Unearthing the Janus-face cholesterogenesis pathways in cancer

Identification of novel human Wnt target genes using adult endodermal tissue-derived organoids

(2021) Kim Elisabeth Boonekamp et al.   DEVELOPMENTAL BIOLOGY

Twin enzymes, divergent control: The cholesterogenic enzymes DHCR14 and LBR are differentially regulated transcriptionally and post-translationally

(2020) Isabelle M. Capell-Hattam et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lipid rafts as signaling hubs in cancer cell survival/death and invasion: implications in tumor progression and therapy

(2020) Faustino Mollinedo et al.   JOURNAL OF LIPID RESEARCH

NAD(P)-dependent steroid dehydrogenase-like is involved in breast cancer cell growth and metastasis

(2020) So-Hyun Yoon et al.   BMC CANCER

A Medicinal Chemistry-Driven Approach Identified the Sterol Isomerase EBP as the Molecular Target of TASIN Colorectal Cancer Toxins

(2020) Panayotis C. Theodoropoulos et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structure of nevanimibe-bound tetrameric human ACAT1

(2020) Tao Long et al.   NATURE

A key mammalian cholesterol synthesis enzyme, squalene monooxygenase, is allosterically stabilized by its substrate

(2020) Hiromasa Yoshioka et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cholesterol Homeostasis Modulates Platinum Sensitivity in Human Ovarian Cancer

(2020) Daniela Criscuolo et al.   Cells

Neuro‐oxysterols and neuro‐sterols as ligands to nuclear receptors, GPCRs, ligand‐gated ion channels and other protein receptors

(2020) Yuqin Wang et al.   BRITISH JOURNAL OF PHARMACOLOGY

Sterol synthesis pathway inhibition as a target for cancer treatment

(2020) Sara Feltrin et al.   CANCER LETTERS

24‐Dehydrocholesterol reductase promotes the growth of breast cancer stem‐like cells through the Hedgehog pathway

(2020) Ting Qiu et al.   CANCER SCIENCE

Lipid composition of the cancer cell membrane

(2020) Wojciech Szlasa et al.   JOURNAL OF BIOENERGETICS AND BIOMEMBRANES

Quality Control of ER Membrane Proteins by the RNF185/Membralin Ubiquitin Ligase Complex

(2020) Michael L. van de Weijer et al.   MOLECULAR CELL

Novel variant in NSDHL gene associated with CHILD syndrome and syndactyly- a case report

(2020) D. Hettiarachchi et al.   BMC Medical Genetics

Genkwadaphnin inhibits growth and invasion in hepatocellular carcinoma by blocking DHCR24-mediated cholesterol biosynthesis and lipid rafts formation

(2020) Jie Wu et al.   BRITISH JOURNAL OF CANCER

Cholesterol Pathway Inhibition Induces TGF-β Signaling to Promote Basal Differentiation in Pancreatic Cancer

(2020) Linara Gabitova-Cornell et al.   CANCER CELL

Reduction of squalene epoxidase by cholesterol accumulation accelerates colorectal cancer progression and metastasis.

(2020) Soo Young Jun et al.   GASTROENTEROLOGY

Post-translational control of the long and winding road to cholesterol

(2020) Laura J. Sharpe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Role of cholesterol metabolism in the anticancer pharmacology of selective estrogen receptor modulators

(2020) Diego Gómez-Coronado et al.   SEMINARS IN CANCER BIOLOGY

The E3 ubiquitin ligase MARCHF6 as a metabolic integrator in cholesterol synthesis and beyond

(2020) Nicola A. Scott et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Pleiotropic effects of statins: A focus on cancer

(2020) Mazaher Ahmadi et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

The effect of statin treatment on intratumoral cholesterol levels and LDL receptor expression: a window-of-opportunity breast cancer trial

