Published in Arterioscler Thromb Vasc Biol on June 03, 2004
A spectrum of PCSK9 alleles contributes to plasma levels of low-density lipoprotein cholesterol. Am J Hum Genet (2006) 7.89
Molecular biology of PCSK9: its role in LDL metabolism. Trends Biochem Sci (2007) 3.59
A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates. Proc Natl Acad Sci U S A (2009) 3.39
The biology and therapeutic targeting of the proprotein convertases. Nat Rev Drug Discov (2012) 3.18
Overexpression of PCSK9 accelerates the degradation of the LDLR in a post-endoplasmic reticulum compartment. Proc Natl Acad Sci U S A (2005) 3.15
Serum proprotein convertase subtilisin/kexin type 9 and cell surface low-density lipoprotein receptor: evidence for a reciprocal regulation. Circulation (2013) 2.03
Genetic and metabolic determinants of plasma PCSK9 levels. J Clin Endocrinol Metab (2009) 1.95
Hepatocyte nuclear factor 1alpha plays a critical role in PCSK9 gene transcription and regulation by the natural hypocholesterolemic compound berberine. J Biol Chem (2009) 1.67
Antagonism of secreted PCSK9 increases low density lipoprotein receptor expression in HepG2 cells. J Biol Chem (2009) 1.65
A new method for measurement of total plasma PCSK9: clinical applications. J Lipid Res (2010) 1.64
High-dose atorvastatin causes a rapid sustained increase in human serum PCSK9 and disrupts its correlation with LDL cholesterol. J Lipid Res (2010) 1.56
Plasma PCSK9 levels are significantly modified by statins and fibrates in humans. Lipids Health Dis (2008) 1.56
The PCSK9 decade. J Lipid Res (2012) 1.50
Dissection of the endogenous cellular pathways of PCSK9-induced low density lipoprotein receptor degradation: evidence for an intracellular route. J Biol Chem (2009) 1.49
Strong induction of PCSK9 gene expression through HNF1alpha and SREBP2: mechanism for the resistance to LDL-cholesterol lowering effect of statins in dyslipidemic hamsters. J Lipid Res (2010) 1.36
Low density lipoprotein binds to proprotein convertase subtilisin/kexin type-9 (PCSK9) in human plasma and inhibits PCSK9-mediated low density lipoprotein receptor degradation. J Biol Chem (2013) 1.29
Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor. Biochem J (2009) 1.24
Lipoprotein(a) catabolism is regulated by proprotein convertase subtilisin/kexin type 9 through the low density lipoprotein receptor. J Biol Chem (2015) 1.24
Deletion of the gene encoding proprotein convertase 5/6 causes early embryonic lethality in the mouse. Mol Cell Biol (2006) 1.23
Pharmacological strategies for lowering LDL cholesterol: statins and beyond. Nat Rev Cardiol (2011) 1.20
A locked nucleic acid antisense oligonucleotide (LNA) silences PCSK9 and enhances LDLR expression in vitro and in vivo. PLoS One (2010) 1.19
Proprotein convertase subtilisin/kexin type 9 (PCSK9) can mediate degradation of the low density lipoprotein receptor-related protein 1 (LRP-1). PLoS One (2013) 1.18
In vivo evidence that furin from hepatocytes inactivates PCSK9. J Biol Chem (2010) 1.18
Atorvastatin increases intestinal expression of NPC1L1 in hyperlipidemic men. J Lipid Res (2010) 1.17
Self-association of human PCSK9 correlates with its LDLR-degrading activity. Biochemistry (2008) 1.16
An anti-PCSK9 antibody reduces LDL-cholesterol on top of a statin and suppresses hepatocyte SREBP-regulated genes. Int J Biol Sci (2012) 1.15
Statins and ezetimibe modulate plasma proprotein convertase subtilisin kexin-9 (PCSK9) levels. Trans Am Clin Climatol Assoc (2009) 1.09
Elevated PCSK9 levels in untreated patients with heterozygous or homozygous familial hypercholesterolemia and the response to high-dose statin therapy. J Am Heart Assoc (2013) 1.08
Annexin A2 is a natural extrahepatic inhibitor of the PCSK9-induced LDL receptor degradation. PLoS One (2012) 1.04
Longitudinal association of PCSK9 sequence variations with low-density lipoprotein cholesterol levels: the Coronary Artery Risk Development in Young Adults Study. Circ Cardiovasc Genet (2009) 1.04
Effects of currently prescribed LDL-C-lowering drugs on PCSK9 and implications for the next generation of LDL-C-lowering agents. Lipids Health Dis (2011) 1.03
PCSK9 function and physiology. J Lipid Res (2008) 1.03
Inflammation stimulates the expression of PCSK9. Biochem Biophys Res Commun (2008) 1.02
Chronic alcohol consumption disrupted cholesterol homeostasis in rats: down-regulation of low-density lipoprotein receptor and enhancement of cholesterol biosynthesis pathway in the liver. Alcohol Clin Exp Res (2009) 1.02
Proprotein convertase subtilisin/kexin type 9 deficiency reduces melanoma metastasis in liver. Neoplasia (2012) 1.02
Furin is the major processing enzyme of the cardiac-specific growth factor bone morphogenetic protein 10. J Biol Chem (2011) 0.99
Indices of cholesterol metabolism and relative responsiveness to ezetimibe and simvastatin. J Clin Endocrinol Metab (2009) 0.99
New therapeutic principles in dyslipidaemia: focus on LDL and Lp(a) lowering drugs. Eur Heart J (2013) 0.96
Nutraceutical pill containing berberine versus ezetimibe on plasma lipid pattern in hypercholesterolemic subjects and its additive effect in patients with familial hypercholesterolemia on stable cholesterol-lowering treatment. Lipids Health Dis (2012) 0.95
Amyloid Precursor-like Protein 2 and Sortilin Do Not Regulate the PCSK9 Convertase-mediated Low Density Lipoprotein Receptor Degradation but Interact with Each Other. J Biol Chem (2015) 0.95
Surface expression of precursor N-cadherin promotes tumor cell invasion. Neoplasia (2010) 0.95
The biology of PCSK9 from the endoplasmic reticulum to lysosomes: new and emerging therapeutics to control low-density lipoprotein cholesterol. Drug Des Devel Ther (2013) 0.94
Alirocumab inhibits atherosclerosis, improves the plaque morphology, and enhances the effects of a statin. J Lipid Res (2014) 0.94
Janus kinase activation by cytokine oncostatin M decreases PCSK9 expression in liver cells. J Lipid Res (2010) 0.93
Fenofibrate treatment increases human serum proprotein convertase subtilisin kexin type 9 levels. J Lipid Res (2009) 0.93
PCSK9 reduces the protein levels of the LDL receptor in mouse brain during development and after ischemic stroke. J Lipid Res (2011) 0.93
PCSK9 function and physiology. J Lipid Res (2008) 0.92
PCSK9 and LDLR degradation: regulatory mechanisms in circulation and in cells. Curr Opin Lipidol (2014) 0.91
CETP inhibitors downregulate hepatic LDL receptor and PCSK9 expression in vitro and in vivo through a SREBP2 dependent mechanism. Atherosclerosis (2014) 0.91
Evidence from a randomized trial that simvastatin, but not ezetimibe, upregulates circulating PCSK9 levels. PLoS One (2013) 0.91
Isolation and characterization of the circulating truncated form of PCSK9. J Lipid Res (2014) 0.90
The mystery of PCSK9. Arterioscler Thromb Vasc Biol (2004) 0.88
Molecular population genetics of PCSK9: a signature of recent positive selection. Pharmacogenet Genomics (2008) 0.88
Modulation of protease activated receptor 1 influences human metapneumovirus disease severity in a mouse model. PLoS One (2013) 0.88
Peroxisome Proliferator-activated receptor γ activation by ligands and dephosphorylation induces proprotein convertase subtilisin kexin type 9 and low density lipoprotein receptor expression. J Biol Chem (2012) 0.87
Plasma PCSK9 concentrations during an oral fat load and after short term high-fat, high-fat high-protein and high-fructose diets. Nutr Metab (Lond) (2013) 0.87
Plasma PCSK9 levels are elevated with acute myocardial infarction in two independent retrospective angiographic studies. PLoS One (2014) 0.86
The proprotein convertase PC5/6 is protective against intestinal tumorigenesis: in vivo mouse model. Mol Cancer (2009) 0.86
Molecular and cellular function of the proprotein convertase subtilisin/kexin type 9 (PCSK9). Basic Res Cardiol (2015) 0.85
A Mechanistic Systems Pharmacology Model for Prediction of LDL Cholesterol Lowering by PCSK9 Antagonism in Human Dyslipidemic Populations. CPT Pharmacometrics Syst Pharmacol (2014) 0.85
Association between cholesterol synthesis/absorption markers and effects of cholesterol lowering by atorvastatin among patients with high risk of coronary heart disease. J Lipid Res (2013) 0.84
Lysine acetylation in the lumen of the ER: a novel and essential function under the control of the UPR. Biochim Biophys Acta (2012) 0.83
Reduction of circulating PCSK9 and LDL-C levels by liver-specific knockdown of HNF1α in normolipidemic mice. J Lipid Res (2015) 0.83
Delineation of molecular pathways that regulate hepatic PCSK9 and LDL receptor expression during fasting in normolipidemic hamsters. Atherosclerosis (2012) 0.83
New developments in atherosclerosis: clinical potential of PCSK9 inhibition. Vasc Health Risk Manag (2015) 0.83
On the function and homeostasis of PCSK9: reciprocal interaction with LDLR and additional lipid effects. Atherosclerosis (2014) 0.82
The KLK5 protease suppresses breast cancer by repressing the mevalonate pathway. Oncotarget (2014) 0.82
Efficiency and safety of proprotein convertase subtilisin/kexin 9 monoclonal antibody on hypercholesterolemia: a meta-analysis of 20 randomized controlled trials. J Am Heart Assoc (2015) 0.82
Plasma levels of PCSK9 and phenotypic variability in familial hypercholesterolemia. J Lipid Res (2012) 0.82
A MARCH6 and IDOL E3 Ubiquitin Ligase Circuit Uncouples Cholesterol Synthesis from Lipoprotein Uptake in Hepatocytes. Mol Cell Biol (2015) 0.81
Impact of currently prescribed lipid-lowering drugs on plasma PCSK9 concentration: single or in combination study in rats. Lipids Health Dis (2014) 0.81
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. FEBS Open Bio (2014) 0.81
MicroRNA-27a decreases the level and efficiency of the LDL receptor and contributes to the dysregulation of cholesterol homeostasis. Atherosclerosis (2015) 0.81
Inhibition of PCSK9 transcription by berberine involves down-regulation of hepatic HNF1α protein expression through the ubiquitin-proteasome degradation pathway. J Biol Chem (2014) 0.81
Modeling and Simulation to Support Phase 2 Dose Selection for RG7652, a Fully Human Monoclonal Antibody Against Proprotein Convertase Subtilisin/Kexin Type 9. AAPS J (2015) 0.80
Decreased PCSK9 expression in human hepatocellular carcinoma. BMC Gastroenterol (2015) 0.79
Suppressor of Cytokine Signaling-3 (SOCS-3) Induces Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9) Expression in Hepatic HepG2 Cell Line. J Biol Chem (2015) 0.78
Enhanced circulating PCSK9 concentration by berberine through SREBP-2 pathway in high fat diet-fed rats. J Transl Med (2014) 0.78
Cholesterol synthesis inhibition elicits an integrated molecular response in human livers including decreased ACAT2. Arterioscler Thromb Vasc Biol (2008) 0.78
Evolving targets for lipid-modifying therapy. EMBO Mol Med (2014) 0.78
Impact of 3'UTR genetic variants in PCSK9 and LDLR genes on plasma lipid traits and response to atorvastatin in Brazilian subjects: a pilot study. Int J Clin Exp Med (2015) 0.77
Trafficking Dynamics of PCSK9-Induced LDLR Degradation: Focus on Human PCSK9 Mutations and C-Terminal Domain. PLoS One (2016) 0.77
PCSK9 inhibition in the management of hyperlipidemia: focus on evolocumab. Vasc Health Risk Manag (2016) 0.77
The effect of genetic variation in PCSK9 on the LDL-cholesterol response to statin therapy. Pharmacogenomics J (2016) 0.77
Dynamics of hepatic and intestinal cholesterol and bile acid pathways: The impact of the animal model of estrogen deficiency and exercise training. World J Hepatol (2016) 0.76
MG132, a proteasome inhibitor, enhances LDL uptake in HepG2 cells in vitro by regulating LDLR and PCSK9 expression. Acta Pharmacol Sin (2014) 0.76
Ancestry and other genetic associations with plasma PCSK9 response to simvastatin. Pharmacogenet Genomics (2014) 0.76
Effect of Porphyromonas gingivalis infection on post-transcriptional regulation of the low-density lipoprotein receptor in mice. Lipids Health Dis (2012) 0.76
Evaluation of the effect of genetic variation on the relationship between statins, cardiovascular disease and cancer. Int J Mol Epidemiol Genet (2013) 0.76
Proprotein convertase subtilisin/kexin type 9: from the discovery to the development of new therapies for cardiovascular diseases. Scientifica (Cairo) (2012) 0.76
Effect of Leptin Replacement on PCSK9 in ob/ob Mice and Female Lipodystrophic Patients. Endocrinology (2016) 0.75
Lupin Peptides Modulate the Protein-Protein Interaction of PCSK9 with the Low Density Lipoprotein Receptor in HepG2 Cells. Sci Rep (2016) 0.75
High dietary cholesterol and ovariectomy in rats repress gene expression of key markers of VLDL and bile acid metabolism in liver. Lipids Health Dis (2015) 0.75
Combined Effects of Rosuvastatin and Exercise on Gene Expression of Key Molecules Involved in Cholesterol Metabolism in Ovariectomized Rats. PLoS One (2016) 0.75
Established and emerging approaches for the management of dyslipidaemia. Scientifica (Cairo) (2012) 0.75
Relationships between genetic polymorphisms of E670G in PCSK9 gene and coronary artery disease: a meta-analysis. Int J Clin Exp Med (2015) 0.75
Proprotein Convertase Subtilisin/Kexin type 9, C-Reactive Protein, Coronary Severity, and Outcomes in Patients With Stable Coronary Artery Disease: A Prospective Observational Cohort Study. Medicine (Baltimore) (2015) 0.75
Lipid profiling of the therapeutic effects of berberine in patients with nonalcoholic fatty liver disease. J Transl Med (2016) 0.75
Mutations in PCSK9 cause autosomal dominant hypercholesterolemia. Nat Genet (2003) 11.67
Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial. JAMA (2006) 9.27
The secretory proprotein convertase neural apoptosis-regulated convertase 1 (NARC-1): liver regeneration and neuronal differentiation. Proc Natl Acad Sci U S A (2003) 5.26
NARC-1/PCSK9 and its natural mutants: zymogen cleavage and effects on the low density lipoprotein (LDL) receptor and LDL cholesterol. J Biol Chem (2004) 4.37
Egg yolk consumption and carotid plaque. Atherosclerosis (2012) 4.20
Automated design of ligands to polypharmacological profiles. Nature (2012) 3.54
The biology and therapeutic targeting of the proprotein convertases. Nat Rev Drug Discov (2012) 3.18
The activation and physiological functions of the proprotein convertases. Int J Biochem Cell Biol (2008) 2.38
Implication of the proprotein convertases in iron homeostasis: proprotein convertase 7 sheds human transferrin receptor 1 and furin activates hepcidin. Hepatology (2013) 2.24
Dietary cholesterol and egg yolks: not for patients at risk of vascular disease. Can J Cardiol (2010) 2.23
The cellular trafficking of the secretory proprotein convertase PCSK9 and its dependence on the LDLR. Traffic (2007) 2.09
Proprotein convertase subtilisin/kexin type 9 (PCSK9): hepatocyte-specific low-density lipoprotein receptor degradation and critical role in mouse liver regeneration. Hepatology (2008) 2.07
The proprotein convertase (PC) PCSK9 is inactivated by furin and/or PC5/6A: functional consequences of natural mutations and post-translational modifications. J Biol Chem (2006) 2.07
Proprotein convertases: lessons from knockouts. FASEB J (2006) 1.92
The proprotein convertase PCSK9 induces the degradation of low density lipoprotein receptor (LDLR) and its closest family members VLDLR and ApoER2. J Biol Chem (2007) 1.84
Deficiency of ABCA1 impairs apolipoprotein E metabolism in brain. J Biol Chem (2004) 1.82
Rosuvastatin, proprotein convertase subtilisin/kexin type 9 concentrations, and LDL cholesterol response: the JUPITER trial. Clin Chem (2011) 1.79
Wild-type PCSK9 inhibits LDL clearance but does not affect apoB-containing lipoprotein production in mouse and cultured cells. J Lipid Res (2005) 1.79
Endothelium-restricted overexpression of human endothelin-1 causes vascular remodeling and endothelial dysfunction. Circulation (2004) 1.65
A new method for measurement of total plasma PCSK9: clinical applications. J Lipid Res (2010) 1.64
A serine protease inhibitor prevents endoplasmic reticulum stress-induced cleavage but not transport of the membrane-bound transcription factor ATF6. J Biol Chem (2003) 1.57
The secretory proprotein convertases furin, PC5, and PC7 activate VEGF-C to induce tumorigenesis. J Clin Invest (2003) 1.51
Inactivation of endothelial proprotein convertase 5/6 decreases collagen deposition in the cardiovascular system: role of fibroblast autophagy. J Mol Med (Berl) (2011) 1.51
Crimean-Congo hemorrhagic fever virus glycoprotein proteolytic processing by subtilase SKI-1. J Virol (2003) 1.50
The LDLR deficient mouse as a model for aortic calcification and quantification by micro-computed tomography. Atherosclerosis (2011) 1.50
Dissection of the endogenous cellular pathways of PCSK9-induced low density lipoprotein receptor degradation: evidence for an intracellular route. J Biol Chem (2009) 1.49
Precursor convertases in the secretory pathway, cytosol and extracellular milieu. Essays Biochem (2002) 1.47
Proprotein convertases in tumor progression and malignancy: novel targets in cancer therapy. Am J Pathol (2002) 1.46
Chloroquine is a potent inhibitor of SARS coronavirus infection and spread. Virol J (2005) 1.43
Biosynthesis and cellular trafficking of the convertase SKI-1/S1P: ectodomain shedding requires SKI-1 activity. J Biol Chem (2001) 1.42
The proprotein convertases are potential targets in the treatment of dyslipidemia. J Mol Med (Berl) (2007) 1.40
Regional distribution and metabolic effect of PCSK9 insLEU and R46L gene mutations and apoE genotype. Can J Cardiol (2013) 1.39
Strong induction of PCSK9 gene expression through HNF1alpha and SREBP2: mechanism for the resistance to LDL-cholesterol lowering effect of statins in dyslipidemic hamsters. J Lipid Res (2010) 1.36
Alzheimer disease Abeta production in the absence of S-palmitoylation-dependent targeting of BACE1 to lipid rafts. J Biol Chem (2008) 1.34
VACTERL/caudal regression/Currarino syndrome-like malformations in mice with mutation in the proprotein convertase Pcsk5. Genes Dev (2008) 1.32
The cysteine-rich domain of the secreted proprotein convertases PC5A and PACE4 functions as a cell surface anchor and interacts with tissue inhibitors of metalloproteinases. Mol Biol Cell (2005) 1.30
The regulated cell surface zymogen activation of the proprotein convertase PC5A directs the processing of its secretory substrates. J Biol Chem (2007) 1.30
Rate of production of plasma and very-low-density lipoprotein (VLDL) apolipoprotein C-III is strongly related to the concentration and level of production of VLDL triglyceride in male subjects with different body weights and levels of insulin sensitivity. J Clin Endocrinol Metab (2004) 1.29
Plasma PCSK9 levels correlate with cholesterol in men but not in women. Biochem Biophys Res Commun (2007) 1.27
Selective inhibition of proprotein convertases represses the metastatic potential of human colorectal tumor cells. J Clin Invest (2008) 1.27
Gene inactivation of proprotein convertase subtilisin/kexin type 9 reduces atherosclerosis in mice. Circulation (2012) 1.26
Antigen processing by nardilysin and thimet oligopeptidase generates cytotoxic T cell epitopes. Nat Immunol (2010) 1.24
Circulating proprotein convertase subtilisin/kexin 9 (PCSK9) regulates VLDLR protein and triglyceride accumulation in visceral adipose tissue. Arterioscler Thromb Vasc Biol (2011) 1.24
ACAT1 gene ablation increases 24(S)-hydroxycholesterol content in the brain and ameliorates amyloid pathology in mice with AD. Proc Natl Acad Sci U S A (2010) 1.23
Deletion of the gene encoding proprotein convertase 5/6 causes early embryonic lethality in the mouse. Mol Cell Biol (2006) 1.23
In vivo functions of the proprotein convertase PC5/6 during mouse development: Gdf11 is a likely substrate. Proc Natl Acad Sci U S A (2008) 1.20
Annexin A2 is a C-terminal PCSK9-binding protein that regulates endogenous low density lipoprotein receptor levels. J Biol Chem (2008) 1.20
Proprotein convertases [corrected] are responsible for proteolysis and inactivation of endothelial lipase. J Biol Chem (2005) 1.20
The proprotein convertases and their implication in sterol and/or lipid metabolism. Biol Chem (2006) 1.20
Residual macrovascular risk in 2013: what have we learned? Cardiovasc Diabetol (2014) 1.20
Apolipoprotein E and atherosclerosis: beyond lipid effect. Arterioscler Thromb Vasc Biol (2005) 1.20
A locked nucleic acid antisense oligonucleotide (LNA) silences PCSK9 and enhances LDLR expression in vitro and in vivo. PLoS One (2010) 1.19
Proprotein convertase subtilisin/kexin type 9 (PCSK9) can mediate degradation of the low density lipoprotein receptor-related protein 1 (LRP-1). PLoS One (2013) 1.18
In vivo evidence that furin from hepatocytes inactivates PCSK9. J Biol Chem (2010) 1.18
Increased apoC-III production is a characteristic feature of patients with hypertriglyceridemia. Atherosclerosis (2004) 1.17
Atorvastatin increases intestinal expression of NPC1L1 in hyperlipidemic men. J Lipid Res (2010) 1.17
Inhibition of Chikungunya virus infection in cultured human muscle cells by furin inhibitors: impairment of the maturation of the E2 surface glycoprotein. J Biol Chem (2008) 1.14
Novel loss-of-function PCSK9 variant is associated with low plasma LDL cholesterol in a French-Canadian family and with impaired processing and secretion in cell culture. Clin Chem (2011) 1.14
The proprotein convertase PC5A and a metalloprotease are involved in the proteolytic processing of the neural adhesion molecule L1. J Biol Chem (2003) 1.14
PCSK9-deficient mice exhibit impaired glucose tolerance and pancreatic islet abnormalities. FEBS Lett (2009) 1.10
Human carcinoma cell growth and invasiveness is impaired by the propeptide of the ubiquitous proprotein convertase furin. Cancer Res (2005) 1.10
Processing of alpha4 integrin by the proprotein convertases: histidine at position P6 regulates cleavage. Biochem J (2003) 1.10
Opposing function of the proprotein convertases furin and PACE4 on breast cancer cells' malignant phenotypes: role of tissue inhibitors of metalloproteinase-1. Cancer Res (2007) 1.09
Implication of the proprotein convertase NARC-1/PCSK9 in the development of the nervous system. J Neurochem (2006) 1.09
Plasma PCSK9 is associated with age, sex, and multiple metabolic markers in a population-based sample of children and adolescents. Clin Chem (2009) 1.09
Altered processing of the neurotensin/neuromedin N precursor in PC2 knock down mice: a biochemical and immunohistochemical study. J Neurochem (2002) 1.08
Dual regulation of the LDL receptor--some clarity and new questions. Cell Metab (2005) 1.08
A rapid fluorometric assay for the proteolytic activity of SKI-1/S1P based on the surface glycoprotein of the hemorrhagic fever Lassa virus. FEBS Lett (2002) 1.08
Implication of proprotein convertases in the processing and spread of severe acute respiratory syndrome coronavirus. Biochem Biophys Res Commun (2005) 1.08
The proprotein convertase SKI-1/S1P. In vitro analysis of Lassa virus glycoprotein-derived substrates and ex vivo validation of irreversible peptide inhibitors. J Biol Chem (2006) 1.06