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Journal
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2018, Volume 28, Issue 2, pp. 85 - 93
We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists.... 
POTENT | AUTOIMMUNE | CHEMISTRY, MEDICINAL | INHIBITION | INTERLEUKIN-17 | NUCLEAR RECEPTORS | MODULATORS | DISEASE | GENE-EXPRESSION | CHEMISTRY, ORGANIC | DISCOVERY | PSORIASIS | Rheumatoid factor | Multiple sclerosis | Sulfonamides | Analysis | Gastrointestinal diseases | Liver | Arthritis
Journal Article
Journal of Allergy and Clinical Immunology, The, ISSN 0091-6749, 2017, Volume 140, Issue 3, pp. 809 - 821.e3
Background Hypertension is considered an immunologic disorder. However, the role of the IL-17 family in genetic hypertension in the spontaneously hypertensive... 
Allergy and Immunology | Hypertension | CD161 | IL-17 | spontaneously hypertensive rat | digoxin | T cells | retinoic acid receptor–related orphan receptor γt | TH17 | Toll-like receptor | gene expression | innate immune system | INTERLEUKIN 17 | ACTIVATION | ENDOTHELIAL DYSFUNCTION | ORGAN DAMAGE | IMMUNOLOGY | NICOTINIC ACETYLCHOLINE-RECEPTORS | RESPONSES | ALLERGY | INFLAMMATION | T(H)17 | retinoic acid receptor-related orphan receptor gamma t | DIFFERENTIATION | TH17 CELLS | LYMPHOCYTES | Animals, Newborn | Rats, Inbred SHR | Nuclear Receptor Subfamily 1, Group F, Member 3 - immunology | Nuclear Receptor Subfamily 1, Group F, Member 3 - antagonists & inhibitors | Poly I-C - pharmacology | Cells, Cultured | Interleukin-17 - immunology | Interleukin-17 - physiology | Interleukin-17 - genetics | Rats, Inbred WKY | Male | Hypertension - immunology | Spleen - cytology | Toll-Like Receptor 3 - agonists | NK Cell Lectin-Like Receptor Subfamily B - immunology | Digoxin - pharmacology | Hypertension - physiopathology | Vasodilation | Aging - immunology | Animals | Aorta, Thoracic - physiology | Blood Pressure - drug effects | Nuclear Receptor Subfamily 1, Group F, Member 3 - genetics | RNA - metabolism | Flow cytometry | Transcription factors | Digoxin | Disease | Helper cells | Nervous system | Lymphocytes T | Birth | Kinases | Signal transduction | Splenocytes | Lymphocytes | Rodents | Measurement methods | Blood pressure | Immune system | Spleen | Immune response | Cytokines | Rats | Pharmacology | Inflammation | T cell receptors | Interleukin 17 | Endothelium | Acids | Prostate | Surface markers | Retinoic acid | Nicotine
Journal Article
Immunity, ISSN 1074-7613, 2010, Volume 33, Issue 5, pp. 736 - 751
Journal Article
Journal of Hepatology, ISSN 0168-8278, 2012, Volume 58, Issue 1, pp. 155 - 168
Summary Bile acid (BA) transporters are critical for maintenance of the enterohepatic BA circulation where BAs exert their multiple physiological functions... 
Gastroenterology and Hepatology | Gallstones | Liver cancer | Bile acids | Fatty liver disease | Cholestasis | Liver regeneration | RAT-LIVER | SALT EXPORT PUMP | GROWTH-FACTOR 19 | ORGANIC ANION TRANSPORTERS | 90-PERCENT PARTIAL-HEPATECTOMY | URSODEOXYCHOLIC ACID | PRIMARY BILIARY-CIRRHOSIS | FARNESOID-X-RECEPTOR | GASTROENTEROLOGY & HEPATOLOGY | PHOSPHOLIPID-ASSOCIATED CHOLELITHIASIS | FAMILIAL INTRAHEPATIC CHOLESTASIS | Animals | Carrier Proteins - metabolism | Cholestasis - metabolism | Membrane Glycoproteins - metabolism | Humans | Liver - metabolism | Bile Acids and Salts - metabolism | Liver Diseases - metabolism | Liver Regeneration - physiology | Receptors, Cytoplasmic and Nuclear - metabolism | Drug resistance in microorganisms | Corticosteroids | Glucagon | Calcifediol | Ursodiol | Deoxycholic acid | Epidermal growth factor | Vitamin D | Physiological aspects | Fibroblast growth factors | Alfacalcidol | IBABP (FABP6, ILBP), intestinal bile acid-binding protein, fatty acid-binding protein 6 | PFIC, progressive familial intrahepatic cholestasis | TNFα, tumor necrosis factor α | 3 (human) | SRC2, p160 steroid receptor coactivator | NAFLD, non-alcoholic fatty liver disease | BA, bile acid | bile acid receptor | 8, cholesterol efflux pump, ATP-binding cassette, subfamily G, member 5 | UDCA, ursodeoxycholic acid | LRH-1 (NR5A2), liver receptor homolog-1 | LCA, lithocholic acid | LXRα (NR1H3), liver X receptor alpha | PPARγ (NR1C3), peroxisome proliferator-activated receptor gamma | OSTαβ, organic solute transporter alpha | ABCG5 | AMPK, AMP activated protein kinase | NASH, non-alcoholic steatohepatitis | SHP (NR0B2), short heterodimer partner | OATP1A2 (SLCO1A2, OATP1, OATP-A, SLC21A3), solute carrier organic anion transporter family, member 1A2 | EGFR, epidermal growth factor receptor | IL6, interleukin 6 | TGR5, G protein-coupled bile acid receptor | PH, partial hepatectomy | AE2, anion exchanger 2 | PSC, primary sclerosing cholangitis | OATP1B1 (SLCO1B1, OATP2, OATP-C, SLC21A6), solute carrier organic anion transporter family, member 1B1 | RARα (NR1B1), retinoic acid receptor alpha | GLP-1, glucagon like peptide 1 | VDR (NR1I1), vitamin D receptor. Please note that for the convenience of better readability and clarity, abbreviations for transporters and nuclear receptors were capitalized throughout this article when symbols were identical for human and rodents | MRP2 (ABCC2), multidrug resistance-associated protein 2, ATP-binding cassette, subfamily C, member 2 | NTCP (SLC10A1), sodium | CAR (NR1I3), constitutive androstane receptor | taurocholate cotransporting polypeptide, solute carrier family 10, member 1 | PPARα (NR1C1), peroxisome proliferator-activated receptor alpha | Review | GR (NR3C1), glucocorticoid receptor | Bile acids, Cholestasis, Fatty liver disease, Gallstones, Liver regeneration, Liver cancer | 19, fibroblast growth factor 15 | Mdr2 | ICP, intrahepatic cholestasis of pregnancy | BRIC, benign recurrent intrahepatic cholestasis | OATP1B3 (SLCO1B3, OATP8, SLC21A8), solute carrier organic anion transporter family, member 1B3 | MRP3 (ABCC3), multidrug resistance-associated protein 3, ATP-binding cassette, subfamily C, member 3 | beta | MDR1 (ABCB1), p-glycoprotein, ATP-binding cassette, subfamily B, member 1 | norUDCA, norursodeoxycholic acid | 6-ECDCA, 6-ethylchenodeoxycholic acid | FXR (NR1H4), farnesoid X receptor | BCRP (ABCG2), breast cancer resistance protein, ATP-binding cassette, subfamily G, member 2 | HNF4α (NR2A1), hepatocyte nuclear factor 4 alpha | PBC, primary biliary cirrhosis | MDR3 (ABCB4), multidrug resistance protein 2 (rodents) | HNF1α, hepatocyte nuclear factor 1 alpha | NR, nuclear receptor | FGF15 | RXRα (NR2B1), retinoid X receptor alpha | PXR (NR1I2), pregnane X receptor | BSEP (ABCB11), bile salt export pump | HCC, hepatocellular carcinoma | MRP4 (ABCC4), multidrug resistance-associated protein 4, ATP-binding cassette, subfamily C, member 4 | TPN, total parenteral nutrition
Journal Article
European Journal of Cancer, ISSN 0959-8049, 2005, Volume 41, Issue 10, pp. 1487 - 1494
We have investigated the presence of oestrogen receptor-related (ERR) mRNA in human colorectal tumour tissues and adjacent normal mucosa by reverse... 
Tumour progression | Peroxisome proliferator-activated receptor γ coactivator-1 | Oestrogen receptor beta | Peroxisome proliferator-activated receptor γ | Oestrogen receptor-related receptor | Colorectal carcinoma | Oestrogen receptor alpha | GAMMA | CELLS | tumour progression | peroxisome proliferator-activated receptor gamma coactivator-1 | oestrogen receptor beta | SUBTYPES | TRANSCRIPTION | oestrogen receptor alpha | oestrogen receptor-related receptor | colorectal carcinoma | COLON-CANCER | BREAST-CANCER | MUCOSA | ONCOLOGY | COACTIVATOR PGC-1 | MICE | peroxisome proliferator-activated receptor gamma | BINDING | Gene Expression | Receptors, Estrogen - metabolism | Receptors, Estrogen - genetics | Colorectal Neoplasms - genetics | Humans | Middle Aged | Male | Receptors, Cytoplasmic and Nuclear - genetics | PPAR gamma - metabolism | RNA, Messenger - metabolism | Disease Progression | Estrogen Receptor beta - metabolism | Transcription Factors - metabolism | Estrogen Receptor alpha - genetics | Estrogen Receptor beta - genetics | Reverse Transcriptase Polymerase Chain Reaction - methods | Aged, 80 and over | Estrogen Receptor alpha - metabolism | Female | Aged | Colorectal Neoplasms - metabolism | Receptors, Cytoplasmic and Nuclear - metabolism | Messenger RNA | Reverse transcriptase | Analysis | Gastrointestinal diseases | Estrogen | Colorectal cancer | Development and progression | Gene expression | Tumors
Journal Article
International Immunopharmacology, ISSN 1567-5769, 11/2013, Volume 17, Issue 3, pp. 638 - 650
Neutrophils play a critical role in the host defense against bacterial and fungal infections, but their inappropriate activation also contributes to tissue... 
Signaling | Receptors | Inflammation | Kinases | Neutrophils | ACTIVATED PROTEIN-KINASE | COLONY-STIMULATING FACTOR | LEUKOCYTE ADHESION DEFICIENCY | IMMUNOLOGY | SRC-FAMILY KINASES | HUMAN POLYMORPHONUCLEAR LEUKOCYTES | HIGH-AFFINITY RECEPTOR | TUMOR-NECROSIS-FACTOR | TOLL-LIKE RECEPTORS | PHARMACOLOGY & PHARMACY | BETA-GAMMA-SUBUNITS | NF-KAPPA-B | Signal Transduction - immunology | Animals | Receptors, Cell Surface - immunology | Humans | Neutrophils - immunology | Selectins - immunology | Mycoses | Lectins | Fc receptors | Integrins | FcR, Fc-receptor | GPI, glycosylphosphatidylinositol anchor | CLEC, C-type lectin | OSCAR, osteoclast-associated receptor | PKB, protein kinase B | DAG, diacyl-glycerol | Tyk2, tyrosine protein kinase 2 | VCAM-1, vascular cell adhesion molecule 1 | ICAM-1, intercellular adhesion molecule 1 | FADD, Fas-associated protein with death domain | IκB, inhibitor of NF-κB | GM-CSF, granulocyte | MyD88, myeloid differentiation protein 88 | TNF, tumor necrosis factor | LTβ, lymphotoxin β | TRADD, TNFR1-associated death domain protein | Abl, Abelson leukemia proto-oncogene | SLP-76, SH2 domain-containing leukocyte protein of 76 kDa | CALDAG-GEFI, calcium and DAG-regulated guanine nucleotide exchange factor I | IL, interleukin | Src, Rous sarcoma virus proto-oncogene | IRF, IFN regulatory factor | RIG, retinoic acid-inducible gene | PLC, phospholipase C | TCR, T-cell receptor | IKK, IκB kinase | ITAM, immunoreceptor tyrosine-based activation motif | CARD, caspase activation and recruitment domain | IP3, inositol-tris-phosphate | CHO, Chinese hamster ovary cells | MKK, MAP kinase kinase | fMLP, formly-Met-Leu-Phe | TRAF, TNF receptor-associated factor | MIP, macrophage inflammatory protein | Rac, Ras-related C3 botulinum toxin substrate | monocyte colony-stimulating factor | PIP3, phosphatidylinositol-3-phosphate | VLA-4, very late antigen 4 (α4β1 integrin) | PAF, platelet activating factor | STAT, signal transducer and activator of transcription | TAK, TGFβ-activated kinase 1 | Mac-1, macrophage antigen 1 (αMβ2 integrin) | FcRγ, Fc-receptor γ-chain | Asc, apoptosis-associated speck-like protein containing a CARD | cIAP, cellular inhibitor of apoptosis | BCR, B-cell receptor | Fgr, Gardner–Rasheed feline sarcoma proto-oncogene | VASP, vasodilator-stimulated phosphoprotein | Hck, hematopoietic cell kinase | TGFβ, transforming growth factor β | Rap, Ras-related protein | SHP-1, SH2 domain-containing protein tyrosine phosphatase 1 | Syk, spleen tyrosine kinase | GPCR, G protein-coupled receptor | G-CSF, granulocyte colony-stimulating factor | TREM, triggering receptor expressed on myeloid cells | DISC, death-inducing signaling complex | MDL-1, myeloid DAP12-associating lectin 1 | C3G, Crk SH3 domain-binding guanine nucleotide exchange factor (RapGEF1) | NF-κB, nuclear factor κB | ERM, ezrin-radixin-moesin | Epac1, exchange protein activated by cyclic AMP 1 | LTB4, leukotriene B4 | Mcl, macrophage C-type lectin | SAP130, Sin3A-associated protein of 130 kDa | SH2, Src-homology 2 domain | MAP kinase, mitogen-activated protein kinase | PSGL-1, P-selectin glycoprotein ligand | PI3K, phoshoinositide-3-kinase | ADAP, adhesion and degranulation promoting adapter protein (Fyb, SLAP-130) | NLRP3, NOD-like receptor family, pyrin domain containing 3 | MDA5, melanoma differentiation-associated protein 5 | TLR, Toll-like receptor | GRK, GPCR kinase | LAD, leukocyte adhesion deficiency | MAPKAP-kinase, MAP kinase-associated protein kinase | ZAP-70, ζ-chain-associated protein of 70 kDa | TRAIL, TNF-related apoptosis-inducing ligand | JNK, c-Jun N-terminal kinase | LFA-1, lymphocyte function-associated receptor 1 (αLβ2 integrin) | ROS, reactive oxygen species | RIP3, receptor-interacting serine-threonine protein kinase 3 | DAP12, DNAX activating protein 12 | IFN, interferon | PIR, paired immunoglobulin-like receptor | PKC, protein kinase C | PAK, p21-activated kinase | ESL-1, E-selectin ligand 1 | GAP, GTPase activating protein | ERK, extracellular signal-regulated kinase | SOCS, suppressor of cytokine signaling | JAK, Janus kinase | RANK, receptor activator of NF-κB | IRAK, IL-1 receptor-associated kinase | NOD, nucleotide-binding oligomerization domain containing protein | CEACAM3, carcinoembryonic antigen-related cell adhesion molecule 3 (CD66b)
Journal Article