(2020) Maria Feldt et al.   Cancer & Metabolism

Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

(2019) Anil K. Padyana et al.   Nature Communications

A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition

(2019) Christopher E. Mahoney et al.   Nature Communications

Squalene epoxidase promotes the proliferation and metastasis of lung squamous cell carcinoma cells though extracellular signal-regulated kinase signaling

(2019) Hong Ge et al.   Thoracic Cancer

The shape of human squalene epoxidase expands the arsenal against cancer

(2019) Andrew J. Brown et al.   Nature Communications

Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC)

(2019) Wentian Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis for human sterol isomerase in cholesterol biosynthesis and multidrug recognition

(2019) Tao Long et al.   Nature Communications

A nematode sterol C4α-methyltransferase catalyzes a new methylation reaction responsible for sterol diversity.

(2019) Wenxu Zhou et al.   JOURNAL OF LIPID RESEARCH

Evolution of the Cholesterol Biosynthesis Pathway in Animals

(2019) Tingting Zhang et al.   MOLECULAR BIOLOGY AND EVOLUTION

Follicular fluid meiosis-activating sterol (FF-MAS) promotes meiotic resumption via the MAPK pathway in porcine oocytes

(2019) Ruijie Guo et al.   THERIOGENOLOGY

Cholesterol accessibility at the ciliary membrane controls hedgehog signaling

(2019) Maia Kinnebrew et al.   eLife

Importance of genetic background of oxysterol signaling in cancer

(2018) P. Holy et al.   BIOCHIMIE

Statins Synergize with Hedgehog Pathway Inhibitors for Treatment of Medulloblastoma

(2018) Renata E. Gordon et al.   CLINICAL CANCER RESEARCH

Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture

(2018) Tatsuya Usui et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Report of the relapsed/refractory cohort of SWOG S0919: A phase 2 study of idarubicin and cytarabine in combination with pravastatin for acute myelogenous leukemia (AML)

(2018) Anjali S. Advani et al.   LEUKEMIA RESEARCH

Synthesis and Biological Activity of Sterol 14α-Demethylase and Sterol C24-Methyltransferase Inhibitors

(2018) David Leaver   MOLECULES

C-4 sterol demethylation enzymes distinguish bacterial and eukaryotic sterol synthesis

(2018) Alysha K. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Squalene epoxidase drives NAFLD-induced hepatocellular carcinoma and is a pharmaceutical target

(2018) Dabin Liu et al.   Science Translational Medicine

Dichlorophenyl piperazines, including a recently-approved atypical antipsychotic, are potent inhibitors of DHCR7, the last enzyme in cholesterol biosynthesis

(2018) Thiago C. Genaro-Mattos et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

The sterol-responsive RNF145 E3 ubiquitin ligase mediates the degradation of HMG-CoA reductase together with gp78 and Hrd1

(2018) Sam A Menzies et al.   eLife

The Effect of Statin Added to Systemic Anticancer Therapy: A Meta-Analysis of Randomized, Controlled Trials

(2018) Hyun Jang et al.   Journal of Clinical Medicine

New chemotype of selective and potent inhibitors of human delta 24-dehydrocholesterol reductase

(2017) Christoph Müller et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Multicenter, Phase III, Randomized, Double-Blind, Placebo-Controlled Trial of Pravastatin Added to First-Line Standard Chemotherapy in Small-Cell Lung Cancer (LUNGSTAR)

(2017) Michael J. Seckl et al.   JOURNAL OF CLINICAL ONCOLOGY

Dendrogenin A drives LXR to trigger lethal autophagy in cancers

(2017) Gregory Segala et al.   Nature Communications

Cholesterol Synthetase DHCR24 Induced by Insulin Aggravates Cancer Invasion and Progesterone Resistance in Endometrial Carcinoma

(2017) Miao Dai et al.   Scientific Reports

Cholesterol Biosynthesis: A Mechanistic Overview

(2016) Nuno M. F. S. A. Cerqueira et al.   BIOCHEMISTRY

The Role of Cholesterol in Cancer

(2016) Omer F. Kuzu et al.   CANCER RESEARCH

Cholesterol-mediated Degradation of 7-Dehydrocholesterol Reductase Switches the Balance from Cholesterol to Vitamin D Synthesis

(2016) Anika V. Prabhu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Human sterol 14α-demethylase as a target for anticancer chemotherapy: towards structure-aided drug design

(2016) Tatiana Y. Hargrove et al.   JOURNAL OF LIPID RESEARCH

The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts

(2016) Zeljka Korade et al.   JOURNAL OF MEDICINAL CHEMISTRY

Investigation of 7-dehydrocholesterol reductase pathway to elucidate off-target prenatal effects of pharmaceuticals: a systematic review

(2016) M R Boland et al.   PHARMACOGENOMICS JOURNAL

Endogenous B-ring oxysterols inhibit the Hedgehog component Smoothened in a manner distinct from cyclopamine or side-chain oxysterols

(2016) Navdar Sever et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer

(2016) L. Zhang et al.   Science Translational Medicine

The Lamin B receptor is essential for cholesterol synthesis and perturbed by disease-causing mutations

(2016) Pei-Ling Tsai et al.   eLife

Squalene epoxidase is a bona fide oncogene by amplification with clinical relevance in breast cancer

(2016) David N. Brown et al.   Scientific Reports

A randomised, double-blind, placebo-controlled multi-centre phase III trial of XELIRI/FOLFIRI plus simvastatin for patients with metastatic colorectal cancer

(2015) S H Lim et al.   BRITISH JOURNAL OF CANCER

Identification of Natural RORγ Ligands that Regulate the Development of Lymphoid Cells

(2015) Fabio R. Santori et al.   Cell Metabolism

Oocyte Induction of EGF Responsiveness in Somatic Cells Is Associated With the Acquisition of Porcine Oocyte Developmental Competence

(2015) Lesley J. Ritter et al.   ENDOCRINOLOGY

Farnesyl Diphosphate Synthase Inhibitors With Unique Ligand-Binding Geometries

(2015) Yi-Liang Liu et al.   ACS Medicinal Chemistry Letters

The loss of Tm7sf gene accelerates skin papilloma formation in mice

(2015) I. Bellezza et al.   Scientific Reports

Identification of NPC1 as the target of U18666A, an inhibitor of lysosomal cholesterol export and Ebola infection

(2015) Feiran Lu et al.   eLife

Disorders of Cholesterol Metabolism and Their Unanticipated Convergent Mechanisms of Disease

(2014) Frances M. Platt et al.   Annual Review of Genomics and Human Genetics

Genkwadaphnin induces reactive oxygen species (ROS)-mediated apoptosis of squamous cell carcinoma (SCC) cells

(2014) Zheng Jun Li et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Squalene mono-oxygenase, a key enzyme in cholesterol synthesis, is stabilized by unsaturated fatty acids

(2014) Julian Stevenson et al.   BIOCHEMICAL JOURNAL

Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071

(2014) Yayun Liang et al.   BREAST CANCER RESEARCH AND TREATMENT

SWOG0919: a Phase 2 study of idarubicin and cytarabine in combination with pravastatin for relapsed acute myeloid leukaemia

(2014) Anjali S. Advani et al.   BRITISH JOURNAL OF HAEMATOLOGY

On the formation of 7-ketocholesterol from 7-dehydrocholesterol in patients with CTX and SLO

(2014) Ingemar Björkhem et al.   JOURNAL OF LIPID RESEARCH

The E3 Ubiquitin Ligase MARCH6 Degrades Squalene Monooxygenase and Affects 3-Hydroxy-3-Methyl-Glutaryl Coenzyme A Reductase and the Cholesterol Synthesis Pathway

(2014) N. Zelcer et al.   MOLECULAR AND CELLULAR BIOLOGY

Cholesterol synthesis inhibitor RO 48-8071 suppresses transcriptional activity of human estrogen and androgen receptor

(2014) BENFORD MAFUVADZE et al.   ONCOLOGY REPORTS

Taxodione and arenarone inhibit farnesyl diphosphate synthase by binding to the isopentenyl diphosphate site

(2014) Y.-L. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cholesterol and Cancer, in the Balance

(2014) S. Silvente-Poirot et al.   SCIENCE

Targeting of Smoothened for therapeutic gain

(2014) Martial Ruat et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Cholesterol selectively activates canonical Wnt signalling over non-canonical Wnt signalling

(2014) Ren Sheng et al.   Nature Communications

Structure of human farnesyl pyrophosphate synthase in complex with an aminopyridine bisphosphonate and two molecules of inorganic phosphate

(2014) Jaeok Park et al.   Acta Crystallographica Section F-Structural Biology Communications

Flavin dependent monooxygenases

(2013) Mieke M.E. Huijbers et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Oxysterols in cancer cell proliferation and death

(2013) Jan de Weille et al.   BIOCHEMICAL PHARMACOLOGY

Randomized double-blinded, placebo-controlled phase II trial of simvastatin and gemcitabine in advanced pancreatic cancer patients

(2013) Jung Yong Hong et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Purification, kinetics, inhibitors and CD for recombinant β-amyrin synthase fromEuphorbia tirucalli L and functional analysis of the DCTA motif, which is highly conserved among oxidosqualene cyclases

(2013) Ryousuke Ito et al.   FEBS Journal

Controlling Cholesterol Synthesis beyond 3-Hydroxy-3-methylglutaryl-CoA Reductase (HMGCR)

(2013) Laura J. Sharpe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Signaling regulates activity of DHCR24, the final enzyme in cholesterol synthesis

(2013) Winnie Luu et al.   JOURNAL OF LIPID RESEARCH

A Novel Role for Tm7sf2 Gene in Regulating TNFα Expression

(2013) Ilaria Bellezza et al.   PLoS One

Triparanol suppresses human tumor growth in vitro and in vivo

(2012) Xinyu Bi et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Cytotoxic Effects of Combination of Oxidosqualene Cyclase Inhibitors with Atorvastatin in Human Cancer Cells

(2012) Davide Staedler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Active Site Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Apoptosis and Inhibition of ERK Phosphorylation in Multiple Myeloma Cells

(2012) Yih-Shyan Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Differential regulation of HMG-CoA reductase and Insig-1 by enzymes of the ubiquitin-proteasome system

(2012) Yien Che Tsai et al.   MOLECULAR BIOLOGY OF THE CELL

Targeting C4-Demethylating Genes in the Cholesterol Pathway Sensitizes Cancer Cells to EGF Receptor Inhibitors via Increased EGF Receptor Degradation

(2012) Anna Sukhanova et al.   Cancer Discovery

Cholesterol-Dependent Degradation of Squalene Monooxygenase, a Control Point in Cholesterol Synthesis beyond HMG-CoA Reductase

(2011) Saloni Gill et al.   Cell Metabolism

Biosynthesis of Cholesterol and Other Sterols

(2011) W. David Nes   CHEMICAL REVIEWS

A Randomized Phase II Study of Gefitinib Plus Simvastatin Versus Gefitinib Alone in Previously Treated Patients with Advanced Non–Small Cell Lung Cancer

(2011) Ji-Youn Han et al.   CLINICAL CANCER RESEARCH

Substrate Preferences and Catalytic Parameters Determined by Structural Characteristics of Sterol 14α-Demethylase (CYP51) fromLeishmania infantum

(2011) Tatiana Y. Hargrove et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lamin B Receptor Regulates the Growth and Maturation of Myeloid Progenitors via its Sterol Reductase Domain: Implications for Cholesterol Biosynthesis in Regulating Myelopoiesis

(2011) G. Subramanian et al.   JOURNAL OF IMMUNOLOGY

Structural complex of sterol 14α-demethylase (CYP51) with 14α-methylenecyclopropyl-Δ7-24, 25-dihydrolanosterol

