List of works - James R Kiefer

2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor

scientific article

A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385

scientific article

A reversed sulfonamide series of selective RORc inverse agonists

scientific article

An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells

scientific article

Characterization of celecoxib and valdecoxib binding to cyclooxygenase.

scientific article published in April 2003

Crystal structure of a thermostable Bacillus DNA polymerase I large fragment at 2.1 A resolution

scientific article

Crystallization and preliminary diffraction analysis of a hyperthermostable DNA polymerase from a Thermococcus archaeon

scientific article published on 01 September 1998

Cyclooxygenase enzymes: catalysis and inhibition

scientific article (publication date: December 2001)

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

scientific article published on 5 April 2016

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells

scientific article published on 06 January 2016

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300

scientific article (publication date: 8 December 2016)

Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)

scientific article published on 02 February 2010

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

scientific article

Expression, purification, characterization and crystallization of non- and phosphorylated states of JAK2 and JAK3 kinase domain.

scientific article published on 23 September 2009

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)

scientific article

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).

scientific article published in June 2017

High resolution crystal structure of the catalytic domain of ADAMTS-5 (aggrecanase-2)

scientific article

Improved crystallographic structures using extensive combinatorial refinement

scientific article

Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.

scientific article

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.

scientific article published on 29 June 2016

MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides

scientific article published on 01 April 2011

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres

scientific article published on 01 April 2011

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

scientific article published on 4 December 2014

Molecular basis for cyclooxygenase inhibition by the non-steroidal anti-inflammatory drug naproxen

scientific article

Observing translesion synthesis of an aromatic amine DNA adduct by a high-fidelity DNA polymerase.

scientific article published on 22 September 2004

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease

scientific article

Structural basis for dual-mode inhibition of the ABC transporter MsbA

scientific article published in Nature

Structure analysis reveals the flexibility of the ADAMTS-5 active site

scientific article

Structure of human ADAM-8 catalytic domain complexed with batimastat

scientific article

Structure of mammalian poly(ADP-ribose) glycohydrolase reveals a flexible tyrosine clasp as a substrate-binding element

scientific article

The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells

scientific article published on 02 June 2020

The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.

scientific article published on 23 July 2010

List of works by James R Kiefer

2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor

A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385

A reversed sulfonamide series of selective RORc inverse agonists

An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells

Characterization of celecoxib and valdecoxib binding to cyclooxygenase.

Crystal structure of a thermostable Bacillus DNA polymerase I large fragment at 2.1 A resolution

Crystallization and preliminary diffraction analysis of a hyperthermostable DNA polymerase from a Thermococcus archaeon

Cyclooxygenase enzymes: catalysis and inhibition

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300

Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

Expression, purification, characterization and crystallization of non- and phosphorylated states of JAK2 and JAK3 kinase domain.

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).

High resolution crystal structure of the catalytic domain of ADAMTS-5 (aggrecanase-2)

Improved crystallographic structures using extensive combinatorial refinement

Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.

MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Molecular basis for cyclooxygenase inhibition by the non-steroidal anti-inflammatory drug naproxen

Observing translesion synthesis of an aromatic amine DNA adduct by a high-fidelity DNA polymerase.

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease

Structural basis for dual-mode inhibition of the ABC transporter MsbA

Structure analysis reveals the flexibility of the ADAMTS-5 active site

Structure of human ADAM-8 catalytic domain complexed with batimastat

Structure of mammalian poly(ADP-ribose) glycohydrolase reveals a flexible tyrosine clasp as a substrate-binding element

The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells

The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate.