List of works - Theodore M Kamenecka

3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors

scientific article

A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an α Subunit

scientific article

An Accessory Agonist Binding Site Promotes Activation of α4β2* Nicotinic Acetylcholine Receptors

scientific article published on 13 April 2015

Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARgamma by Cdk5.

scientific article

Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation

scientific article

Antiobesity Effect of a Small Molecule Repressor of RORγ.

scientific article published on 22 April 2015

Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1

scientific article published on 08 December 2020

Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor

scientific article

Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis

scientific journal article

Cytochrome P450-mediated bioactivation of the epidermal growth factor receptor inhibitor erlotinib to a reactive electrophile

scientific article

Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists

scientific article

Development of a high-throughput screening-compatible cell-based functional assay to identify small molecule probes of the galanin 3 receptor (GalR3).

scientific article

Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration.

scientific article

Discovery of a Highly Selective CYP3A4 Inhibitor Suitable for Reaction Phenotyping Studies and Differentiation of CYP3A4 and CYP3A5 ⬇️

scientific article published on June 13, 2012

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists ⬇️

scientific article published on May 4, 2012

Efficient methodology for the synthesis of 3-amino-1,2,4-triazoles

scientific article

Hypocretin (orexin) facilitates reward by attenuating the antireward effects of its cotransmitter dynorphin in ventral tegmental area.

scientific article published on 24 March 2014

Identification of SR2211: a potent synthetic RORγ-selective modulator.

scientific article published on 13 February 2012

Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.

scientific article

Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors

scientific article

Insular hypocretin transmission regulates nicotine reward

scholarly article

LXR-Mediated Inhibition of CD4+ T Helper Cells ⬇️

scientific article published on September 28, 2012

Ligand and receptor dynamics contribute to the mechanism of graded PPARγ agonism.

scientific article published on January 2012

Multigram-scale Synthesis of Enantiopure 3,3-Difluoroproline

scientific article

Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation.

scientific article

Partial agonists activate PPARgamma using a helix 12 independent mechanism

scientific article

Pharmacologic repression of retinoic acid receptor-related orphan nuclear receptor γ is therapeutic in the collagen-induced arthritis experimental model

scientific article published on March 2014

Pharmacological Targeting the REV-ERBs in Sleep/Wake Regulation

scientific article

Pharmacological repression of PPARγ promotes osteogenesis

scientific article published on 12 June 2015

Pharmacological targeting of the mammalian clock regulates sleep architecture and emotional behaviour

scientific article

Quantitative structural assessment of graded receptor agonism

scientific article published on 14 October 2019

ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes

scientific article

RORα modulates semaphorin 3E transcription and neurovascular interaction in pathological retinal angiogenesis

scientific article published on 23 June 2017

Regulation of adipogenesis by natural and synthetic REV-ERB ligands.

scientific article

Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists

scientific article

Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy

scientific article

SR2067 Reveals a Unique Kinetic and Structural Signature for PPARγ Partial Agonism

scientific article published on 18 November 2015

Site-Selective γ-C(sp3 )-H and γ-C(sp2 )-H Arylation of Free Amino Esters Promoted by a Catalytic Transient Directing Group

scientific article published on 06 June 2018

Small molecule amides as potent ROR-γ selective modulators.

scientific article

Structural mechanism for signal transduction in RXR nuclear receptor heterodimers.

scientific article

Structure-Activity Relationships and X-ray Structures Describing the Selectivity of Aminopyrazole Inhibitors for c-Jun N-terminal Kinase 3 (JNK3) over p38

scientific article

Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand

scientific article

Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

scientific article

Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors

scientific article

Synthesis of 2-aryl-2H-tetrazoles via a regioselective [3+2] cycloaddition reaction

scientific article published on April 2016

Synthesis, Biological Evaluation, X-ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors

scientific article

Synthetic RORγt Agonists Enhance Protective Immunity

scientific article published on 19 January 2016

TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis

scientific journal article

The Methionine Transamination Pathway Controls Hepatic Glucose Metabolism through Regulation of the GCN5 Acetyltransferase and the PGC-1α Transcriptional Coactivator

scientific article published on 28 March 2016

The Secreted Enzyme PM20D1 Regulates Lipidated Amino Acid Uncouplers of Mitochondria

scientific journal article

The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).

scientific article

Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways

scientific article published on 15 April 2019

List of works by Theodore M Kamenecka

3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors

A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an α Subunit

An Accessory Agonist Binding Site Promotes Activation of α4β2* Nicotinic Acetylcholine Receptors

Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARgamma by Cdk5.

Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation

Antiobesity Effect of a Small Molecule Repressor of RORγ.

Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1

Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor

Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis

Cytochrome P450-mediated bioactivation of the epidermal growth factor receptor inhibitor erlotinib to a reactive electrophile

Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists

Development of a high-throughput screening-compatible cell-based functional assay to identify small molecule probes of the galanin 3 receptor (GalR3).

Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration.

Discovery of a Highly Selective CYP3A4 Inhibitor Suitable for Reaction Phenotyping Studies and Differentiation of CYP3A4 and CYP3A5 ⬇️

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists ⬇️

Efficient methodology for the synthesis of 3-amino-1,2,4-triazoles

Hypocretin (orexin) facilitates reward by attenuating the antireward effects of its cotransmitter dynorphin in ventral tegmental area.

Identification of SR2211: a potent synthetic RORγ-selective modulator.

Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.

Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors

Insular hypocretin transmission regulates nicotine reward

LXR-Mediated Inhibition of CD4+ T Helper Cells ⬇️

Ligand and receptor dynamics contribute to the mechanism of graded PPARγ agonism.

Multigram-scale Synthesis of Enantiopure 3,3-Difluoroproline

Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation.

Partial agonists activate PPARgamma using a helix 12 independent mechanism

Pharmacologic repression of retinoic acid receptor-related orphan nuclear receptor γ is therapeutic in the collagen-induced arthritis experimental model

Pharmacological Targeting the REV-ERBs in Sleep/Wake Regulation

Pharmacological repression of PPARγ promotes osteogenesis

Pharmacological targeting of the mammalian clock regulates sleep architecture and emotional behaviour

Quantitative structural assessment of graded receptor agonism

ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes

RORα modulates semaphorin 3E transcription and neurovascular interaction in pathological retinal angiogenesis

Regulation of adipogenesis by natural and synthetic REV-ERB ligands.

Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists

Rev-erb-α modulates skeletal muscle oxidative capacity by regulating mitochondrial biogenesis and autophagy

SR2067 Reveals a Unique Kinetic and Structural Signature for PPARγ Partial Agonism

Site-Selective γ-C(sp3 )-H and γ-C(sp2 )-H Arylation of Free Amino Esters Promoted by a Catalytic Transient Directing Group

Small molecule amides as potent ROR-γ selective modulators.

Structural mechanism for signal transduction in RXR nuclear receptor heterodimers.

Structure-Activity Relationships and X-ray Structures Describing the Selectivity of Aminopyrazole Inhibitors for c-Jun N-terminal Kinase 3 (JNK3) over p38

Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand

Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors

Synthesis of 2-aryl-2H-tetrazoles via a regioselective [3+2] cycloaddition reaction

Synthesis, Biological Evaluation, X-ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors

Synthetic RORγt Agonists Enhance Protective Immunity

TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis

The Methionine Transamination Pathway Controls Hepatic Glucose Metabolism through Regulation of the GCN5 Acetyltransferase and the PGC-1α Transcriptional Coactivator

The Secreted Enzyme PM20D1 Regulates Lipidated Amino Acid Uncouplers of Mitochondria

The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).

Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways