Development of small-molecule PCSK9 inhibitors for the treatment of hypercholesterolemia
出版年份 2022 全文链接
标题
Development of small-molecule PCSK9 inhibitors for the treatment of hypercholesterolemia
作者
关键词
Atherosclerosis, Low-density lipoprotein-cholesterol, PCSK9 inhibitors, Small-molecule drugs, Protein–protein interaction inhibitors
出版物
DRUG DISCOVERY TODAY
Volume -, Issue -, Pages -
出版商
Elsevier BV
发表日期
2022-02-02
DOI
10.1016/j.drudis.2022.01.014
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Sesquiterpenoids from the Aerial Parts of Salvia plebeia with Inhibitory Activities on Proprotein Convertase Subtilisin/Kexin Type 9 Expression
- (2021) Piseth Nhoek et al. JOURNAL OF NATURAL PRODUCTS
- Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells
- (2021) Jagadeesh Nagarajappa Masagalli et al. MOLECULES
- Structure–activity relationship and biological evaluation of berberine derivatives as PCSK9 down-regulating agents
- (2021) Tian–Yun Fan et al. BIOORGANIC CHEMISTRY
- Dilignans with a Chromanol Motif Discovered by Molecular Networking from the Stem Barks of Magnolia obovata and Their Proprotein Convertase Subtilisin/Kexin Type 9 Expression Inhibitory Activity
- (2021) Jongmin Ahn et al. Biomolecules
- Role of PCSK9 Inhibitors in Patients with Familial Hypercholesterolemia
- (2021) Brian Tomlinson et al. Endocrinology and Metabolism
- Prenylated Flavonoid Glycosides with PCSK9 mRNA Expression Inhibitory Activity from the Aerial Parts of Epimedium koreanum
- (2021) Eeray Kim et al. MOLECULES
- Identification of neolignans with PCSK9 downregulatory and LDLR upregulatory activities from Penthorum chinense and the potential in cholesterol uptake by transcriptional regulation of LDLR via SREBP2
- (2021) Hee-Sung Chae et al. JOURNAL OF ETHNOPHARMACOLOGY
- A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove
- (2020) Benny J. Evison et al. BIOORGANIC & MEDICINAL CHEMISTRY
- A small-molecule inhibitor of PCSK9 transcription ameliorates atherosclerosis through the modulation of FoxO1/3 and HNF1α
- (2020) Xuelei Wang et al. EBioMedicine
- Aloe-emodin exerts cholesterol-lowering effects by inhibiting proprotein convertase subtilisin/kexin type 9 in hyperlipidemic rats
- (2020) Zhen-li Su et al. ACTA PHARMACOLOGICA SINICA
- Beneficial impact of epigallocatechingallate on LDL-C through PCSK9/LDLR pathway by blocking HNF1α and activating FoxO3a
- (2020) Chuan-Jue Cui et al. Journal of Translational Medicine
- From Methylene Bridged Diindole to Carbonyl Linked Benzimidazoleindole: Development of Potent and Metabolically Stable PCSK9 Modulators
- (2020) Haibo Xie et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Pseurotin A as a novel suppressor of hormone dependent breast cancer progression and recurrence by inhibiting PCSK9 secretion and interaction with LDL receptor
- (2020) Khaldoun S. Abdelwahed et al. PHARMACOLOGICAL RESEARCH
- Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) in the Brain and Relevance for Neuropsychiatric Disorders
- (2020) Emma M. O’Connell et al. Frontiers in Neuroscience
- Ascorbic acid enhances low-density lipoprotein receptor expression by suppressing proprotein convertase subtilisin/kexin 9 expression
- (2020) Dandan Wang et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Lipid-Lowering Activities of Cucurbitacins Isolated from Trichosanthes cucumeroides and Their Synthetic Derivatives
- (2020) Xianjing Zhang et al. JOURNAL OF NATURAL PRODUCTS
- In vivo genome and base editing of a human PCSK9 knock-in hypercholesterolemic mouse model
- (2019) Alba Carreras et al. BMC BIOLOGY
- Lipoprotein(a), PCSK9 Inhibition and Cardiovascular Risk: Insights from the FOURIER Trial
- (2019) Michelle L. O'Donoghue et al. CIRCULATION
- Pretreatment With PCSK9 Inhibitor Protects the Brain Against Cardiac Ischemia/Reperfusion Injury Through a Reduction of Neuronal Inflammation and Amyloid Beta Aggregation
- (2019) Nattayaporn Apaijai et al. Journal of the American Heart Association
- Prenylated Flavonoids from the Roots and Rhizomes of Sophora tonkinensis and Their Effects on the Expression of Inflammatory Mediators and Proprotein Convertase Subtilisin/Kexin Type 9
- (2019) Jongmin Ahn et al. JOURNAL OF NATURAL PRODUCTS
- Proprotein Convertase Subtilisin/Kexin Type 9, Brain Cholesterol Homeostasis and Potential Implication for Alzheimer’s Disease
- (2019) Maria Pia Adorni et al. Frontiers in Aging Neuroscience
- 23,24-Dihydrocucurbitacin B promotes lipid clearance by dual transcriptional regulation of LDLR and PCSK9
- (2019) Hui-hui Li et al. ACTA PHARMACOLOGICA SINICA
- Discovery of 2,3′-diindolylmethanes as a novel class of PCSK9 modulators
- (2019) Gabrielle N. Winston-McPherson et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Computationally Driven Structure Optimization, Synthesis, and Biological Evaluation of Imidazole-Based Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) Inhibitors
- (2019) Carmen Lammi et al. JOURNAL OF MEDICINAL CHEMISTRY
- Design, synthesis, and biological evaluation of novel tetrahydroprotoberberine derivatives (THPBs) as proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators for the treatment of hyperlipidemia
- (2019) Chenglin Wu et al. Acta Pharmaceutica Sinica B
- Fragment-based design of small molecule PCSK9 inhibitors using simulated annealing of chemical potential simulations
- (2019) Frank Guarnieri et al. PLoS One
- Zebrafish-Based Discovery of Antiseizure Compounds from the Red Sea: Pseurotin A2 and Azaspirofuran A
- (2018) Daniëlle Copmans et al. ACS Chemical Neuroscience
- Small molecule modulators of PCSK9 – A literature and patent overview
- (2018) Daniel Pettersen et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Therapeutic potential of quercetin as a cardiovascular agent
- (2018) Rahul V. Patel et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Pinostrobin Inhibits Proprotein Convertase Subtilisin/Kexin-type 9 (PCSK9) Gene Expression through the Modulation of FoxO3a Protein in HepG2 Cells
- (2018) Wan-Yun Gao et al. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
- Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents
- (2018) Allyn T. Londregan et al. JOURNAL OF MEDICINAL CHEMISTRY
- Generation and Characterization of a Novel Small Biologic Alternative to Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Antibodies, DS-9001a, Albumin Binding Domain–Fused Anticalin Protein
- (2018) Yusuke Masuda et al. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
- Small Molecule Inhibitors of the PCSK9·LDLR Interaction
- (2018) Jaru Taechalertpaisarn et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Discovery of Flavonoids from Scutellaria baicalensis with Inhibitory Activity Against PCSK 9 Expression: Isolation, Synthesis and Their Biological Evaluation
- (2018) Piseth Nhoek et al. MOLECULES
- Naringin Activates AMPK Resulting in Altered Expression of SREBPs, PCSK9, and LDLR To Reduce Body Weight in Obese C57BL/6J Mice
- (2018) Guo-Guang Sui et al. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
- Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9
- (2018) Allyn T. Londregan et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Small molecules as inhibitors of PCSK9: Current status and future challenges
- (2018) Shengtao Xu et al. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- The AT04A vaccine against proprotein convertase subtilisin/kexin type 9 reduces total cholesterol, vascular inflammation, and atherosclerosis in APOE*3Leiden.CETP mice
- (2017) Christine Landlinger et al. EUROPEAN HEART JOURNAL
- New Aromatic Compounds from the Fruiting Body of Sparassis crispa (Wulf.) and Their Inhibitory Activities on Proprotein Convertase Subtilisin/Kexin Type 9 mRNA Expression
- (2017) Sunghee Bang et al. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
- Safety of Very Low Low-Density Lipoprotein Cholesterol Levels With Alirocumab
- (2017) Jennifer G. Robinson et al. JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY
- Global, regional, and national age-sex specific mortality for 264 causes of death, 1980–2016: a systematic analysis for the Global Burden of Disease Study 2016
- (2017) Mohsen Naghavi et al. LANCET
- Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease
- (2017) Marc S. Sabatine et al. NEW ENGLAND JOURNAL OF MEDICINE
- Lipid-Reduction Variability and Antidrug-Antibody Formation with Bococizumab