(2011) Tatiana Y. Hargrove et al.   JOURNAL OF LIPID RESEARCH

DHCEO accumulation is a critical mediator of pathophysiology in a Smith–Lemli–Opitz syndrome model

(2011) Libin Xu et al.   NEUROBIOLOGY OF DISEASE

Sterol-induced degradation of HMG CoA reductase depends on interplay of two Insigs and two ubiquitin ligases, gp78 and Trc8

(2011) Y. Jo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Contemporary experience with ketoconazole in patients with metastatic castration-resistant prostate cancer: Clinical factors associated with PSA response and disease progression

(2011) Daniel Keizman et al.   PROSTATE

Hypomorphic Temperature-Sensitive Alleles of NSDHL Cause CK Syndrome

(2010) Keith W. McLarren et al.   AMERICAN JOURNAL OF HUMAN GENETICS

Lovastatin induces apoptosis of ovarian cancer cells and synergizes with doxorubicin: potential therapeutic relevance

(2010) Anna Martirosyan et al.   BMC CANCER

The addition of pravastatin to chemotherapy in advanced gastric carcinoma: A randomised phase II trial

(2010) Inge R.H.M. Konings et al.   EUROPEAN JOURNAL OF CANCER

Biological activities of 7-dehydrocholesterol-derived oxysterols: implications for Smith-Lemli-Opitz syndrome

(2010) Zeljka Korade et al.   JOURNAL OF LIPID RESEARCH

Crystal Structures of Human HMG-CoA Synthase Isoforms Provide Insights into Inherited Ketogenesis Disorders and Inhibitor Design

(2010) Naeem Shafqat et al.   JOURNAL OF MOLECULAR BIOLOGY

Structural Basis of Human CYP51 Inhibition by Antifungal Azoles

(2010) Natallia Strushkevich et al.   JOURNAL OF MOLECULAR BIOLOGY

Oxysterols from Free Radical Chain Oxidation of 7-Dehydrocholesterol: Product and Mechanistic Studies

(2010) Libin Xu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery

(2010) Wolfgang Jahnke et al.   Nature Chemical Biology

Identification and pharmacological characterization of cholesterol-5,6-epoxide hydrolase as a target for tamoxifen and AEBS ligands

(2010) P. de Medina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tamoxifen and AEBS ligands induced apoptosis and autophagy in breast cancer cells through the stimulation of sterol accumulation

(2009) Philippe de Medina et al.   Autophagy

The oxysterol receptor LXR inhibits proliferation of human breast cancer cells

(2009) Lise-Lotte Vedin et al.   CARCINOGENESIS

Ligands of the antiestrogen-binding site induce active cell death and autophagy in human breast cancer cells through the modulation of cholesterol metabolism

(2009) P de Medina et al.   CELL DEATH AND DIFFERENTIATION

Cholesterol Synthesis Inhibitor U18666A and the Role of Sterol Metabolism and Trafficking in Numerous Pathophysiological Processes

(2009) Richard J. Cenedella   LIPIDS

Human mevalonate diphosphate decarboxylase: Characterization, investigation of the mevalonate diphosphate binding site, and crystal structure

(2008) Natalia E. Voynova et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Biochemical and Structural Basis for Feedback Inhibition of Mevalonate Kinase and Isoprenoid Metabolism†,‡

(2008) Zhuji Fu et al.   BIOCHEMISTRY

A phase II clinical trial does not show that high dose simvastatin has beneficial effect on markers of bone turnover in multiple myeloma

(2008) TE Sondergaard et al.   HEMATOLOGICAL ONCOLOGY

Involvement of mitogen-activated protein kinase (MAPK) pathway in LH- and meiosis-activating sterol (MAS)-induced maturation in rat and mouse oocytes

(2008) Shmulik Motola et al.   MOLECULAR REPRODUCTION AND DEVELOPMENT

Crystal structure of human phosphomavelonate kinase at 1.8 Å resolution

(2008) Qing Chang et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS