An overview of patented small molecule stearoyl coenzyme-A desaturase inhibitors (2009 – 2013)

A Novel Inhibitor of Stearoyl-CoA Desaturase-1 Attenuates Hepatic Lipid Accumulation, Liver Injury and Inflammation in Model of Nonalcoholic Steatohepatitis

(2013) Nobuya Kurikawa et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Medicinal Chemistry Design Principles for Liver Targeting Through OATP Transporters

(2013) Meihua Tu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Pharmacological Inhibition of Stearoyl CoA Desaturase in the Skin Induces Atrophy of the Sebaceous Glands

(2013) Josef G. Meingassner et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Stearoyl-CoA desaturase: a novel therapeutic target for RCC

(2013) Annette Fenner   Nature Reviews Urology

Discovery of liver-targeted inhibitors of stearoyl-CoA desaturase (SCD1)

(2012) Yongqi Deng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recent Advances on Stearoyl-Coa Desaturase Regulation in Fatty Liver Diseases

(2012) Michel Narce et al.   CURRENT DRUG METABOLISM

Discovery of Piperazin-1-ylpyridazine-Based Potent and Selective Stearoyl-CoA Desaturase-1 Inhibitors for the Treatment of Obesity and Metabolic Syndrome

(2012) Zaihui Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Estimated plasma stearoyl co-A desaturase-1 activity and risk of incident diabetes: The Atherosclerosis Risk in Communities (ARIC) study

(2012) Lisa S. Chow et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

StearoylCoA Desaturase-5: A Novel Regulator of Neuronal Cell Proliferation and Differentiation

(2012) Debora I. Sinner et al.   PLoS One

Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: From systemic to liver-targeting inhibitors

(2011) Yeeman K. Ramtohul et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Nicotinic acids: Liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy

(2011) David A. Powell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

N-Benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors

(2011) Karen A. Atkinson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors

(2011) Jean-Philippe Leclerc et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series

(2011) Nicolas Lachance et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series

(2011) Nicolas Lachance et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bioinformatics and Systems Biology of the Lipidome

(2011) Shankar Subramaniam et al.   CHEMICAL REVIEWS

Plasma-based approach to measure target engagement for liver-targeting stearoyl-CoA desaturase 1 inhibitors

(2011) France Landry et al.   JOURNAL OF LIPID RESEARCH

Development of a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor (MK-8245) to Establish a Therapeutic Window for the Treatment of Diabetes and Dyslipidemia

(2011) Renata M. Oballa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stearoyl CoA desaturase (SCD) facilitates proliferation of prostate cancer cells through enhancement of androgen receptor transactivation

(2011) Seung-Jin Kim et al.   MOLECULES AND CELLS

Elevated Stearoyl-CoA Desaturase in Brains of Patients with Alzheimer's Disease

(2011) Giuseppe Astarita et al.   PLoS One

SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors

(2010) Yeeman K. Ramtohul et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

2-Aryl benzimidazoles: Human SCD1-specific stearoyl coenzyme-A desaturase inhibitors

(2010) David A. Powell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors

(2010) Elise Isabel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Stearoyl-coenzyme A desaturase 1 inhibition and the metabolic syndrome: considerations for future drug discovery

(2010) J Mark Brown et al.   CURRENT OPINION IN LIPIDOLOGY

Recent Advances in Stearoyl-CoA Desaturase 1 Inhibitors for Dyslipidemia and Obesity

(2010) Gang Liu   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Hepatic OATP and OCT uptake transporters: their role for drug-drug interactions and pharmacogenetic aspects

(2010) Christina Fahrmayr et al.   DRUG METABOLISM REVIEWS

Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1′-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3,4-dihydrospiro[chromene-2,4′-piperidine] analogs

(2010) Yoshikazu Uto et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel substituted heteroaromatic compounds as inhibitors of stearoyl-CoA desaturase

(2010) Pawel Dobrzyn et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Genetic variation in lipid desaturases and its impact on the development of human disease

(2010) Diana M Merino et al.   Lipids in Health and Disease

Rapamycin Regulates Stearoyl CoA Desaturase 1 Expression in Breast Cancer

(2010) D. Luyimbazi et al.   MOLECULAR CANCER THERAPEUTICS

Inhibition of StearoylCoA Desaturase Activity Blocks Cell Cycle Progression and Induces Programmed Cell Death in Lung Cancer Cells

(2010) Daniel Hess et al.   PLoS One

Lipid oversupply, selective insulin resistance, and lipotoxicity: Molecular mechanisms

(2009) Jose Antonio Chavez et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Thiazole analog as stearoyl-CoA desaturase 1 inhibitor

(2009) Chun Sing Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors

(2009) Dmitry O. Koltun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide

(2009) Yoshikazu Uto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors

(2009) Dmitry O. Koltun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part II: Identification of 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide and its biological evaluation

(2009) Yoshikazu Uto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors

(2009) Dmitry O. Koltun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel benzoylpiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-ylethyl)amide and its plasma triglyceride-lowering effects in Zucker fatty rats

(2009) Yoshikazu Uto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438)

(2009) Serge Léger et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel spiropiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 1′-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-5-(trifluoromethyl)-3,4-dihydrospiro[chromene-2,4′-piperidine]

(2009) Yoshikazu Uto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacological inhibition of Stearoyl-CoA Desaturase 1 improves insulin sensitivity in insulin-resistant rat models

(2009) Marc Issandou et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Azacycloalkane derivatives as inhibitors of delta-9 stearoyl-coenzyme A desaturase

(2009) Gang Liu   EXPERT OPINION ON THERAPEUTIC PATENTS

Stearoyl-CoA desaturase inhibitors: update on patented compounds

(2009) Gang Liu   EXPERT OPINION ON THERAPEUTIC PATENTS

Inhibition of StearoylCoA Desaturase-1 Inactivates Acetyl-CoA Carboxylase and Impairs Proliferation in Cancer Cells: Role of AMPK

(2009) Natalia Scaglia et al.   PLoS One

Association of Stearoyl-CoA Desaturase 1 Activity With Familial Combined Hyperlipidemia

(2008) Rebecca Mar-Heyming et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

(2008) Zhili Xin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of Stearoyl-Coenzyme A Desaturase 1 Dissociates Insulin Resistance and Obesity From Atherosclerosis

(2008) J. Mark Brown et al.   CIRCULATION

Comparison of pig, sheep and chicken SCD5 homologs: Evidence for an early gene duplication event

(2008) Andrea J. Lengi et al.   COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY B-BIOCHEMISTRY & MOLECULAR BIOLOGY

Low hepatic stearoyl-CoA desaturase 1 activity is associated with fatty liver and insulin resistance in obese humans

(2008) N. Stefan et al.   DIABETOLOGIA