- (2017) Paul M Ridker et al. NEW ENGLAND JOURNAL OF MEDICINE
- Inclisiran in Patients at High Cardiovascular Risk with Elevated LDL Cholesterol
- (2017) Kausik K. Ray et al. NEW ENGLAND JOURNAL OF MEDICINE
- Inhibiting Translation One Protein at a Time
- (2017) Matthew D. Disney TRENDS IN BIOCHEMICAL SCIENCES
- Heparan sulfate proteoglycans present PCSK9 to the LDL receptor
- (2017) Camilla Gustafsen et al. Nature Communications
- Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain
- (2017) Nathanael G. Lintner et al. PLOS BIOLOGY
- A Phase I Randomized Study of a Specifically Engineered, pH-Sensitive PCSK9 Inhibitor RN317 (PF-05335810) in Hypercholesterolemic Subjects on Statin Therapy
- (2016) M Levisetti et al. CTS-Clinical and Translational Science
- Safety and efficacy of LY3015014, a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 (PCSK9): a randomized, placebo-controlled Phase 2 study
- (2016) John J.P. Kastelein et al. EUROPEAN HEART JOURNAL
- Association Between Lowering LDL-C and Cardiovascular Risk Reduction Among Different Therapeutic Interventions
- (2016) Michael G. Silverman et al. JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION
- Disrupting the PCSK9/LDLR protein–protein interaction by an imidazole-based minimalist peptidomimetic
- (2016) Mattia Stucchi et al. ORGANIC & BIOMOLECULAR CHEMISTRY
- Population Pharmacokinetics (PK) and Pharmacodynamics (PD) Analysis of LY3015014, a Monoclonal Antibody to Protein Convertase Subtilisin/Kexin Type 9 (PCSK9) in Healthy Subjects and Hypercholesterolemia Patients
- (2016) Tong Shen et al. PHARMACEUTICAL RESEARCH
- Divergent Reactivity of Rhodium(I) Carbenes Derived from Indole Annulations
- (2015) Xiaoxun Li et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Position paper Statin intolerance – an attempt at a unified definition. Position paper from an International Lipid Expert Panel
- (2015) Maciej Banach et al. Archives of Medical Science
- Proprotein Convertase Subtilisin/Kexin Type 9 Inhibition
- (2015) Nathalie Bergeron et al. CIRCULATION
- Lipoprotein(a) Catabolism Is Regulated by Proprotein Convertase Subtilisin/Kexin Type 9 through the Low Density Lipoprotein Receptor
- (2015) Rocco Romagnuolo et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Inhibition of PCSK9 with evolocumab in homozygous familial hypercholesterolaemia (TESLA Part B): a randomised, double-blind, placebo-controlled trial
- (2015) Frederick J Raal et al. LANCET
- Metabolites Produced by the Endophytic Fungus Aspergillus fumigatus from the Stem of Erythrophloeum fordii Oliv.
- (2015) Yu-Sheng Shi et al. MOLECULES
- Efficacy and Safety of Alirocumab in Reducing Lipids and Cardiovascular Events
- (2015) Jennifer G. Robinson et al. NEW ENGLAND JOURNAL OF MEDICINE
- Application of the Ugi reaction with multiple amino acid-derived components: synthesis and conformational evaluation of piperazine-based minimalist peptidomimetics
- (2015) Mattia Stucchi et al. ORGANIC & BIOMOLECULAR CHEMISTRY
- Effect of Alirocumab, a Monoclonal Proprotein Convertase Subtilisin/Kexin 9 Antibody, on Lipoprotein(a) Concentrations (a Pooled Analysis of 150 mg Every Two Weeks Dosing from Phase 2 Trials)
- (2014) Daniel Gaudet et al. AMERICAN JOURNAL OF CARDIOLOGY
- Trial evaluating evolocumab, a pcsk9 antibody, in patients with homozygous fh (tesla): Results of the randomized, double-blind, placebo-controlled trial
- (2014) F. Raal et al. ATHEROSCLEROSIS
- Copper-catalyzed tandem annulation/arylation for the synthesis of diindolylmethanes from propargylic alcohols
- (2014) Hui Li et al. CHEMICAL COMMUNICATIONS
- Design and Synthesis of Truncated EGF-A Peptides that Restore LDL-R Recycling in the Presence of PCSK9 In Vitro
- (2014) Christina I. Schroeder et al. CHEMISTRY & BIOLOGY
- PCSK9
- (2014) Nabil G. Seidah et al. CIRCULATION RESEARCH
- Homozygous familial hypercholesterolaemia: new insights and guidance for clinicians to improve detection and clinical management. A position paper from the Consensus Panel on Familial Hypercholesterolaemia of the European Atherosclerosis Society
- (2014) M. Cuchel et al. EUROPEAN HEART JOURNAL
- Aloe-emodin from rhubarb (Rheum rhabarbarum) inhibits lipopolysaccharide-induced inflammatory responses in RAW264.7 macrophages
- (2014) Boyang Hu et al. JOURNAL OF ETHNOPHARMACOLOGY
- Reduction in Lipoprotein(a) With PCSK9 Monoclonal Antibody Evolocumab (AMG 145)
- (2014) Frederick J. Raal et al. JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY
- Peptide-Based Anti-PCSK9 Vaccines - An Approach for Long-Term LDLc Management
- (2014) Gergana Galabova et al. PLoS One
- Small molecule probes that perturb a protein–protein interface in antithrombin
- (2014) Dongyue Xin et al. Chemical Science
- Quercetin-3-glucoside increases low-density lipoprotein receptor (LDLR) expression, attenuates proprotein convertase subtilisin/kexin 9 (PCSK9) secretion, and stimulates LDL uptake by Huh7 human hepatocytes in culture
- (2014) Majambu Mbikay et al. FEBS Open Bio
- PCSK9 plays a significant role in cholesterol homeostasis and lipid transport in intestinal epithelial cells
- (2013) Emile Levy et al. ATHEROSCLEROSIS
- Immunity, atherosclerosis and cardiovascular disease
- (2013) Johan Frostegård BMC Medicine
- Effect of the Proprotein Convertase Subtilisin/Kexin 9 Monoclonal Antibody, AMG 145, in Homozygous Familial Hypercholesterolemia
- (2013) Evan A. Stein et al. CIRCULATION
- Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor
- (2013) Yingnan Zhang et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Platinum-Catalyzed Tandem Indole Annulation/Arylation for the Synthesis of Diindolylmethanes and Indolo[3,2-b]carbazoles
- (2013) Dongxu Shu et al. ORGANIC LETTERS
- Synthesis and cytotoxic activity evaluation of dihydrocucurbitacin B and cucurbitacin B derivatives
- (2012) Karen Luise Lang et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Genome-wide association study of genetic determinants of LDL-c response to atorvastatin therapy: importance of Lp(a)
- (2012) Harshal A. Deshmukh et al. JOURNAL OF LIPID RESEARCH
- Exploring Key Orientations at Protein–Protein Interfaces with Small Molecule Probes
- (2012) Eunhwa Ko et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- The biology and therapeutic targeting of the proprotein convertases
- (2012) Nabil G. Seidah et al. NATURE REVIEWS DRUG DISCOVERY
- Circulating Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) Regulates VLDLR Protein and Triglyceride Accumulation in Visceral Adipose Tissue
- (2011) Anna Roubtsova et al. ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY
- Triglycerides and Cardiovascular Disease
- (2011) Michael Miller et al. CIRCULATION
- Hyperlipidemia-Triggered Neutrophilia Promotes Early Atherosclerosis
- (2010) Maik Drechsler et al. CIRCULATION
- Lipoprotein(a) as a cardiovascular risk factor: current status
- (2010) Børge G. Nordestgaard et al. EUROPEAN HEART JOURNAL
- Efficacy and Safety of Rosuvastatin Therapy for Children With Familial Hypercholesterolemia
- (2010) Hans J. Avis et al. JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY
- Evaluation of the antitumoral effect of dihydrocucurbitacin-B in both in vitro and in vivo models
- (2009) Jarbas Mota Siqueira et al. CANCER CHEMOTHERAPY AND PHARMACOLOGY
- PCSK9 impedes hepatitis C virus infectionin vitroand modulates liver CD81 expression
- (2009) Patrick Labonté et al. HEPATOLOGY
- A randomized, multicentre, open-label, parallel-group trial to compare the efficacy and safety profile of daming capsule in patients with hypercholesterolemia
- (2009) Ai Jing et al. PHYTOTHERAPY RESEARCH
- Molecular basis of PCSK9 function
- (2008) Gilles Lambert et al. ATHEROSCLEROSIS
- Proprotein convertase subtilisin/kexin type 9 (PCSK9): Hepatocyte-specific low-density lipoprotein receptor degradation and critical role in mouse liver regeneration
- (2008) Ahmed Zaid et al. HEPATOLOGY
- Structural and Biochemical Characterization of the Wild Type PCSK9-EGF(AB) Complex and Natural Familial Hypercholesterolemia Mutants
- (2008) Matthew J. Bottomley et al. JOURNAL OF BIOLOGICAL CHEMISTRY
Find Funding. Review Successful Grants.
Explore over 25,000 new funding opportunities and over 6,000,000 successful grants.
ExploreFind the ideal target journal for your manuscript
Explore over 38,000 international journals covering a vast array of academic fields.
Search