Lista de obras - James R Kiefer - Dominio Público Uruguay

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

artículo científico publicado en 2009

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

artículo científico publicado en 2003

A reversed sulfonamide series of selective RORc inverse agonists

artículo científico publicado en 2014

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

artículo científico publicado en 2016

Characterization of celecoxib and valdecoxib binding to cyclooxygenase.

artículo científico publicado en 2003

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

artículo científico publicado en 1997

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

artículo científico publicado en 1998

Cyclooxygenase enzymes: catalysis and inhibition

artículo científico publicado en 2001

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

artículo científico publicado en 2016

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

artículo científico publicado en 2016

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

artículo científico publicado en 2016

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

artículo científico

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

artículo científico publicado en 2016

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

artículo científico publicado en 2009

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

artículo científico publicado en 2016

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

artículo científico publicado en 2017

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

artículo científico publicado en 2008

Improved crystallographic structures using extensive combinatorial refinement

artículo científico publicado en 2013

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

artículo científico publicado en 2017

Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters ⬇️

artículo científico publicado el 13 de abril de 2012

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.

artículo científico publicado en 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.

artículo científico publicado en 2014

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

artículo científico publicado en 2010

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

artículo científico publicado en 2004

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

artículo científico publicado en 2010

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

artículo científico publicado en 2018

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

artículo científico publicado en 2011

Structure of human ADAM-8 catalytic domain complexed with batimastat

artículo científico publicado en 2012

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

artículo científico publicado en 2012

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.

artículo científico publicado en 2010

Visualizing DNA replication in a catalytically active Bacillus DNA polymerase crystal ⬇️

artículo científico publicado el 15 de enero de 1998

Lista de obras de 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.

Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters ⬇️

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.

Visualizing DNA replication in a catalytically active Bacillus DNA polymerase crystal ⬇️