List of works - Adam Nelson

7.3 Directed Evolution and (Semi-) Rational Design Strategies for the Creation of Synthetically useful, Stereoselective Biocatalysts

A conceptual framework for analysing and planning synthetic approaches to diverse lead-like scaffolds ⬇️

scientific article published on March 2013

A convergent rhodium-catalysed asymmetric synthesis of tetrahydroquinolines ⬇️

scientific article published in September 2014

A fluorous-tagged "safety catch" linker for preparing heterocycles by ring-closing metathesis

scientific article published on February 2009

A fluorous-tagged linker from which small molecules are released by ring-closing metathesis

scientific article published on 8 March 2008

A general, two-directional approach to aza-C-(1 ? 1)-linked disaccharide mimetics

A method for the stereospecific conversion of 1,3-diols into oxetanes

article

A modular lead-oriented synthesis of diverse piperazine, 1,4-diazepane and 1,5-diazocane scaffolds ⬇️

scientific article published in April 2014

A novel chemically directed route for the generation of definitive endoderm from human embryonic stem cells based on inhibition of GSK-3.

scientific article published on 24 May 2011

A stereodivergent, two-directional synthesis of stereoisomeric C-linked disaccharide mimetics

scientific article

A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids ⬇️

scientific article published in June 2015

A two-directional synthesis of the C58-C71 fragment of palytoxin

scientific article published on 5 January 2004

A unified lead-oriented synthesis of over fifty molecular scaffolds ⬇️

scientific article

Activity-Directed Synthesis with Intermolecular Reactions: Development of a Fragment into a Range of Androgen Receptor Agonists ⬇️

scientific article published on 11 September 2015

Activity-directed expansion of a series of antibacterial agents

scientific article published on 15 June 2020

Aldolase-catalysed stereoselective synthesis of fluorinated small molecules ⬇️

scientific article

Alkenyl diols by E-selective Horner-Wittig elimination: Formal synthesis of any isomer (RR, RS, SR or SS) bearing 1,5-related stereogenic centres across an E double bond

Aminomethylhydroxylation of alkenes: Exploitation in the synthesis of scaffolds for small molecule libraries.

scientific article published on 11 February 2015

An Enantio- and Diastereoselective Chemoenzymatic Synthesis of α-Fluoro β-Hydroxy Carboxylic Esters ⬇️

scientific article published on 19 April 2016

An Enantio- and Diastereoselective Chemoenzymatic Synthesis of α-Fluoro β-Hydroxy Carboxylic Esters ⬇️

An approach to the total synthesis of lankacidins: synthesis of advanced macrocyclic precursors

An approach to the total synthesis of lankacidins: synthesis of the requisite building blocks

article by Christopher T Brain et al published February 2001 in Tetrahedron Letters

An efficient method for synthesising unsymmetrical silaketals: substrates for ring-closing, including macrocycle-closing, metathesis

scientific article published on 10 April 2008

An efficient protocol for a sharpless style racemic dihydroxylation

Asymmetric Phase-Transfer Catalysis

scientific article published in June 1999

Asymmetric addition of Davies's chiral lithium amide to prochiral vinyl phosphine oxides

article

Asymmetric dihydroxylations of allylic phosphine oxides

Asymmetric double ring-opening of a C(2h)-symmetric bis-epoxide: improved enantiomeric excess of the product through enantioselective desymmetrisation and 'proof-reading' steps

scientific article published on 23 May 2005

Catalyst control in sequential asymmetric allylic substitution: stereodivergent access to N,N-diprotected unnatural amino acids

scientific article published on 8 June 2011

Catalytic and stoichiometric approaches to the desymmetrisation of centrosymmetric piperazines by enantioselective acylation: a total synthesis of Dragmacidin A

scientific article published on 01 November 2006

Chiral phosphine oxides and chiral esters in stereoselective intermolecular acylation reactions of phosphine oxides

Cloning, over-expression, purification, and characterisation of N-acetylneuraminate synthase from Streptococcus agalactiae

scientific article published in February 2003

Comparison of the ATP binding sites of protein kinases using conformationally diverse bisindolylmaleimides

scientific article published in August 2005

Configurational stability of bisindolylmaleimide cyclophanes: from conformers to the first configurationally stable, atropisomeric bisindolylmaleimides

scientific article

Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase

scientific article published on 26 April 2019

Convergent synthesis of dihydroquinolones from o-aminoarylboronates

article

Convergent, regiospecific synthesis of quinolines from o-aminophenylboronates

scientific article published on 23 August 2008

Correction: Correction: Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions ⬇️

scientific article published on 02 February 2018

Creation of a pair of stereochemically complementary biocatalysts

scientific article published in December 2006

Creation of a tailored aldolase for the parallel synthesis of sialic acid mimetics

scientific article published in March 2005

Design and synthesis of a fragment set based on twisted bicyclic lactams ⬇️

scientific article published on 22 February 2018

Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries.

scientific article published on 29 December 2014

Design, synthesis and in vitro evaluation of novel bivalent S-adenosylmethionine analogues

scientific article published on 11 November 2011

Desymmetrisation of a Centrosymmetric Molecule by Carbon–Carbon Bond Formation: Asymmetric Aldol Reactions of a Centrosymmetric Dialdehyde

Desymmetrization of a centrosymmetric diepoxide: efficient synthesis of a key intermediate in a total synthesis of hemibrevetoxin B

scientific article (publication date: 7 February 2003)

Development of an approach to the synthesis of the ABC ring system of Hemibrevetoxin B.

scientific article published in September 2006

Development of an organo- and enzyme-catalysed one-pot, sequential three-component reaction ⬇️

article

Diastereoselective reactions of optically active γ-substituted vinyl phosphine oxides

Directed evolution of aldolases for exploitation in synthetic organic chemistry

scientific article published on 19 January 2008

Directed evolution of enzymes for biocatalysis and the life sciences.

scientific article

Discovery of novel FabF ligands inspired by platensimycin by integrating structure-based design with diversity-oriented synthetic accessibility ⬇️

scientific article

Efficient unified synthesis of diverse bridged polycyclic scaffolds using a complexity-generating 'stitching' annulation approach

scientific article published on 21 December 2020

Engineering aldolases as biocatalysts ⬇️

scientific article published on 04 January 2014

Erratum: Further Correction: Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions ⬇️

scientific article published on 01 February 2018

Evaluating New Chemistry to Drive Molecular Discovery: Fit for Purpose? ⬇️

scientific article

Evaluation of alternative approaches for the synthesis of macrocyclic bisindolylmaleimides

scientific article published on 10 September 2004

Evaluation of fluoropyruvate as nucleophile in reactions catalysed by N-acetyl neuraminic acid lyase variants: scope, limitations and stereoselectivity ⬇️

scientific article published on 5 November 2015

Evaluierung neuer Reaktionen zur Steuerung der Wirkstoff-Forschung: ein Eignungstest

Expansion of the structure-activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach

scientific article published on 22 March 2019

Exploitation of the Ugi–Joullié Reaction in the Synthesis of Libraries of Drug-Like Bicyclic Hydantoins ⬇️

Exploiting predisposition in the stereoselective synthesis of mono-, bi- and tetracyclic oxygen heterocycles: equilibration between, and trapping of, alternative di- and tetraacetals

scientific article published in July 2003

Exploration of the HIF-1α/p300 interface using peptide and Adhiron phage display technologies ⬇️

scientific article

Extending enzyme molecular recognition with an expanded amino acid alphabet ⬇️

scientific article

First Desymmetrization of a Centrosymmetric Molecule in Natural Product Synthesis: Preparation of a Key Fragment in the Synthesis of Hemibrevetoxin B.

scientific article published in November 2001

Fragment-oriented synthesis: β-elaboration of cyclic amine fragments using enecarbamates as platform intermediates

scientific article published on 06 July 2020

High-content, high-throughput screening for the identification of cytotoxic compounds based on cell morphology and cell proliferation markers ⬇️

scientific article (publication date: 2014)

Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions ⬇️

scientific article published on 26 April 2017

Identification and characterization of important residues in the catalytic mechanism of CMP-Neu5Ac synthetase from Neisseria meningitidis

scientific article

Identification of stable S-adenosylmethionine (SAM) analogues derivatised with bioorthogonal tags: effect of ligands on the affinity of the E. coli methionine repressor, MetJ, for its operator DNA. ⬇️

scientific article published on 19 December 2008

Innovative approaches to the design and synthesis of small molecule libraries

scientific article published on 28 February 2015

Intramolecular acylations of γ-benzoyloxy phosphine oxides: synthesis of optically active cyclopropyl ketones

Involvement of GSK-3 in regulation of murine embryonic stem cell self-renewal revealed by a series of bisindolylmaleimides

scientific article published in January 2009

Iridium-Catalyzed Asymmetric Allylic Amination with Polar Amines: Access to Building Blocks with Lead-Like Molecular Properties

scientific article

Methods for the synthesis of polyhydroxylated piperidines by diastereoselective dihydroxylation: exploitation in the two-directional synthesis of aza-C-linked disaccharide derivatives ⬇️

scientific article

Modifying the stereochemistry of an enzyme-catalyzed reaction by directed evolution ⬇️

scholarly article

Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity ⬇️

scientific article published on 4 April 2017

Modular synthesis of thirty lead-like scaffolds suitable for CNS drug discovery ⬇️

scientific article published on 3 November 2017

Modular, gold-catalyzed approach to the synthesis of lead-like piperazine scaffolds ⬇️

scientific article published on 12 November 2013

Natural products as an inspiration in the diversity-oriented synthesis of bioactive compound libraries

scientific article

Photochemical transformations of pyridinium salts: mechanistic studies and applications in synthesis

scientific article published on 29 June 2007

Reaching the target: small molecules aim to probe barrier quality

scientific article published in November 2005

Reaction Mechanism of N -Acetylneuraminic Acid Lyase Revealed by a Combination of Crystallography, QM/MM Simulation, and Mutagenesis ⬇️

scientific article

Recent advances and applications of iridium-catalysed asymmetric allylic substitution

scientific article published on 12 March 2012

Regioselective side-chain amination of 2-alkyl azacycles by radical translocation: total synthesis of tetraponerine T8

scientific article published on 04 January 2021

Regulation of Nanog Expression by Phosphoinositide 3-Kinase-dependent Signaling in Murine Embryonic Stem Cells

scientific article published in Journal of Biological Chemistry

Remarkably slow rotation about a single bond between an sp(3)-hybridised carbon atom and an aromatic ring without ortho substituents

scientific article published in January 2009

Scanning conformational space with a library of stereo- and regiochemically diverse aminoglycoside derivatives: the discovery of new ligands for RNA hairpin sequences

scientific article

Small-molecule proteomimetic inhibitors of the HIF-1α-p300 protein-protein interaction ⬇️

scientific article

Stereospecific conversion of (1R,3S)- and (1R,3R)-3-cyclohexyl-1-phenylpropane-1,3-diol into the corresponding 2,4-disubstituted oxetanes

article

Structural Insights into Substrate Specificity in Variants of N-Acetylneuraminic Acid Lyase Produced by Directed Evolution

scientific article

Structural Insights into the Recovery of Aldolase Activity inN-Acetylneuraminic Acid Lyase by Replacement of the Catalytically Active Lysine with γ-Thialysine by Using a Chemical Mutagenesis Strategy

scientific article

Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase

scientific article published in December 2005

Structure of anEscherichia coli N-acetyl-D-neuraminic acid lyase mutant, E192N, in complex with pyruvate at 1.45 Å resolution

scientific article

Structure-guided saturation mutagenesis of N-acetylneuraminic acid lyase for the synthesis of sialic acid mimetics.

scientific article published on 16 May 2005

Stuart Warren (24 Dec 1938-22 Mar 2020)

scientific article published on 16 September 2020

Synthesis and Demonstration of the Biological Relevance of sp3 -rich Scaffolds Distantly Related to Natural Product Frameworks. ⬇️

scientific article published on 6 October 2017

Synthesis and investigation of the configurational stability of some dimethylammonium borate salts

Synthesis of 3-Sulfonyloxypyridines: Oxidative Ring Expansion of α-Furylsulfonamides and N→O Sulfonyl Transfer

Synthesis of Skeletally Diverse Alkaloid-Like Small Molecules

Synthesis of a library of stereo- and regiochemically diverse aminoglycoside derivatives

scientific article published on 23 June 2005

Synthesis of highly functionalized oligobenzamide proteomimetic foldamers by late stage introduction of sensitive groups ⬇️

scientific article

Synthesis of macrocyclic precursors of lankacidins using Stille reactions of 4-(2-iodo-alkenyl)azetidinones and related compounds for ring closure

Synthesis of natural-product-like molecules with over eighty distinct scaffolds

scientific article published on January 2009

Synthesis of screening substrates for the directed evolution of sialic acid aldolase: towards tailored enzymes for the preparation of influenza A sialidase inhibitor analogues

scientific article published on 12 April 2005

Synthesis of skeletally diverse alkaloid-like molecules: exploitation of metathesis substrates assembled from triplets of building blocks

scientific article published on 22 April 2013

Synthesis of small molecules with high scaffold diversity: exploitation of metathesis cascades in combination with inter- and intramolecular Diels-Alder reactions

scientific article published in August 2010

The development of strategies and methods for the synthesis of biologically active compounds

article

Towards "bionic" proteins: replacement of continuous sequences from HIF-1α with proteomimetics to create functional p300 binding HIF-1α mimics ⬇️

scientific article published on 24 March 2016

Towards phase-transfer catalysts with a chiral anion: inducing asymmetry in the reactions of cations

Towards the realisation of lead-oriented synthesis

scientific article

Towards the systematic exploration of chemical space

scientific article

Translation of innovative chemistry into screening libraries: an exemplar partnership from the European Lead Factory ⬇️

scientific article published on 09 May 2018

List of works by Adam Nelson

7.3 Directed Evolution and (Semi-) Rational Design Strategies for the Creation of Synthetically useful, Stereoselective Biocatalysts

A conceptual framework for analysing and planning synthetic approaches to diverse lead-like scaffolds ⬇️

A convergent rhodium-catalysed asymmetric synthesis of tetrahydroquinolines ⬇️

A fluorous-tagged "safety catch" linker for preparing heterocycles by ring-closing metathesis

A fluorous-tagged linker from which small molecules are released by ring-closing metathesis

A general, two-directional approach to aza-C-(1 ? 1)-linked disaccharide mimetics

A method for the stereospecific conversion of 1,3-diols into oxetanes

A modular lead-oriented synthesis of diverse piperazine, 1,4-diazepane and 1,5-diazocane scaffolds ⬇️

A novel chemically directed route for the generation of definitive endoderm from human embryonic stem cells based on inhibition of GSK-3.

A stereodivergent, two-directional synthesis of stereoisomeric C-linked disaccharide mimetics

A systematic approach to diverse, lead-like scaffolds from α,α-disubstituted amino acids ⬇️

A two-directional synthesis of the C58-C71 fragment of palytoxin

A unified lead-oriented synthesis of over fifty molecular scaffolds ⬇️

Activity-Directed Synthesis with Intermolecular Reactions: Development of a Fragment into a Range of Androgen Receptor Agonists ⬇️

Activity-directed expansion of a series of antibacterial agents

Aldolase-catalysed stereoselective synthesis of fluorinated small molecules ⬇️

Alkenyl diols by E-selective Horner-Wittig elimination: Formal synthesis of any isomer (RR, RS, SR or SS) bearing 1,5-related stereogenic centres across an E double bond

Aminomethylhydroxylation of alkenes: Exploitation in the synthesis of scaffolds for small molecule libraries.

An Enantio- and Diastereoselective Chemoenzymatic Synthesis of α-Fluoro β-Hydroxy Carboxylic Esters ⬇️

An Enantio- and Diastereoselective Chemoenzymatic Synthesis of α-Fluoro β-Hydroxy Carboxylic Esters ⬇️

An approach to the total synthesis of lankacidins: synthesis of advanced macrocyclic precursors

An approach to the total synthesis of lankacidins: synthesis of the requisite building blocks

An efficient method for synthesising unsymmetrical silaketals: substrates for ring-closing, including macrocycle-closing, metathesis

An efficient protocol for a sharpless style racemic dihydroxylation

Asymmetric Phase-Transfer Catalysis

Asymmetric addition of Davies's chiral lithium amide to prochiral vinyl phosphine oxides

Asymmetric dihydroxylations of allylic phosphine oxides

Asymmetric double ring-opening of a C(2h)-symmetric bis-epoxide: improved enantiomeric excess of the product through enantioselective desymmetrisation and 'proof-reading' steps

Catalyst control in sequential asymmetric allylic substitution: stereodivergent access to N,N-diprotected unnatural amino acids

Catalytic and stoichiometric approaches to the desymmetrisation of centrosymmetric piperazines by enantioselective acylation: a total synthesis of Dragmacidin A

Chiral phosphine oxides and chiral esters in stereoselective intermolecular acylation reactions of phosphine oxides

Cloning, over-expression, purification, and characterisation of N-acetylneuraminate synthase from Streptococcus agalactiae

Comparison of the ATP binding sites of protein kinases using conformationally diverse bisindolylmaleimides

Configurational stability of bisindolylmaleimide cyclophanes: from conformers to the first configurationally stable, atropisomeric bisindolylmaleimides

Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase

Convergent synthesis of dihydroquinolones from o-aminoarylboronates

Convergent, regiospecific synthesis of quinolines from o-aminophenylboronates

Correction: Correction: Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions ⬇️

Creation of a pair of stereochemically complementary biocatalysts

Creation of a tailored aldolase for the parallel synthesis of sialic acid mimetics

Design and synthesis of a fragment set based on twisted bicyclic lactams ⬇️

Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries.

Design, synthesis and in vitro evaluation of novel bivalent S-adenosylmethionine analogues

Desymmetrisation of a Centrosymmetric Molecule by Carbon–Carbon Bond Formation: Asymmetric Aldol Reactions of a Centrosymmetric Dialdehyde

Desymmetrization of a centrosymmetric diepoxide: efficient synthesis of a key intermediate in a total synthesis of hemibrevetoxin B

Development of an approach to the synthesis of the ABC ring system of Hemibrevetoxin B.

Development of an organo- and enzyme-catalysed one-pot, sequential three-component reaction ⬇️

Diastereoselective reactions of optically active γ-substituted vinyl phosphine oxides

Directed evolution of aldolases for exploitation in synthetic organic chemistry

Directed evolution of enzymes for biocatalysis and the life sciences.

Discovery of novel FabF ligands inspired by platensimycin by integrating structure-based design with diversity-oriented synthetic accessibility ⬇️

Efficient unified synthesis of diverse bridged polycyclic scaffolds using a complexity-generating 'stitching' annulation approach

Engineering aldolases as biocatalysts ⬇️

Erratum: Further Correction: Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions ⬇️

Evaluating New Chemistry to Drive Molecular Discovery: Fit for Purpose? ⬇️

Evaluation of alternative approaches for the synthesis of macrocyclic bisindolylmaleimides

Evaluation of fluoropyruvate as nucleophile in reactions catalysed by N-acetyl neuraminic acid lyase variants: scope, limitations and stereoselectivity ⬇️

Evaluierung neuer Reaktionen zur Steuerung der Wirkstoff-Forschung: ein Eignungstest

Expansion of the structure-activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach

Exploitation of the Ugi–Joullié Reaction in the Synthesis of Libraries of Drug-Like Bicyclic Hydantoins ⬇️

Exploiting predisposition in the stereoselective synthesis of mono-, bi- and tetracyclic oxygen heterocycles: equilibration between, and trapping of, alternative di- and tetraacetals

Exploration of the HIF-1α/p300 interface using peptide and Adhiron phage display technologies ⬇️

Extending enzyme molecular recognition with an expanded amino acid alphabet ⬇️

First Desymmetrization of a Centrosymmetric Molecule in Natural Product Synthesis: Preparation of a Key Fragment in the Synthesis of Hemibrevetoxin B.

Fragment-oriented synthesis: β-elaboration of cyclic amine fragments using enecarbamates as platform intermediates

High-content, high-throughput screening for the identification of cytotoxic compounds based on cell morphology and cell proliferation markers ⬇️

Hypoxia inducible factor (HIF) as a model for studying inhibition of protein-protein interactions ⬇️

Identification and characterization of important residues in the catalytic mechanism of CMP-Neu5Ac synthetase from Neisseria meningitidis

Identification of stable S-adenosylmethionine (SAM) analogues derivatised with bioorthogonal tags: effect of ligands on the affinity of the E. coli methionine repressor, MetJ, for its operator DNA. ⬇️

Innovative approaches to the design and synthesis of small molecule libraries

Intramolecular acylations of γ-benzoyloxy phosphine oxides: synthesis of optically active cyclopropyl ketones

Involvement of GSK-3 in regulation of murine embryonic stem cell self-renewal revealed by a series of bisindolylmaleimides

Iridium-Catalyzed Asymmetric Allylic Amination with Polar Amines: Access to Building Blocks with Lead-Like Molecular Properties

Methods for the synthesis of polyhydroxylated piperidines by diastereoselective dihydroxylation: exploitation in the two-directional synthesis of aza-C-linked disaccharide derivatives ⬇️

Modifying the stereochemistry of an enzyme-catalyzed reaction by directed evolution ⬇️

Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity ⬇️

Modular synthesis of thirty lead-like scaffolds suitable for CNS drug discovery ⬇️

Modular, gold-catalyzed approach to the synthesis of lead-like piperazine scaffolds ⬇️

Natural products as an inspiration in the diversity-oriented synthesis of bioactive compound libraries

Stereospecific conversion of (1R,3S)- and (1R,3R)-3-cyclohexyl-1-phenylpropane-1,3-diol into the corresponding 2,4-disubstituted oxetanes