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Mitochondrial Protease ClpP is a Target for the Anticancer Compounds ONC201 and Related Analogues

ACS chemical biology, 2019-05, Vol.14 (5), p.1020-1029

2019

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The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor

Trends in pharmacological sciences (Regular ed.), 2011-11, Vol.32 (11), p.631-636

2011

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Positive allosteric modulators of the human sweet taste receptor enhance sweet taste

Proceedings of the National Academy of Sciences - PNAS, 2010-03, Vol.107 (10), p.4746-4751

2010

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Potent ClpP agonists with anticancer properties bind with improved structural complementarity and alter the mitochondrial N-terminome

Structure (London), 2023-02, Vol.31 (2), p.185-200.e10

2023

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The CIpP activator, TR-57, is highly effective as a single agent and in combination with venetoclax against CLL cells in vitro

Leukemia & lymphoma, 2024-05, Vol.65 (5), p.585-13

2024

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Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists

Journal of medicinal chemistry, 2020-05, Vol.63 (9), p.4957-4977

2020

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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Journal of medicinal chemistry, 2013-07, Vol.56 (14), p.5675-5690

2013

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Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2

Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (8), p.2109-2112

2006

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Correction to “Mitochondrial Protease ClpP Is a Target for the Anticancer Compounds ONC201 and Related Analogues”

ACS chemical biology, 2022-08, Vol.17 (8), p.2377-2378

2022

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Characterization of TR‐107, a novel chemical activator of the human mitochondrial protease ClpP

Pharmacology research & perspectives, 2022-08, Vol.10 (4), p.e00993-n/a

2022

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Toxicological evaluation of two flavors with modifying properties: 3-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2,2-dimethyl-N-propylpropanamide and (S)-1-(3-(((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)methyl)piperidin-1-yl)-3-methylbutan-1-one

Food and chemical toxicology, 2015-02, Vol.76, p.33-45

2015

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The ClpP activator ONC‐212 (TR‐31) inhibits BCL2 and B‐cell receptor signaling in CLL

EJHaem, 2021-02, Vol.2 (1), p.81-93

2021

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Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models

ACS medicinal chemistry letters, 2012-02, Vol.3 (2), p.140-145

2012

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Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1H-1,2,4-triazol-5-yl)thio)methyl)pyridine

Toxicology reports, 2016-01, Vol.3, p.501-512

2016

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Toxicological evaluation of two novel bitter modifying flavour compounds: 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione and 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)-5,5-dimethylimidazolidine-2,4-dione

Toxicology reports, 2016-01, Vol.3, p.310-327

2016

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Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists

Journal of medicinal chemistry, 2010-01, Vol.53 (1), p.77-105

2010

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Toxicological evaluation of the flavour ingredient N -(1-((4-amino-2,2-dioxido-1 H -benzo[ c ][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218)

Toxicology reports, 2017-01, Vol.4, p.507-520

2017

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Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (12), p.3504-3508

2008

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Toxicological evaluation and metabolism of two N -alkyl benzamide umami flavour compounds: N -(heptan-4-yl)benzo[d][1,3]dioxole-5-carboxamide and ( R )- N -(1-methoxy-4-methylpentan-2-yl)-3,4-dimethylbenzamide

Toxicology reports, 2016-01, Vol.3, p.841-860

2016

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Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1 H -1,2,4-triazol-5-yl)thio)methyl)pyridine

Toxicology reports, 2016, Vol.3, p.501-512

2016

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Toxicological evaluation of two novel bitter modifying flavour compounds: 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1 H -pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione and 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1 H -pyrazol-4-yl)-1-(3-hydroxybenzyl)-5,5-dimethylimidazolidine-2,4-dione

Toxicology reports, 2016, Vol.3, p.310-327

2016

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Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)- N -(1 H -pyrazol-3-yl)- N -(2-thienylmethyl)acetamide

Toxicology reports, 2015-01, Vol.2 (C), p.1291-1309

2015

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Discovery and biological evaluation of benzo[ a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor

Bioorganic & medicinal chemistry, 2008-10, Vol.18 (19), p.5255-5258

2008

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Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid

Toxicology reports, 2015-01, Vol.2 (C), p.1255-1264

2015

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Activation of the CED3/ICE-Related Protease CPP32 in Cerebellar Granule Neurons Undergoing Apoptosis But Not Necrosis

The Journal of neuroscience, 1997-01, Vol.17 (2), p.553-562

1997

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Mitochondrial Protease ClpP is a Target for the Anticancer Compounds ONC201 and Related Analogues

The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor

Positive allosteric modulators of the human sweet taste receptor enhance sweet taste

Potent ClpP agonists with anticancer properties bind with improved structural complementarity and alter the mitochondrial N-terminome

The CIpP activator, TR-57, is highly effective as a single agent and in combination with venetoclax against CLL cells in vitro

Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists

Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2

Correction to “Mitochondrial Protease ClpP Is a Target for the Anticancer Compounds ONC201 and Related Analogues”

Characterization of TR‐107, a novel chemical activator of the human mitochondrial protease ClpP

Toxicological evaluation of two flavors with modifying properties: 3-((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)-2,2-dimethyl-N-propylpropanamide and (S)-1-(3-(((4-amino-2,2-dioxido-1H-benzo[c][1,2,6]thiadiazin-5-yl)oxy)methyl)piperidin-1-yl)-3-methylbutan-1-one

The ClpP activator ONC‐212 (TR‐31) inhibits BCL2 and B‐cell receptor signaling in CLL

Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models

Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1H-1,2,4-triazol-5-yl)thio)methyl)pyridine

Toxicological evaluation of two novel bitter modifying flavour compounds: 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione and 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)-5,5-dimethylimidazolidine-2,4-dione

Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists

Toxicological evaluation of the flavour ingredient N -(1-((4-amino-2,2-dioxido-1 H -benzo[ c ][1,2,6]thiadiazin-5-yl)oxy)-2-methylpropan-2-yl)-2,6-dimethylisonicotinamide (S2218)

Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines

Toxicological evaluation and metabolism of two N -alkyl benzamide umami flavour compounds: N -(heptan-4-yl)benzo[d][1,3]dioxole-5-carboxamide and ( R )- N -(1-methoxy-4-methylpentan-2-yl)-3,4-dimethylbenzamide

Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1 H -1,2,4-triazol-5-yl)thio)methyl)pyridine

Toxicological evaluation of two novel bitter modifying flavour compounds: 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1 H -pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione and 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1 H -pyrazol-4-yl)-1-(3-hydroxybenzyl)-5,5-dimethylimidazolidine-2,4-dione

Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)- N -(1 H -pyrazol-3-yl)- N -(2-thienylmethyl)acetamide

Discovery and biological evaluation of benzo[ a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor

Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid

Activation of the CED3/ICE-Related Protease CPP32 in Cerebellar Granule Neurons Undergoing Apoptosis But Not Necrosis

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