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Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors

Journal of medicinal chemistry, 2013-12, Vol.56 (24), p.9820-9825

2013

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Small-molecule activation of SERCA2a SUMOylation for the treatment of heart failure

Nature communications, 2015-06, Vol.6 (1), p.7229-7229, Article 7229

2015

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Small Molecule Inhibition of Ligand-Stimulated RAGE-DIAPH1 Signal Transduction

Scientific reports, 2016-03, Vol.6 (1), p.22450-22450, Article 22450

2016

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Acyl-CoA dehydrogenase substrate promiscuity: Challenges and opportunities for development of substrate reduction therapy in disorders of valine and isoleucine metabolism

Journal of inherited metabolic disease, 2023-09, Vol.46 (5), p.931-942

2023

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Structure-Activity Relationships and Biological Evaluation of 7-Substituted Harmine Analogs for Human β-Cell Proliferation

Molecules (Basel, Switzerland), 2020-04, Vol.25 (8), p.1983

2020

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Current Status of the Research and Development of Diacylglycerol O‑Acyltransferase 1 (DGAT1) Inhibitors: Miniperspective

Journal of medicinal chemistry, 2013-12, Vol.56 (24), p.9820-9825

2013

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Characterization and structure of the human lysine-2-oxoglutarate reductase domain, a novel therapeutic target for treatment of glutaric aciduria type 1

Open biology, 2022-09, Vol.12 (9), p.220179-220179

2022

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Monoubiquitination empowers ubiquitin chain elongation

The Journal of biological chemistry, 2024-03, Vol.300 (3), p.105753-105753, Article 105753

2024

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Modulation of Cullin-RING E3 ubiquitin ligase-dependent ubiquitination by small molecule compounds

The Journal of biological chemistry, 2024-03, Vol.300 (3), p.105752-105752, Article 105752

2024

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A case of hyperlysinemia identified by urine newborn screening

JIMD reports, 2023-11, Vol.64 (6), p.440-445

2023

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DYRK1A Inhibitors as Potential Therapeutics for β‑Cell Regeneration for Diabetes

Journal of medicinal chemistry, 2021-03, Vol.64 (6), p.2901-2922

2021

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Identification and characterization of sebaceous gland atrophy-sparing DGAT1 inhibitors

PloS one, 2014-02, Vol.9 (2), p.e88908

2014

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Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β‑Cell Proliferation

Journal of medicinal chemistry, 2018-09, Vol.61 (17), p.7687-7699

2018

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Food colorants metabolized by commensal bacteria promote colitis in mice with dysregulated expression of interleukin-23

Cell metabolism, 2021-07, Vol.33 (7), p.1358-1371.e5

2021

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IUPAC-Richter Prize Call for Nominations

Journal of medicinal chemistry, 2021-10, Vol.64 (19), p.13937-13937

2021

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Small-molecule antagonism of the interaction of the RAGE cytoplasmic domain with DIAPH1 reduces diabetic complications in mice

Science translational medicine, 2021-11, Vol.13 (621), p.eabf7084

2021

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CRL4b Inhibition Ameliorates Experimental Autoimmune Encephalomyelitis Progression

The Journal of immunology (1950), 2024-03, Vol.212 (6), p.982

2024

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Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β‑Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor

Journal of medicinal chemistry, 2020-03, Vol.63 (6), p.2986-3003

2020

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349-OR: Selected DYRK1A Inhibitors Simultaneously Drive Both Human Beta-Cell Proliferation and Differentiation

Diabetes (New York, N.Y.), 2023-06, Vol.72 (Supplement_1), p.1

2023

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DHTKD1 and OGDH display substrate overlap in cultured cells and form a hybrid 2-oxo acid dehydrogenase complex in vivo

Human molecular genetics, 2020-05, Vol.29 (7), p.1168-1179

2020

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The use of stable-isotopically labeled oleic acid to interrogate lipid assembly in vivo: assessing pharmacological effects in preclinical species

Journal of lipid research, 2011-06, Vol.52 (6), p.1150-1161

2011

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Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity

European journal of medicinal chemistry, 2018-09, Vol.157, p.1005-1016

2018

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Encounter and React: Computer-Guided Design of Covalent Inhibitors

Cell chemical biology, 2019-01, Vol.26 (1), p.6-8

2019

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Deletion of 2‐aminoadipic semialdehyde synthase limits metabolite accumulation in cell and mouse models for glutaric aciduria type 1

Journal of inherited metabolic disease, 2020-11, Vol.43 (6), p.1154-1164

2020

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Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl‑1H‑benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors

Journal of medicinal chemistry, 2017-05, Vol.60 (9), p.3594-3605

2017

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Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors

Small-molecule activation of SERCA2a SUMOylation for the treatment of heart failure

Small Molecule Inhibition of Ligand-Stimulated RAGE-DIAPH1 Signal Transduction

Acyl-CoA dehydrogenase substrate promiscuity: Challenges and opportunities for development of substrate reduction therapy in disorders of valine and isoleucine metabolism

Structure-Activity Relationships and Biological Evaluation of 7-Substituted Harmine Analogs for Human β-Cell Proliferation

Current Status of the Research and Development of Diacylglycerol O‑Acyltransferase 1 (DGAT1) Inhibitors: Miniperspective

Characterization and structure of the human lysine-2-oxoglutarate reductase domain, a novel therapeutic target for treatment of glutaric aciduria type 1

Monoubiquitination empowers ubiquitin chain elongation

Modulation of Cullin-RING E3 ubiquitin ligase-dependent ubiquitination by small molecule compounds

A case of hyperlysinemia identified by urine newborn screening

DYRK1A Inhibitors as Potential Therapeutics for β‑Cell Regeneration for Diabetes

Identification and characterization of sebaceous gland atrophy-sparing DGAT1 inhibitors

Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β‑Cell Proliferation

Food colorants metabolized by commensal bacteria promote colitis in mice with dysregulated expression of interleukin-23

IUPAC-Richter Prize Call for Nominations

Small-molecule antagonism of the interaction of the RAGE cytoplasmic domain with DIAPH1 reduces diabetic complications in mice

CRL4b Inhibition Ameliorates Experimental Autoimmune Encephalomyelitis Progression

Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β‑Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor

349-OR: Selected DYRK1A Inhibitors Simultaneously Drive Both Human Beta-Cell Proliferation and Differentiation

DHTKD1 and OGDH display substrate overlap in cultured cells and form a hybrid 2-oxo acid dehydrogenase complex in vivo

The use of stable-isotopically labeled oleic acid to interrogate lipid assembly in vivo: assessing pharmacological effects in preclinical species

Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity

Encounter and React: Computer-Guided Design of Covalent Inhibitors

Deletion of 2‐aminoadipic semialdehyde synthase limits metabolite accumulation in cell and mouse models for glutaric aciduria type 1

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl‑1H‑benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors

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