(Q38580461)

4 September 2017

Dissecting fibrosis: therapeutic insights from the small-molecule toolbox (English)

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4 September 2017

Carmel B Nanthakumar

1

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4 September 2017

Richard J D Hatley

2

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4 September 2017

Seble Lemma

3

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4 September 2017

Jack Gauldie

4

1 reference

4 September 2017

Richard P Marshall

5

1 reference

4 September 2017

Simon J F Macdonald

6

1 reference

4 September 2017

4 September 2015

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Nature Reviews Drug Discovery

4 September 2017

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4 September 2017

14

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4 September 2017

10

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4 September 2017

693-720

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https://scigraph.springernature.com/pub.10.1038/nrd4592

4 September 2017

0 references

cites work

Incidence and prevalence of idiopathic pulmonary fibrosis

1 reference

Mortality from pulmonary fibrosis increased in the United States from 1992 to 2003.

21 January 2018

1 reference

A phase 3 trial of pirfenidone in patients with idiopathic pulmonary fibrosis

21 January 2018

1 reference

Novel therapeutic approaches for pulmonary fibrosis

21 January 2018

1 reference

Interstitial lung disease in rheumatoid arthritis: recent advances

21 January 2018

1 reference

Effect of diagnosis on survival benefit of lung transplantation for end-stage lung disease

21 January 2018

1 reference

Prednisone, azathioprine, and N-acetylcysteine for pulmonary fibrosis

21 January 2018

1 reference

Pirfenidone for diabetic nephropathy

21 January 2018

1 reference

Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents

21 January 2018

1 reference

Clinical practice. Nephropathy in patients with type 2 diabetes

21 January 2018

1 reference

Chronic kidney disease: the global challenge

21 January 2018

1 reference

Aliskiren combined with losartan in type 2 diabetes and nephropathy

21 January 2018

1 reference

Effects of losartan on hepatic expression of nonphagocytic NADPH oxidase and fibrogenic genes in patients with chronic hepatitis C

21 January 2018

1 reference

BUILD-3: a randomized, controlled trial of bosentan in idiopathic pulmonary fibrosis

21 January 2018

1 reference

21 January 2018

1 reference

Strategic management of keloid disease in ethnic skin: a structured approach supported by the emerging literature.

21 January 2018

1 reference

Urinary proteomics for early diagnosis in diabetic nephropathy

21 January 2018

1 reference

Diminished prostaglandin E2 contributes to the apoptosis paradox in idiopathic pulmonary fibrosis

21 January 2018

1 reference

A systems approach identifies HIPK2 as a key regulator of kidney fibrosis

21 January 2018

1 reference

Molecular mechanisms of epithelial-mesenchymal transition

21 January 2018

1 reference

Functional Wnt signaling is increased in idiopathic pulmonary fibrosis

21 January 2018

1 reference

Identification of human epididymis protein-4 as a fibroblast-derived mediator of fibrosis

21 January 2018

1 reference

Fate tracing reveals the pericyte and not epithelial origin of myofibroblasts in kidney fibrosis

21 January 2018

1 reference

Multiple stromal populations contribute to pulmonary fibrosis without evidence for epithelial to mesenchymal transition

21 January 2018

1 reference

Randomized trial of acetylcysteine in idiopathic pulmonary fibrosis

21 January 2018

1 reference

Bardoxolone methyl in type 2 diabetes and stage 4 chronic kidney disease

21 January 2018

1 reference

Superoxide scavenging activity of pirfenidone-iron complex

21 January 2018

1 reference

Combined corticosteroid and cyclophosphamide therapy does not alter survival in idiopathic pulmonary fibrosis.

21 January 2018

1 reference

Identification of steroid sensitive responders versus non-responders in the treatment of keloid disease.

21 January 2018

1 reference

Corticosteroid plus pentoxifylline is not better than corticosteroid alone for improving survival in severe alcoholic hepatitis (COPE trial).

21 January 2018

1 reference

Influence of ursodeoxycholic acid on the mortality and malignancy associated with primary biliary cirrhosis: a population-based cohort study.

21 January 2018

1 reference

CCR2 promotes hepatic fibrosis in mice

21 January 2018

1 reference

The relationship between individual histologic features and disease progression in idiopathic pulmonary fibrosis.

21 January 2018

1 reference

Identification of a cell-of-origin for fibroblasts comprising the fibrotic reticulum in idiopathic pulmonary fibrosis.

21 January 2018

1 reference

Role of lung pericytes and resident fibroblasts in the pathogenesis of pulmonary fibrosis.

21 January 2018

1 reference

Mechanisms of hepatic fibrogenesis

21 January 2018

1 reference

Cyclooxygenase-2 deficiency results in a loss of the anti-proliferative response to transforming growth factor-beta in human fibrotic lung fibroblasts and promotes bleomycin-induced pulmonary fibrosis in mice

21 January 2018

1 reference

Adenoviral overexpression and small interfering RNA suppression demonstrate that plasminogen activator inhibitor-1 produces elevated collagen accumulation in normal and keloid fibroblasts

21 January 2018

1 reference

Hypermethylation of PTGER2 confers prostaglandin E2 resistance in fibrotic fibroblasts from humans and mice

21 January 2018

1 reference

Methylation determines fibroblast activation and fibrogenesis in the kidney

21 January 2018

1 reference

Delayed stress fiber formation mediates pulmonary myofibroblast differentiation in response to TGF-β.

21 January 2018

1 reference

Myofibroblast differentiation by transforming growth factor-beta1 is dependent on cell adhesion and integrin signaling via focal adhesion kinase.

21 January 2018

1 reference

Protection from liver fibrosis by a peroxisome proliferator-activated receptor δ agonist

21 January 2018

1 reference

Multigenerational epigenetic adaptation of the hepatic wound-healing response

21 January 2018

1 reference

MeCP2 controls an epigenetic pathway that promotes myofibroblast transdifferentiation and fibrosis

21 January 2018

1 reference

Long-term efficacy of rosiglitazone in nonalcoholic steatohepatitis: results of the fatty liver improvement by rosiglitazone therapy (FLIRT 2) extension trial

21 January 2018

1 reference

A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis

21 January 2018

1 reference

mTOR and cancer: insights into a complex relationship

21 January 2018

1 reference

Two TOR complexes, only one of which is rapamycin sensitive, have distinct roles in cell growth control

21 January 2018

1 reference

Imatinib: a selective tyrosine kinase inhibitor

21 January 2018

1 reference

Imatinib as a novel antifibrotic agent in bleomycin-induced pulmonary fibrosis in mice

21 January 2018

1 reference

Imatinib treatment for idiopathic pulmonary fibrosis: Randomized placebo-controlled trial results

21 January 2018

1 reference

Imatinib mesylate in scleroderma-associated diffuse skin fibrosis: a phase II multicentre randomized double-blinded controlled trial.

21 January 2018

1 reference

Efficacy and safety of nintedanib in idiopathic pulmonary fibrosis

21 January 2018

1 reference

Therapeutic approaches to diabetic nephropathy--beyond the RAS.

21 January 2018

1 reference

c-Jun N-terminal kinase 1 is required for the development of pulmonary fibrosis

21 January 2018

1 reference

Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).

21 January 2018

1 reference

SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7

21 January 2018

1 reference

Induction of heart valve lesions by small-molecule ALK5 inhibitors.

21 January 2018

1 reference

Targeting the TGFβ signalling pathway in disease

21 January 2018

1 reference

Smad3 null mice develop airspace enlargement and are resistant to TGF-beta-mediated pulmonary fibrosis

21 January 2018

1 reference

Targeted disruption of TGF-β1/Smad3 signaling protects against renal tubulointerstitial fibrosis induced by unilateral ureteral obstruction

21 January 2018

1 reference

The integrin alpha v beta 6 binds and activates latent TGF beta 1: a mechanism for regulating pulmonary inflammation and fibrosis

21 January 2018

1 reference

Inhibition of integrin alphavbeta6 on cholangiocytes blocks transforming growth factor-beta activation and retards biliary fibrosis progression

21 January 2018

1 reference

Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs

21 January 2018

1 reference

Allosteric inhibition of lysyl oxidase-like-2 impedes the development of a pathologic microenvironment

21 January 2018

1 reference

Modulation of lysyl oxidase-like 2 enzymatic activity by an allosteric antibody inhibitor

21 January 2018

1 reference

Transglutaminase 2 and its role in pulmonary fibrosis.

21 January 2018

1 reference

Tissue transglutaminase and the progression of human renal scarring

21 January 2018

1 reference

Increased TG2 expression can result in induction of transforming growth factor beta1, causing increased synthesis and deposition of matrix proteins, which can be regulated by nitric oxide

21 January 2018

1 reference

Always cleave up your mess: targeting collagen degradation to treat tissue fibrosis

21 January 2018

1 reference

Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis

21 January 2018

1 reference

Pirfenidone inhibits the expression of HSP47 in TGF-beta1-stimulated human lung fibroblasts

21 January 2018

1 reference

Noninvasive assessment of liver fibrosis by measurement of stiffness in patients with chronic hepatitis C.

21 January 2018

1 reference

Tissue stiffness, latent TGF-beta1 activation, and mechanical signal transduction: implications for the pathogenesis and treatment of fibrosis.

21 January 2018

1 reference

A multiwell platform for studying stiffness-dependent cell biology

21 January 2018

1 reference

Feedback amplification of fibrosis through matrix stiffening and COX-2 suppression

21 January 2018

1 reference

Proteasome inhibition improves diaphragm function in an animal model for COPD.

21 January 2018

1 reference

Peptide-mediated inhibition of mitogen-activated protein kinase-activated protein kinase-2 ameliorates bleomycin-induced pulmonary fibrosis

21 January 2018

1 reference

The bleomycin animal model: a useful tool to investigate treatment options for idiopathic pulmonary fibrosis?

21 January 2018

1 reference

Open access chemical and clinical probes to support drug discovery

21 January 2018

1 reference

Designed multiple ligands. An emerging drug discovery paradigm

21 January 2018

1 reference

BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy

21 January 2018

1 reference

Network pharmacology: the next paradigm in drug discovery

21 January 2018

1 reference

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology

21 January 2018

1 reference

Automated design of ligands to polypharmacological profiles.

21 January 2018

1 reference

Phenotypic screening in cancer drug discovery - past, present and future

21 January 2018

1 reference

The why and how of phenotypic small-molecule screens

21 January 2018

1 reference

How were new medicines discovered?

21 January 2018

1 reference

Idiopathic pulmonary fibrosis. Clinical, histologic, radiographic, physiologic, scintigraphic, cytologic, and biochemical aspects

21 January 2018

1 reference

Pirfenidone treatment decreases transforming growth factor-beta1 and matrix proteins and ameliorates fibrosis in chronic cyclosporine nephrotoxicity

21 January 2018

1 reference

A novel anti-fibrotic agent pirfenidone suppresses tumor necrosis factor-alpha at the translational level

21 January 2018

1 reference

Pirfenidone suppresses tumor necrosis factor-alpha, enhances interleukin-10 and protects mice from endotoxic shock

21 January 2018

1 reference

Antifibrotic activities of pirfenidone in animal models

21 January 2018

1 reference

Pirfenidone in patients with idiopathic pulmonary fibrosis (CAPACITY): two randomised trials

21 January 2018

1 reference

Antifibrotic and anti-inflammatory activity of the tyrosine kinase inhibitor nintedanib in experimental models of lung fibrosis

21 January 2018

1 reference

Angiotensin II type 1 receptor blockers

21 January 2018

1 reference

Endothelin antagonism in portal hypertensive mice: implications for endothelin receptor-specific signaling in liver disease

21 January 2018

1 reference

Addition of atrasentan to renin-angiotensin system blockade reduces albuminuria in diabetic nephropathy

21 January 2018

1 reference

Endothelin-1 in idiopathic pulmonary fibrosis

21 January 2018

1 reference

Endothelin-1 induces alveolar epithelial-mesenchymal transition through endothelin type A receptor-mediated production of TGF-beta1

21 January 2018

1 reference

Treatment of idiopathic pulmonary fibrosis with ambrisentan: a parallel, randomized trial

21 January 2018

1 reference

Digital ulcers in systemic sclerosis: prevention by treatment with bosentan, an oral endothelin receptor antagonist.

21 January 2018

1 reference

The chemistry and biological activities of N-acetylcysteine

21 January 2018

1 reference

Molecular mechanisms of N-acetylcysteine actions

21 January 2018

1 reference

Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo.

21 January 2018

1 reference

First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis

21 January 2018

1 reference

Genetic targeting or pharmacologic inhibition of NADPH oxidase nox4 provides renoprotection in long-term diabetic nephropathy

21 January 2018

1 reference

Reversal of persistent fibrosis in aging by targeting Nox4-Nrf2 redox imbalance

21 January 2018

1 reference

Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent

21 January 2018

1 reference

Bardoxolone methyl decreases megalin and activates nrf2 in the kidney

21 January 2018

1 reference

Triterpenoid CDDO-Me blocks the NF-kappaB pathway by direct inhibition of IKKbeta on Cys-179.

21 January 2018

1 reference

Bardoxolone methyl and kidney function in CKD with type 2 diabetes

21 January 2018

1 reference

Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding

21 January 2018

1 reference

Dual peroxisome proliferator-activated receptor α/δ agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects

21 January 2018

1 reference

Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis

21 January 2018

1 reference

Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARα agonist with moderate PPARγ agonist activity in healthy human subjects.

21 January 2018

1 reference

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents

21 January 2018

1 reference

Pioglitazone prevents hepatic steatosis, fibrosis, and enzyme-altered lesions in rat liver cirrhosis induced by a choline-deficient L-amino acid-defined diet

21 January 2018

1 reference

Chemical modification of rapamycin: the discovery of SDZ RAD.

21 January 2018

1 reference

Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin

21 January 2018

1 reference

Rapamycin prevents transforming growth factor-alpha-induced pulmonary fibrosis.

21 January 2018

1 reference

Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors

21 January 2018

1 reference

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

21 January 2018

1 reference

Inhibition of PDGF, TGF-β, and Abl signaling and reduction of liver fibrosis by the small molecule Bcr-Abl tyrosine kinase antagonist Nilotinib.

21 January 2018

1 reference

Nilotinib attenuates renal injury and prolongs survival in chronic kidney disease

21 January 2018

1 reference

Effect of nilotinib on bleomycin-induced acute lung injury and pulmonary fibrosis in mice.

21 January 2018

1 reference

BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis

21 January 2018

1 reference

New insights into the antifibrotic effects of sorafenib on hepatic stellate cells and liver fibrosis

21 January 2018

1 reference

Sorafenib inhibits transforming growth factor β1-mediated epithelial-mesenchymal transition and apoptosis in mouse hepatocytes

21 January 2018

1 reference

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (d

21 January 2018

1 reference

Dual inhibition of c-abl and PDGF receptor signaling by dasatinib and nilotinib for the treatment of dermal fibrosis

21 January 2018

1 reference

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.

21 January 2018

1 reference

JAK-2 as a novel mediator of the profibrotic effects of transforming growth factor β in systemic sclerosis.

21 January 2018

1 reference

21 January 2018

1 reference

Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor

21 January 2018

1 reference

Jun N-terminal kinase as a potential molecular target for prevention and treatment of dermal fibrosis.

21 January 2018

1 reference

Peptide inhibitors of MK2 show promise for inhibition of abdominal adhesions

21 January 2018

1 reference

MMI-0100 inhibits cardiac fibrosis in myocardial infarction by direct actions on cardiomyocytes and fibroblasts via MK2 inhibition

21 January 2018

1 reference

Inhibition of Mitogen Activated Protein Kinase Activated Protein Kinase II with MMI-0100 reduces intimal hyperplasia ex vivo and in vivo

21 January 2018

1 reference

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist

21 January 2018

1 reference

Macitentan for the treatment of idiopathic pulmonary fibrosis: the randomised controlled MUSIC trial

21 January 2018

1 reference

Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis

21 January 2018

1 reference

Thrombin-activatable fibrinolysis inhibitor deficiency attenuates bleomycin-induced lung fibrosis

21 January 2018

1 reference

Cation-independent mannose 6-phosphate receptor inhibitor (PXS25) inhibits fibrosis in human proximal tubular cells by inhibiting conversion of latent to active TGF-beta1.

21 January 2018

1 reference

A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model

21 January 2018

1 reference

The lysophosphatidic acid receptor LPA1 links pulmonary fibrosis to lung injury by mediating fibroblast recruitment and vascular leak

21 January 2018

1 reference

Targeted delivery of cytokine therapy to rheumatoid tissue by a synovial targeting peptide

21 January 2018

1 reference

Thalidomide selectively inhibits tumor necrosis factor alpha production by stimulated human monocytes

21 January 2018

1 reference

Thalidomide prevents bleomycin-induced pulmonary fibrosis in mice

21 January 2018

1 reference

Anti-fibrotic effect of thalidomide through inhibiting TGF-beta-induced ERK1/2 pathways in bleomycin-induced lung fibrosis in mice

21 January 2018

1 reference

Isosteric analogs of lenalidomide and pomalidomide: synthesis and biological activity

21 January 2018

1 reference

First-in-class pan caspase inhibitor developed for the treatment of liver disease

21 January 2018

1 reference

The Caspase Inhibitor IDN-6556 Attenuates Hepatic Injury and Fibrosis in the Bile Duct Ligated Mouse

21 January 2018

1 reference

Targeting antioxidants to mitochondria by conjugation to lipophilic cations.

21 January 2018

1 reference

Prevention of diabetic nephropathy in Ins2(+/)⁻(AkitaJ) mice by the mitochondria-targeted therapy MitoQ.

21 January 2018

1 reference

Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells

21 January 2018

1 reference

Effect of beraprost sodium (BPS) in a new rat partial unilateral ureteral obstruction model.

21 January 2018

1 reference

Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist

21 January 2018

1 reference

A prostacyclin analogue, iloprost, protects from bleomycin-induced pulmonary fibrosis in mice

21 January 2018

1 reference

A pilot trial of treprostinil for the treatment and prevention of digital ulcers in patients with systemic sclerosis

21 January 2018

1 reference

A synthetic peptide from transforming growth factor beta type III receptor inhibits liver fibrogenesis in rats with carbon tetrachloride liver injury

21 January 2018

1 reference

A synthetic peptide from transforming growth factor-beta1 type III receptor prevents myocardial fibrosis in spontaneously hypertensive rats

21 January 2018

1 reference

Identification of human S100A9 as a novel target for treatment of autoimmune disease via binding to quinoline-3-carboxamides

21 January 2018

1 reference

6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.

21 January 2018

1 reference

Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease

21 January 2018

1 reference

The farnesoid X receptor modulates renal lipid metabolism and diet-induced renal inflammation, fibrosis, and proteinuria

21 January 2018

1 reference

21 January 2018

1 reference

S-adenosylmethionine blocks collagen I production by preventing transforming growth factor-beta induction of the COL1A2 promoter

21 January 2018

1 reference

Heavy drugs draw heavy interest from pharma backers

21 January 2018

1 reference

A post-Amadori inhibitor pyridoxamine also inhibits chemical modification of proteins by scavenging carbonyl intermediates of carbohydrate and lipid degradation

21 January 2018

1 reference

Effects of pyridoxamine in combined phase 2 studies of patients with type 1 and type 2 diabetes and overt nephropathy

21 January 2018

1 reference

Pyridoxamine inhibits early renal disease and dyslipidemia in the streptozotocin-diabetic rat.

21 January 2018

1 reference

Tocopherol activity correlates with its location in a membrane: a new perspective on the antioxidant vitamin E.

21 January 2018

1 reference

Pioglitazone, vitamin E, or placebo for nonalcoholic steatohepatitis

21 January 2018

1 reference

The chemokine monocyte chemoattractant protein-1 contributes to renal dysfunction in swine renovascular hypertension

21 January 2018

1 reference

Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity

21 January 2018

1 reference

Maraviroc, a CCR5 antagonist, prevents development of hepatocellular carcinoma in a mouse model

21 January 2018

1 reference

Maraviroc, a CCR5 antagonist, ameliorates the development of hepatic steatosis in a mouse model of non-alcoholic fatty liver disease (NAFLD).

21 January 2018

1 reference

Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle

21 January 2018

1 reference

Blockade of CCR2 ameliorates progressive fibrosis in kidney.

21 January 2018

1 reference

A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats

21 January 2018

1 reference

Development of focal adhesion kinase inhibitors in cancer therapy

21 January 2018

1 reference

Inhibition of focal adhesion kinase prevents experimental lung fibrosis and myofibroblast formation

21 January 2018

1 reference

Selective inhibition of activin receptor-like kinase 5 signaling blocks profibrotic transforming growth factor beta responses in skin fibroblasts

21 January 2018

1 reference

Blockade of endothelial-mesenchymal transition by a Smad3 inhibitor delays the early development of streptozotocin-induced diabetic nephropathy

21 January 2018

1 reference

The αvβ1 integrin plays a critical in vivo role in tissue fibrosis

21 January 2018

1 reference

Interactions between growth factors and integrins: latent forms of transforming growth factor-beta are ligands for the integrin alphavbeta1

21 January 2018

1 reference

Transglutaminase inhibition ameliorates experimental diabetic nephropathy.

21 January 2018

1 reference

Beneficial effects of inhibitors of prolyl 4-hydroxylase in CCl4-induced fibrosis of the liver in rats

21 January 2018

1 reference

Protease-activated receptor 1 inhibition by SCH79797 attenuates left ventricular remodeling and profibrotic activities of cardiac fibroblasts.

21 January 2018

1 reference

A novel inhibitor of plasminogen activator inhibitor-1 provides antithrombotic benefits devoid of bleeding effect in nonhuman primates

21 January 2018

1 reference

Therapeutic value of small molecule inhibitor to plasminogen activator inhibitor-1 for lung fibrosis

21 January 2018

1 reference

ONO-5046, a novel inhibitor of human neutrophil elastase

21 January 2018

1 reference

Halofuginone, an inhibitor of type-I collagen synthesis and skin sclerosis, blocks transforming-growth-factor-beta-mediated Smad3 activation in fibroblasts.

21 January 2018

1 reference

Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase

21 January 2018

1 reference

Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response

21 January 2018

1 reference

Halofuginone to prevent and treat thioacetamide-induced liver fibrosis in rats

21 January 2018

1 reference

A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists

21 January 2018

1 reference

Inhibitory effect of CXC chemokine receptor 4 antagonist AMD3100 on bleomycin induced murine pulmonary fibrosis

21 January 2018

1 reference

Antifibrotic effects of CXCR4 antagonist in bleomycin-induced pulmonary fibrosis in mice

21 January 2018

1 reference

An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway

21 January 2018

1 reference

Pregnenolone-16alpha-carbonitrile inhibits rodent liver fibrogenesis via PXR (pregnane X receptor)-dependent and PXR-independent mechanisms.

21 January 2018

1 reference

The immune modulator FTY720 targets sphingosine 1-phosphate receptors

21 January 2018

1 reference

The lymphocyte migration inhibitor FTY720 attenuates experimental hypertensive nephropathy.

21 January 2018

1 reference

Cross-talk between PDGF and S1P signalling elucidates the inhibitory effect and potential antifibrotic action of the immunomodulator FTY720 in activated HSC-cultures.

21 January 2018

1 reference

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

21 January 2018

1 reference

Inactivation of tankyrases reduces experimental fibrosis by inhibiting canonical Wnt signalling

21 January 2018

1 reference

ICG-001, a novel small molecule regulator of TCF/beta-catenin transcription

21 January 2018

1 reference

Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis

21 January 2018

1 reference

The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs

21 January 2018

1 reference

Prostaglandin E(2) inhibits collagen expression and proliferation in patient-derived normal lung fibroblasts via E prostanoid 2 receptor and cAMP signaling.

21 January 2018

1 reference

Prostaglandin F2α facilitates collagen synthesis in cardiac fibroblasts via an F-prostanoid receptor/protein kinase C/Rho kinase pathway independent of transforming growth factor β1.

21 January 2018

1 reference

Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists

21 January 2018

1 reference

Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states

21 January 2018

1 reference

P2X(7) receptor antagonism attenuates the hypertension and renal injury in Dahl salt-sensitive rats.

21 January 2018

1 reference

Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant

21 January 2018

1 reference

Renal fibrosis is attenuated by targeted disruption of KCa3.1 potassium channels

21 January 2018

1 reference

Blockade of KCa3.1 ameliorates renal fibrosis through the TGF-β1/Smad pathway in diabetic mice

21 January 2018

1 reference

Identification of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels

21 January 2018

1 reference

T-type calcium channel blockade as a therapeutic strategy against renal injury in rats with subtotal nephrectomy

21 January 2018

1 reference

Identification of small molecule chemical inhibitors of the collagen-specific chaperone Hsp47.

21 January 2018

1 reference

Suppression of renal tubulointerstitial fibrosis by small interfering RNA targeting heat shock protein 47.

21 January 2018

1 reference

Regulation of transforming growth factor-β1-driven lung fibrosis by galectin-3

21 January 2018

1 reference

Selective protein kinase C inhibitors and their applications

21 January 2018

1 reference

PKCδ as a regulator for TGFβ1-induced α-SMA production in a murine nonalcoholic steatohepatitis model

21 January 2018

1 reference

A new class of angiotensin-converting enzyme inhibitors

21 January 2018

1 reference

Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling

21 January 2018

1 reference

5-HT2A receptor antagonists inhibit hepatic stellate cell activation and facilitate apoptosis

21 January 2018

1 reference

A 5-hydroxytryptamine receptor antagonist, sarpogrelate, reduces renal tubulointerstitial fibrosis by suppressing PAI-1.

21 January 2018

1 reference

Aromatic phosphonates inhibit the lysophospholipase D activity of autotaxin

21 January 2018

1 reference

Prevention of bleomycin-induced pulmonary fibrosis by a novel antifibrotic peptide with relaxin-like activity

21 January 2018

1 reference

Selective inhibition of BET bromodomains

21 January 2018

1 reference

BML-11, a lipoxin receptor agonist, protected carbon tetrachloride-induced hepatic fibrosis in rats

21 January 2018

1 reference

Cytosporone B is an agonist for nuclear orphan receptor Nur77.

21 January 2018

1 reference

Orphan nuclear receptor NR4A1 regulates transforming growth factor-β signaling and fibrosis

21 January 2018

1 reference

Transglutaminase Inhibition Reduces Fibrosis and Preserves Function in Experimental Chronic Kidney Disease

21 January 2018

1 reference

Stromedix acquisition signals growing interest in fibrosis

21 January 2018

1 reference

Understanding CT patterns in idiopathic pulmonary fibrosis

31 March 2020

1 reference

Origin and function of myofibroblasts in kidney fibrosis

31 March 2020

1 reference

Colchicine, D-penicillamine, and prednisone in the treatment of idiopathic pulmonary fibrosis: a controlled clinical trial

31 March 2020

1 reference

Fibrocytes are a potential source of lung fibroblasts in idiopathic pulmonary fibrosis

31 March 2020

1 reference

Scleroderma lung fibroblasts exhibit elevated and dysregulated type I collagen biosynthesis

31 March 2020

1 reference

An investigator-driven study of everolimus in surgical lung biopsy confirmed idiopathic pulmonary fibrosis

31 March 2020

1 reference

Is Cirrhosis of the Liver Experimentally Produced by CC14 an Adequate Model of Human Cirrhosis?

31 March 2020

1 reference

Increased endothelin-1 in bleomycin-induced pulmonary fibrosis and the effect of an endothelin receptor antagonist

31 March 2020

1 reference

Involution of keloid implants in athymic mice treated with pirfenidone or with triamcinolone

31 March 2020

1 reference

Evaluation of the antifibrotic effect of fenofibrate and rosiglitazone on bleomycin-induced pulmonary fibrosis in rats

31 March 2020

1 reference

HS-173, a novel PI3K inhibitor, attenuates the activation of hepatic stellate cells in liver fibrosis

31 March 2020

1 reference

Rapamycin attenuates unilateral ureteral obstruction-induced renal fibrosis

31 March 2020

1 reference

Pomalidomide is effective for prevention and treatment of experimental skin fibrosis

31 March 2020

1 reference

Iloprost suppresses connective tissue growth factor production in fibroblasts and in the skin of scleroderma patients

31 March 2020

1 reference

Topical application of a peptide inhibitor of transforming growth factor-beta1 ameliorates bleomycin-induced skin fibrosis

31 March 2020

1 reference

Synthetic farnesoid X receptor agonists induce high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-)

31 March 2020

1 reference

S-adenosylmethionine treatment prevents carbon tetrachloride-induced S-adenosylmethionine synthetase inactivation and attenuates liver injury

31 March 2020

1 reference

Pyridoxamine, an inhibitor of advanced glycation reactions, also inhibits advanced lipoxidation reactions. Mechanism of action of pyridoxamine

31 March 2020

1 reference

Y-27632 prevents tubulointerstitial fibrosis in mouse kidneys with unilateral ureteral obstruction

31 March 2020

1 reference

Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression

31 March 2020

1 reference

Prolyl 4-hydroxylase inhibitor (HOE 077) inhibits pig serum-induced rat liver fibrosis by preventing stellate cell activation

31 March 2020

1 reference

Potent and selective nonpeptidic inhibitors of procollagen C-proteinase

31 March 2020

1 reference

Inhibition of cellular action of thrombin by N3-cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist

31 March 2020

1 reference

Effects of neutrophil elastase inhibitor on bleomycin-induced pulmonary fibrosis in mice

31 March 2020

1 reference

A neutrophil elastase inhibitor prevents bleomycin-induced pulmonary fibrosis in mice

31 March 2020

1 reference

Reduction in pulmonary fibrosis in vivo by halofuginone

31 March 2020

1 reference

Blockade of canonical Wnt signalling ameliorates experimental dermal fibrosis

31 March 2020

1 reference

SB 239063, a p38 MAPK inhibitor, reduces neutrophilia, inflammatory cytokines, MMP-9, and fibrosis in lung

31 March 2020

1 reference

Enalapril reduces collagen type IV synthesis and expansion of the interstitium in the obstructed rat kidney

31 March 2020

1 reference

Pulmonary autotaxin expression contributes to the pathogenesis of pulmonary fibrosis

31 March 2020

1 reference

Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1.

31 March 2020

1 reference

BET bromodomain proteins mediate downstream signaling events following growth factor stimulation in human lung fibroblasts and are involved in bleomycin-induced pulmonary fibrosis

31 March 2020

1 reference

Inhibition of leukotriene B4-induced neutrophil migration by lipoxin A4: structure-function relationships

31 March 2020

1 reference

Effects of AT1 receptor antagonist, losartan, on rat hepatic fibrosis induced by CCl(4).

31 March 2020

1 reference

12 December 2020

Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases

1 reference

12 December 2020

Randomized, prospective, placebo-controlled trial of bosentan in interstitial lung disease secondary to systemic sclerosis

1 reference

12 December 2020

beta-Aminopropionitrile prevents bleomycin-induced pulmonary fibrosis in the hamster

1 reference

12 December 2020

Effects of pirfenidone on transforming growth factor-beta gene expression at the transcriptional level in bleomycin hamster model of lung fibrosis

1 reference

12 December 2020

Hepatic stellate cells require a stiff environment for myofibroblastic differentiation.

1 reference

12 December 2020

Modeling liver fibrosis in rodents

1 reference

12 December 2020

Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist

1 reference

12 December 2020

The prolyl 4-hydroxylase inhibitor HOE 077 prevents activation of Ito cells, reducing procollagen gene expression in rat liver fibrosis induced by choline-deficient L-amino acid-defined diet

1 reference

12 December 2020

CCR1 and CCR5 promote hepatic fibrosis in mice

1 reference

12 December 2020

Predictors of mortality and progression in scleroderma-associated interstitial lung disease: a systematic review

1 reference

12 December 2020

AL-8810: a novel prostaglandin F2 alpha analog with selective antagonist effects at the prostaglandin F2 alpha (FP) receptor

1 reference

12 December 2020

PPARγ downregulation by TGFß in fibroblast and impaired expression and function in systemic sclerosis: a novel mechanism for progressive fibrogenesis

1 reference

12 December 2020

Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist.

1 reference

12 December 2020

Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma

1 reference

12 December 2020

PPAR-γ ligands repress TGFβ-induced myofibroblast differentiation by targeting the PI3K/Akt pathway: implications for therapy of fibrosis

1 reference

12 December 2020

Impact of the anti-inflammatory agent bindarit on the chemokinome: selective inhibition of the monocyte chemotactic proteins

1 reference

12 December 2020

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD4592

1 reference

4 September 2017

1 reference