 complex

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Interaction of fluorescence probes with acetylcholinesterase. Site and specificity of propidium binding

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Desorption-ionization mass spectrometry on porous silicon

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

In-situ synthesis of a tacrine-triazole-based inhibitor of acetylcholinesterase: configurational selection imposed by steric interactions.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Molecular basis of interactions of cholinesterases with tight binding inhibitors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Freeze-frame inhibitor captures acetylcholinesterase in a unique conformation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Structural insights into conformational flexibility at the peripheral site and within the active center gorge of AChE.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Carbonic anhydrase inhibitors: 4-sulfamoyl-benzenecarboxamides and 4-chloro-3-sulfamoyl-benzenecarboxamides with strong topical antiglaucoma properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Carbonic anhydrase inhibitors: synthesis and inhibition against isozymes I, II and IV of topically acting antiglaucoma sulfonamides incorporating cis-5-norbornene-endo-3-carboxy-2-carboxamido moieties

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Screening derivatized peptide libraries for tight binding inhibitors to carbonic anhydrase II by electrospray ionization-mass spectrometry

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Combinatorial computational method gives new picomolar ligands for a known enzyme

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Integrated microfluidics for parallel screening of an in situ click chemistry library

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Recent developments in sequence selective minor groove DNA effectors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Triplex-forming molecules: from concepts to applications

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Studies on Some Interactions and Reactions of Oligonucleotides in Aqueous Solution*

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

DNA-templated dimerization of hairpin polyamides

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Financial anatomy of biomedical research

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Do enzymes sleep and work?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Differences in the chemical reactivity of individual molecules of an enzyme

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.1.6.525

Stretched exponential decay and correlations in the catalytic activity of fluctuating single lipase molecules

21 January 2018

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Syntheses of FDA Approved HIV Protease Inhibitors

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Using an Enzyme's Active Site To Template Inhibitors This work was supported by the Centre National de la Recherche Scientifique and by the Ecole Polytechnique (predoctoral fellowship to R.N.). We thank Prof. Jean-Marie Lehn for stimulating discussi

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Single molecule studies of enzyme mechanisms

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Dimerization of an Inactive Fragment of Huperzine A Produces a Drug with Twice the Potency of the Natural Product This work was supported by the Research Grants Council of Hong Kong (HKUST6156/97M), the Biotechnology Research Institute (HKUST), the

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

DNA methyltransferase-moderated click chemistry

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Sequence-Specific DNA Minor Groove Binders. Design and Synthesis of Netropsin and Distamycin Analogues

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Fluctuating enzymes: lessons from single-molecule studies.

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Click chemistry in situ: acetylcholinesterase as a reaction vessel for the selective assembly of a femtomolar inhibitor from an array of building blocks

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Synthesis and single enzyme activity of a clicked lipase–BSA hetero-dimer

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Direct synthesis of 1,5-disubstituted-4-magnesio-1,2,3-triazoles, revisited

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Single-enzyme kinetics of CALB-catalyzed hydrolysis

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Mechanisms of antibody binding to a protein

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Synthesis and biological evaluation of vancomycin dimers with potent activity against vancomycin-resistant bacteria: target-accelerated combinatorial synthesis.

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Inhibitors of HIV-1 protease by using in situ click chemistry

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Conformation coupled enzyme catalysis: single-molecule and transient kinetics investigation of dihydrofolate reductase

1 reference

11 October 2022

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10-Formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

The dynamic energy landscape of dihydrofolate reductase catalysis

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Dynamic combinatorial chemistry

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Polyvalent Interactions in Biological Systems: Implications for Design and Use of Multivalent Ligands and Inhibitors

1 reference

11 October 2022

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Structural basis for ligand promiscuity in cytochrome P450 3A4.

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Dynamic combinatorial chemistry: lysozyme selects an aromatic motif that mimics a carbohydrate residue

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

In situ click chemistry: enzyme-generated inhibitors of carbonic anhydrase II.

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Target-Accelerated Combinatorial Synthesis and Discovery of Highly Potent Antibiotics Effective Against Vancomycin-Resistant Bacteria

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Single-molecule enzymatic dynamics

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

The physical basis for induction of protein-reactive antipeptide antibodies

1 reference

11 October 2022

https://opencitations.net/index/coci/api/v1/references/10.1517/17460441.1.6.525

Identifiers

DOI

10.1517/17460441.1.6.525

1 reference

3 August 2017

1 reference