pyrazines has been researched along with cgs 27023a in 58 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 14 (24.14) | 18.2507 |
| 2000's | 39 (67.24) | 29.6817 |
| 2010's | 5 (8.62) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Authors | Studies |
|---|---|
| Blancuzzi, V; Ganu, VS; Goldberg, RL; Ludewig, R; MacPherson, LJ; O'Byrne, EM; Parker, DT; Roberts, ED; Singh, HN; Wilson, D | 1 |
| Doughty, J; Ganu, V; Goldberg, RL; O'Byrne, E; Spirito, S | 1 |
| Pratta, MA | 1 |
| Bayburt, EK; Blancuzzi, V; Capparelli, MP; Carroll, BJ; Doughty, JR; Fryer, L; Ganu, V; Goldberg, RL; Goldstein, R; Hu, S; Justice, MR; MacPherson, LJ; Melton, RA; O'Byrne, EM; Parker, DT; Spirito, S; Wilson, D; Zhu, L | 1 |
| Blancuzzi, V; Doughty, JR; Goldberg, RL; O'Byrne, E; Singh, HN; Spirito, S | 1 |
| Gonnella, NC; Li, YC; Paris, CG; Zhang, X | 1 |
| Epps, DE; Laborde, AL; Petzold, GL; Poorman, RA; Stuchly, CW; Van Drie, JH | 1 |
| Albright, JD; DiJoseph, JF; Killar, LM; Levin, JI; Roth, CE; Sharr, MA; Skotnicki, JS; Sung, A; Walter, T | 1 |
| Chanda, PK; Chen, JM; Cosmi, S; Edris, W; Moy, FJ; Powers, R; Skotnicki, JS; Wilhelm, J | 1 |
| Caplan, SL; Chou, M; Jeng, AY; Jeune, M; Prescott, MF; Sawyer, WK; Von Linden-Reed, J | 1 |
| Ganu, V; Melton, R; Roberts, D; Wang, W | 1 |
| Hande, KR; Nelson, AR; Rothenberg, ML | 1 |
| Caldarelli, M; Habermann, J; Ley, SV | 1 |
| Choi, L; Eskens, FA; Harris, AL; Levitt, NC; Mather, R; Sparreboom, A; Verweij, J | 1 |
| Chiba, T; Ko, K; Konda, Y; Nakajima, M; Takahashi, R; Yazumi, S; Yoshikawa, K | 1 |
| Brady, CS; FitzGerald, MX; Mackarel, AJ; O'Connor, CM; Russell, KJ | 1 |
| Chanda, PK; Chen, JM; Cosmi, S; Edris, W; Levin, JI; Moy, FJ; Powers, R | 1 |
| Hwang, JJ; Ip, MM; Lee, PP; Murphy, G | 1 |
| Choy, M; Dias, S; Hattori, K; Heissig, B; Lane, WJ; Moore, MA; Rabbany, SY; Rafii, S; Wood, J | 1 |
| Eckhardt, SG; Hidalgo, M | 1 |
| Hwang, JJ; Ip, MM; Lee, PP; Mead, L | 1 |
| Choi, L; Denis, LJ; Eskens, FA; Foekens, JA; Harris, AL; Levitt, NC; Nakajima, M; O'Byrne, KJ; Owen, SJ; Propper, DJ; Steward, WP; Talbot, DC; Verweij, J; Wilner, S; Wood, JM | 1 |
| Bauer, MM; Dollinger, H; Jung, B; Nar, H; Werle, K | 1 |
| Albright, JD; Chen, JM; Cowling, R; Delos Santos, E; DiJoseph, JF; Jin, G; Killar, LM; Levin, JI; Nelson, FC; Roth, CE; Sharr, MA; Skotnicki, JS; Sung, A | 1 |
| Bin Sun, H; Fei, X; Hutchins, GD; Lee Stone, K; Liu, X; Martinez, TD; Miller, KD; Mock, BH; Sledge, GW; Wang, JQ; Zheng, QH | 1 |
| Antolín, M; Guarner, F; Malagelada, JR; Medina, C; Radomski, A; Radomski, MW; Salas, A; Videla, S; Vilaseca, J | 1 |
| Hirayama, R; Inoue, Y; Ishibushi, E; Ito, Y; Kiyoi, T; Kondo, H; Kumihara, H; Miyasaka, T; Nakajima, F; Ohmoto, H; Sawa, M; Yamamoto, M; Yamamoto, T; Yoshiizumi, K; Yoshino, K | 1 |
| Corbett, RL; Covington, MB; Decicco, CP; Duan, JJ; He, X; Liu, RQ; Magolda, RL; Newton, RC; Roderick, J; Trzaskos, JM; Wexler, RR; Xue, CB | 1 |
| Kawai, N; Kawanishi, M; Nagao, S | 1 |
| Breyholz, HJ; Guilbert, B; Kopka, K; Law, MP; Levkau, B; Riemann, B; Schäfers, M; Schober, O; Schröer, S; Trub, M; Wagner, S | 1 |
| DiMicco, MA; Grodzinsky, AJ; Kim, YJ; Kumar, S; Lark, MW; Patwari, P; Pratta, MA; Siparsky, PN | 1 |
| Majumdar, TK; Tse, FL; Vedananda, S | 1 |
| Breyholz, HJ; Kopka, K; Law, MP; Levkau, B; Riemann, B; Schäfers, KP; Schäfers, M; Schober, O; Wagner, S | 1 |
| Hattori, K; Nakajima, M; Nakashima, E; Oku, N; Tamura, M; Tsukada, H; Unno, K; Yonezawa, S | 1 |
| Blackey, R; Cassidy, J; Choi, L; Devlin, M; Eatock, M; Johnson, J; Morrison, R; Owen, S; Twelves, C | 1 |
| Li, MY; Matsumoto, K; Mizuno, S; Nakamura, T | 1 |
| Askew, C; Cosgrove, D; Gratton, MA; Meehan, DT; Rao, VH | 1 |
| Matono, K; Mizobe, T; Nagase, H; Nakajima, M; Ogata, Y; Sasatomi, T; Shirouzu, K | 1 |
| Adachi, E; Akutsu, N; Amano, S; Kadoya, K; Matsunaga, Y; Nishiyama, T; Ogura, Y | 1 |
| Díaz-Gonzalez, F; Farre, E; Medina, C; Paz, MC; Quintero, E; Radomski, MW; Salas, A; Santana, A | 1 |
| Fujita, M; Harada, E; Ikegame, S; Inoshima, I; Nakanishi, Y; Ouchi, H; Ye, Q | 1 |
| Howes, JM; Laing, GD; Theakston, RD | 1 |
| Amano, S; Ehama, R; Matsunaga, Y; Nishiyama, T; Ogura, Y; Tagami, H | 1 |
| Breyholz, HJ; Kopka, K; Levkau, B; Schäfers, M; Schober, O; Wagner, S | 1 |
| Breyholz, HJ; Faust, A; Haufe, G; Höltke, C; Kopka, K; Law, MP; Levkau, B; Schäfers, M; Schober, O; Schröer, S; Wagner, S | 1 |
| Fujita, M; Harada, E; Ikegame, S; Inoshima, I; Kuwano, K; Nakanishi, Y; Ouchi, H; Ye, Q | 1 |
| Burke, SL; Huang, Z; Karnachi, P; Lagu, B; Murray, WV; Rhodes, KJ; Scannevin, RH; Wang, B; Wilson, LJ; Yang, SM | 1 |
| Burke, SL; Karnachi, P; Lagu, B; Murray, WV; Rhodes, KJ; Scannevin, RH; Wang, B; Wilson, LJ; Yang, SM | 1 |
| Kasaoka, T; Nakajima, M; Nishiyama, H; Okada, M | 1 |
| Breyholz, HJ; Faust, A; Höltke, C; Kopka, K; Schäfers, M; Schober, O; Wagner, S | 1 |
| Agrawal, A; Cohen, S; Jacobsen, J; Romero-Perez, D; Thomas, R; Villarreal, F; Yan, Y | 1 |
| Bremer, C; Breyholz, HJ; Faust, A; Heindel, W; Höltke, C; Kopka, K; Schäfers, M; Schober, O; Wagner, S; Waldeck, J; Waschkau, B | 1 |
| Agback, T; Isaksson, J; Kovacs, H | 1 |
| Baldock, PA; Kostenuik, PJ; Little, DG; McDonald, MM; Mikulec, K; Morse, A; Peacock, L | 1 |
| Fisher, GJ; Hammerberg, C; He, T; Li, Y; Quan, T; Voorhees, JJ; Xia, W | 1 |
| Behrends, M; Haufe, G; Kopka, K; Kumbhar, S; Schäfers, M; Schober, O; Wagner, S; Waller, M | 1 |
| Cook, H; Gillen, K; Large, JM; Love, EA; Matthews, D; Merritt, A; Patel, S; Sattikar, A | 1 |
1 review(s) available for pyrazines and cgs 27023a
| Article | Year |
|---|---|
Development of matrix metalloproteinase inhibitors in cancer therapy.
Topics: Animals; Antibiotics, Antineoplastic; Antineoplastic Agents; Biphenyl Compounds; Clinical Trials as Topic; Drugs, Investigational; Enzyme Inhibitors; Humans; Hydroxamic Acids; Imidazoles; Matrix Metalloproteinase Inhibitors; Neoplasms; Organic Chemicals; Phenylalanine; Phenylbutyrates; Protease Inhibitors; Pyrazines; Sulfonamides; Tetracycline; Tetracyclines; Thiophenes | 2001 |
3 trial(s) available for pyrazines and cgs 27023a
| Article | Year |
|---|---|
Effect of food on the pharmacokinetics of oral MMI270B (CGS 27023A), a novel matrix metalloproteinase inhibitor.
Topics: Administration, Oral; Area Under Curve; Dose-Response Relationship, Drug; Eating; Fasting; Humans; Hydroxamic Acids; Metalloendopeptidases; Neoplasms; Postprandial Period; Protease Inhibitors; Pyrazines; Sulfonamides | 2000 |
Phase I and pharmacological study of the oral matrix metalloproteinase inhibitor, MMI270 (CGS27023A), in patients with advanced solid cancer.
Topics: Administration, Oral; Adult; Aged; Area Under Curve; Dose-Response Relationship, Drug; Exanthema; Female; Humans; Hydroxamic Acids; Male; Metabolic Clearance Rate; Metalloendopeptidases; Middle Aged; Musculoskeletal Diseases; Nausea; Neoplasms; Protease Inhibitors; Pyrazines; Sulfonamides; Treatment Outcome | 2001 |
A dose-finding and pharmacokinetic study of the matrix metalloproteinase inhibitor MMI270 (previously termed CGS27023A) with 5-FU and folinic acid.
Topics: Administration, Oral; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Colonic Neoplasms; Drug Interactions; Female; Fluorouracil; Humans; Hydroxamic Acids; Leucovorin; Male; Metalloendopeptidases; Middle Aged; Protease Inhibitors; Pyrazines; Rectal Neoplasms; Sulfonamides | 2005 |
54 other study(ies) available for pyrazines and cgs 27023a
| Article | Year |
|---|---|
Oral administration of a matrix metalloproteinase inhibitor, CGS 27023A, protects the cartilage proteoglycan matrix in a partial meniscectomy model of osteoarthritis in rabbits.
Topics: Animals; Cartilage, Articular; Hindlimb; Hydroxamic Acids; Joints; Male; Metalloendopeptidases; Osteoarthritis; Protease Inhibitors; Proteoglycans; Pyrazines; Rabbits; Sulfonamides | 1995 |
Metalloprotease inhibitors halt collagen breakdown in IL-1 induced bovine nasal cartilage cultures.
Topics: Animals; Cartilage; Cattle; Collagen; Hydroxamic Acids; Interleukin-1; Metalloendopeptidases; Nasal Mucosa; Nose; Organ Culture Techniques; Protease Inhibitors; Proteoglycans; Pyrazines; Sulfonamides | 1995 |
Biological evaluation of matrix metalloproteinase inhibitors, 18 May 1995, New York.
Topics: Animals; Humans; Hydroxamic Acids; Metalloendopeptidases; Osteoarthritis; Protease Inhibitors; Proteoglycans; Pyrazines; Sulfonamides | 1995 |
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.
Topics: Administration, Oral; Animals; Binding Sites; Cartilage; Chromatography, High Pressure Liquid; Enzyme-Linked Immunosorbent Assay; Humans; Hydroxamic Acids; In Vitro Techniques; Kinetics; Matrix Metalloproteinase Inhibitors; Models, Chemical; Protease Inhibitors; Pyrazines; Rabbits; Rats; Recombinant Proteins; Structure-Activity Relationship; Substance P; Sulfonamides | 1997 |
The effect of CGS 27023A on the level of 3B3 (-) epitope in a rabbit meniscectomy model.
Topics: Animals; Enzyme-Linked Immunosorbent Assay; Epitopes; Glucuronates; Glucuronic Acid; Hydroxamic Acids; Kinetics; Knee Joint; Male; Menisci, Tibial; Metalloendopeptidases; Osteoarthritis; Protease Inhibitors; Pyrazines; Rabbits; Sulfonamides | 1997 |
Bioactive conformation of a potent stromelysin inhibitor determined by X-nucleus filtered and multidimensional NMR spectroscopy.
Topics: Binding Sites; Collagenases; Computer Simulation; Fibroblasts; Humans; Hydroxamic Acids; Magnetic Resonance Spectroscopy; Matrix Metalloproteinase 3; Matrix Metalloproteinase Inhibitors; Models, Molecular; Protease Inhibitors; Protein Binding; Protein Conformation; Pyrazines; Sulfonamides | 1997 |
The constituent tryptophans and bisANS as fluorescent probes of the active site and of a secondary binding site of stromelysin-1 (MMP-3).
Topics: Acrylamides; Anilino Naphthalenesulfonates; Binding Sites; Catalytic Domain; Fluorescence Polarization; Fluorescent Dyes; Hydroxamic Acids; Matrix Metalloproteinase 3; Matrix Metalloproteinase Inhibitors; Models, Chemical; Phenylalanine; Protease Inhibitors; Protein Binding; Pyrazines; Spectrometry, Fluorescence; Sulfonamides; Thiophenes; Tryptophan | 1998 |
The synthesis and biological activity of a novel series of diazepine MMP inhibitors.
Topics: Animals; Antineoplastic Agents; Azepines; Enzyme Inhibitors; Hydroxamic Acids; Matrix Metalloproteinase 1; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Mice; Organic Chemicals; Protease Inhibitors; Pyrazines; Structure-Activity Relationship; Sulfonamides | 1998 |
NMR solution structure of the catalytic fragment of human fibroblast collagenase complexed with a sulfonamide derivative of a hydroxamic acid compound.
Topics: Catalysis; Collagenases; Computer Simulation; Crystallography, X-Ray; Fibroblasts; Humans; Hydroxamic Acids; Macromolecular Substances; Matrix Metalloproteinase 1; Matrix Metalloproteinase 3; Matrix Metalloproteinase 8; Matrix Metalloproteinase Inhibitors; Models, Molecular; Nuclear Magnetic Resonance, Biomolecular; Peptide Fragments; Protease Inhibitors; Protein Conformation; Pyrazines; Solutions; Sulfonamides | 1999 |
Effect of matrix metalloproteinase inhibition on progression of atherosclerosis and aneurysm in LDL receptor-deficient mice overexpressing MMP-3, MMP-12, and MMP-13 and on restenosis in rats after balloon injury.
Topics: Animals; Aorta, Abdominal; Aortic Aneurysm, Abdominal; Arteriosclerosis; Carotid Arteries; Carotid Artery Injuries; Catheterization; Cell Movement; Collagenases; Elastin; Hydroxamic Acids; Male; Matrix Metalloproteinase 12; Matrix Metalloproteinase 13; Matrix Metalloproteinase 3; Metalloendopeptidases; Mice; Mice, Knockout; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Receptors, LDL; Recurrence; Sulfonamides; Transcription, Genetic | 1999 |
Matrix metalloproteinase inhibitor CGS 27023A protects COMP and proteoglycan in the bovine articular cartilage but not the release of their fragments from cartilage after prolonged stimulation in vitro with IL-1 alpha.
Topics: Animals; Cartilage Oligomeric Matrix Protein; Cartilage, Articular; Cattle; Extracellular Matrix Proteins; Glycoproteins; Humans; Hydroxamic Acids; Interleukin-1; Kinetics; Matrilin Proteins; Metalloendopeptidases; Organ Culture Techniques; Protease Inhibitors; Proteoglycans; Pyrazines; Recombinant Proteins; Sulfonamides; Time Factors | 1999 |
New drugs on the horizon: matrix metalloproteinase inhibitors.
Topics: Antineoplastic Agents; Azepines; Biphenyl Compounds; Humans; Hydroxamic Acids; Metalloendopeptidases; Organic Chemicals; Phenylalanine; Phenylbutyrates; Protease Inhibitors; Pyrazines; Sulfonamides; Thiophenes | 1999 |
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.
Topics: Chemistry, Organic; Chromatography, Liquid; Hydroxamic Acids; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mass Spectrometry; Matrix Metalloproteinase Inhibitors; Metalloendopeptidases; Polymers; Protease Inhibitors; Pyrazines; Sulfonamides | 1999 |
CGS 27023A. CDG 27023A.
Topics: Animals; Antineoplastic Agents; Antirheumatic Agents; Drugs, Investigational; Humans; Hydroxamic Acids; Metalloendopeptidases; Mice; Neoplasms; Protease Inhibitors; Pyrazines; Rabbits; Rats; Rheumatic Diseases; Sulfonamides | 1999 |
Activation of fibroblast-derived matrix metalloproteinase-2 by colon-cancer cells in non-contact Co-cultures.
Topics: Basement Membrane; Blotting, Northern; Caco-2 Cells; Cell Line; Cell Membrane; Chelating Agents; Coculture Techniques; Colonic Neoplasms; Edetic Acid; Enzyme Activation; Fibroblasts; Gelatin; Humans; Hydroxamic Acids; Matrix Metalloproteinase 2; Matrix Metalloproteinases, Membrane-Associated; Metalloendopeptidases; Protease Inhibitors; Pyrazines; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sulfonamides; Tissue Inhibitor of Metalloproteinase-2; Tumor Cells, Cultured | 2000 |
Interleukin-8 and leukotriene-B(4), but not formylmethionyl leucylphenylalanine, stimulate CD18-independent migration of neutrophils across human pulmonary endothelial cells in vitro.
Topics: CD11 Antigens; CD18 Antigens; Cell Line; Cell Movement; Chemotactic Factors; Dose-Response Relationship, Drug; Endothelium, Vascular; Glycine; Humans; Hydroxamic Acids; Interleukin-8; L-Selectin; Leukotriene B4; Lung; N-Formylmethionine Leucyl-Phenylalanine; Neutrophils; Permeability; Phenylalanine; Protease Inhibitors; Pyrazines; Sulfonamides; Thiophenes | 2000 |
High-resolution solution structure of the catalytic fragment of human collagenase-3 (MMP-13) complexed with a hydroxamic acid inhibitor.
Topics: Amino Acid Sequence; Binding Sites; Catalytic Domain; Collagenases; Crystallography, X-Ray; Humans; Hydroxamic Acids; Inhibitory Concentration 50; Matrix Metalloproteinase 1; Matrix Metalloproteinase 13; Matrix Metalloproteinase Inhibitors; Models, Molecular; Molecular Sequence Data; Nuclear Magnetic Resonance, Biomolecular; Peptide Fragments; Protease Inhibitors; Protein Structure, Secondary; Pyrazines; Sequence Alignment; Sequence Homology, Amino Acid; Solutions; Sulfonamides; Zinc | 2000 |
Functional significance of MMP-9 in tumor necrosis factor-induced proliferation and branching morphogenesis of mammary epithelial cells.
Topics: Animals; Antibodies; Cell Division; Cells, Cultured; Enzyme Induction; Epithelial Cells; Female; Hydroxamic Acids; Mammary Glands, Animal; Matrix Metalloproteinase 9; Phenylalanine; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides; Thiophenes; Tumor Necrosis Factor-alpha | 2000 |
Stromal-derived factor 1-induced megakaryocyte migration and platelet production is dependent on matrix metalloproteinases.
Topics: Adult; Animals; Blood Platelets; Cells, Cultured; Chemokine CXCL12; Chemokines, CXC; Chemotactic Factors; Chemotaxis; Culture Media, Serum-Free; Enzyme Induction; Extracellular Matrix Proteins; Humans; Hydroxamic Acids; Leukemia, Megakaryoblastic, Acute; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Megakaryocytes; Metalloendopeptidases; Mice; Mice, Inbred BALB C; Protease Inhibitors; Pyrazines; Receptors, CXCR4; Recombinant Fusion Proteins; Sulfonamides; Thrombin; Thrombopoietin; Tissue Inhibitor of Metalloproteinase-1; Transfection; Tumor Cells, Cultured | 2000 |
Functional role of matrix metalloproteinases (MMPs) in mammary epithelial cell development.
Topics: Animals; Cell Size; Cells, Cultured; Culture Media, Conditioned; Culture Media, Serum-Free; Epidermal Growth Factor; Epithelial Cells; Extracellular Matrix; Female; Gelatinases; Humans; Hydroxamic Acids; Immunoblotting; Mammary Glands, Animal; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Organoids; Peptides; Phenylalanine; Phenylmercury Compounds; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides; Thiophenes; Transforming Growth Factor alpha | 2001 |
Crystal structure of human macrophage elastase (MMP-12) in complex with a hydroxamic acid inhibitor.
Topics: Amino Acid Sequence; Binding Sites; Cations, Divalent; Crystallization; Crystallography, X-Ray; Drug Design; Humans; Hydrogen Bonding; Hydroxamic Acids; Macrophages; Matrix Metalloproteinase 12; Metalloendopeptidases; Models, Molecular; Molecular Sequence Data; Protease Inhibitors; Protein Conformation; Pyrazines; Sequence Alignment; Substrate Specificity; Sulfonamides; Zinc | 2001 |
Benzodiazepine inhibitors of the MMPs and TACE.
Topics: ADAM Proteins; ADAM17 Protein; Benzodiazepines; Cartilage; Hydroxamic Acids; Indicators and Reagents; Matrix Metalloproteinase Inhibitors; Metalloendopeptidases; Protease Inhibitors; Pyrazines; Structure-Activity Relationship; Sulfonamides | 2002 |
Synthesis and preliminary biological evaluation of MMP inhibitor radiotracers [11C]methyl-halo-CGS 27023A analogs, new potential PET breast cancer imaging agents.
Topics: Animals; Biomarkers, Tumor; Breast Neoplasms; Carbon Radioisotopes; Humans; Hydroxamic Acids; Metalloendopeptidases; Protease Inhibitors; Pyrazines; Radiopharmaceuticals; Sulfonamides; Tomography, Emission-Computed | 2002 |
Increased activity and expression of matrix metalloproteinase-9 in a rat model of distal colitis.
Topics: Animals; Anticoagulants; Colitis, Ulcerative; Colon; Dextran Sulfate; Diarrhea; Disease Models, Animal; Gastrointestinal Hemorrhage; Hydroxamic Acids; Male; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Protease Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides | 2003 |
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydropyrido[3,4-b]pyrazine-based hydroxamic acids as HB-EGF shedding inhibitors.
Topics: Epidermal Growth Factor; Heparin-binding EGF-like Growth Factor; Humans; Hydroxamic Acids; Intercellular Signaling Peptides and Proteins; Protease Inhibitors; Pyrazines; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Tumor Cells, Cultured | 2003 |
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Topics: ADAM Proteins; ADAM17 Protein; Drug Design; Enzyme Inhibitors; Hydroxamic Acids; Metalloendopeptidases; Models, Molecular; Molecular Conformation; Protease Inhibitors; Pyrazines; Structure-Activity Relationship; Succinates; Sulfonamides | 2003 |
Treatment of cold injury-induced brain edema with a nonspecific matrix metalloproteinase inhibitor MMI270 in rats.
Topics: Animals; Blood-Brain Barrier; Body Water; Brain; Brain Edema; Brain Injuries; Capillary Permeability; Cold Temperature; Enzyme Inhibitors; Hydroxamic Acids; Male; Matrix Metalloproteinase Inhibitors; Parietal Lobe; Pyrazines; Rats; Rats, Sprague-Dawley; Staining and Labeling; Sulfonamides | 2003 |
Synthesis and preliminary biological evaluation of new radioiodinated MMP inhibitors for imaging MMP activity in vivo.
Topics: Animals; Feasibility Studies; Hydroxamic Acids; Iodine Radioisotopes; Isotope Labeling; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Metabolic Clearance Rate; Mice; Mice, Inbred C57BL; Organ Specificity; Pilot Projects; Pyrazines; Radiopharmaceuticals; Sulfonamides; Tissue Distribution | 2004 |
Mechanisms and kinetics of glycosaminoglycan release following in vitro cartilage injury.
Topics: Animals; Cartilage, Articular; Cattle; Cell Survival; Dipeptides; Endopeptidases; Glycosaminoglycans; Hydroxamic Acids; In Vitro Techniques; Indenes; Kinetics; Pressure; Protease Inhibitors; Pyrazines; Sulfonamides; Time Factors; Wounds and Injuries | 2004 |
Rapid analysis of MMI270B, an inhibitor of matrix metalloproteases in human plasma by liquid chromatography-tandem mass spectrometry: matrix interference in patient samples.
Topics: Chromatography, Liquid; Humans; Hydroxamic Acids; Mass Spectrometry; Matrix Metalloproteinase Inhibitors; Protease Inhibitors; Pyrazines; Reproducibility of Results; Sensitivity and Specificity; Sulfonamides | 2004 |
Scintigraphic imaging of matrix metalloproteinase activity in the arterial wall in vivo.
Topics: Animals; Apolipoproteins E; Autoradiography; Carotid Artery, Common; Diet, Atherogenic; Feasibility Studies; Hydroxamic Acids; Iodine Radioisotopes; Ligation; Macrophages; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Mice; Mice, Inbred C57BL; Mice, Knockout; Protease Inhibitors; Pyrazines; Radionuclide Imaging; Radiopharmaceuticals; Sulfonamides | 2004 |
In vivo trafficking of endothelial progenitor cells their possible involvement in the tumor neovascularization.
Topics: Animals; Cell Line, Tumor; Cell Movement; Dose-Response Relationship, Drug; Endothelium, Vascular; Fluorodeoxyglucose F18; Gamma Rays; Hydroxamic Acids; Metalloendopeptidases; Neoplasm Transplantation; Neoplasms, Experimental; Neovascularization, Pathologic; Pyrazines; Rats; Stem Cells; Sulfonamides; Tomography, Emission-Computed | 2004 |
HGF reduces advancing lung fibrosis in mice: a potential role for MMP-dependent myofibroblast apoptosis.
Topics: Actins; Animals; Apoptosis; Bleomycin; Cell Line; Enzyme Inhibitors; Fibroblasts; Fibronectins; Hepatocyte Growth Factor; Humans; Hydroxamic Acids; Lung; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Mice, Inbred C57BL; Muscle Cells; Proto-Oncogene Proteins c-met; Pulmonary Fibrosis; Pyrazines; Recombinant Proteins; Signal Transduction; Sulfonamides; Tissue Distribution | 2005 |
Matrix metalloproteinase dysregulation in the stria vascularis of mice with Alport syndrome: implications for capillary basement membrane pathology.
Topics: Animals; Basement Membrane; Capillaries; Computer Systems; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Mice, Knockout; Nephritis, Hereditary; Protease Inhibitors; Pyrazines; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Stria Vascularis; Sulfonamides | 2005 |
Efficacy of the MMP inhibitor MMI270 against lung metastasis following removal of orthotopically transplanted human colon cancer in rat.
Topics: Administration, Oral; Animals; Apoptosis; Chemoprevention; Colonic Neoplasms; Humans; Hydroxamic Acids; Lung Neoplasms; Neoplastic Cells, Circulating; Neovascularization, Pathologic; Pyrazines; Rats; Rats, Nude; Sulfonamides; Survival Analysis; Transplantation, Heterologous | 2006 |
Protective effect of matrix metalloproteinase inhibitors against epidermal basement membrane damage: skin equivalents partially mimic photoageing process.
Topics: Basement Membrane; Cell Adhesion Molecules; Cells, Cultured; Collagen Type IV; Collagen Type VII; Enzyme-Linked Immunosorbent Assay; Epidermis; Humans; Hydroxamic Acids; Kalinin; Male; Matrix Metalloproteinase 1; Matrix Metalloproteinase 2; Matrix Metalloproteinase 3; Matrix Metalloproteinase 9; Microscopy, Electron; Models, Biological; Oligopeptides; Protease Inhibitors; Pyrazines; Skin Aging; Sulfonamides; Tissue Inhibitor of Metalloproteinase-1; Tissue Inhibitor of Metalloproteinase-2; Ultraviolet Rays | 2005 |
Matrix metalloproteinase-9 modulates intestinal injury in rats with transmural colitis.
Topics: Animals; Colitis; Colon; Disease Models, Animal; Enzyme Activation; Enzyme Inhibitors; Hydroxamic Acids; Inflammation Mediators; Intestinal Mucosa; Male; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Neutrophils; Pyrazines; Rats; Rats, Sprague-Dawley; Sulfonamides; Trinitrobenzenesulfonic Acid; Up-Regulation | 2006 |
Doxycycline attenuated lung injury by its biological effect apart from its antimicrobial function.
Topics: Animals; Anti-Bacterial Agents; Disease Models, Animal; Doxycycline; Drug Resistance, Bacterial; Hydroxamic Acids; Immunologic Factors; Inflammation; Lipopolysaccharides; Lung; Lung Diseases; Matrix Metalloproteinases; Mice; Mice, Inbred C57BL; Neutrophils; Pulmonary Alveoli; Pyrazines; Streptococcus pneumoniae; Sulfonamides | 2007 |
Neutralization of the haemorrhagic activities of viperine snake venoms and venom metalloproteinases using synthetic peptide inhibitors and chelators.
Topics: Animals; Biphenyl Compounds; Chelating Agents; Chromatography, Gel; Chromatography, Liquid; Edetic Acid; Egtazic Acid; Ethylenediamines; Evaluation Studies as Topic; Hemorrhage; Hydroxamic Acids; Metalloproteases; Mice; Molecular Structure; Organic Chemicals; Phenylbutyrates; Protein Kinase Inhibitors; Pyrazines; Snake Bites; Statistics, Nonparametric; Sulfonamides; Viper Venoms | 2007 |
Establishment of a mouse skin model of the lichenification in human chronic eczematous dermatitis.
Topics: Animals; Disease Models, Animal; Eczema; Epidermis; Glycine; Glycine Agents; Humans; Hydroxamic Acids; Male; Metalloendopeptidases; Mice; Mice, Hairless; Pyrazines; Skin Aging; Sulfonamides | 2007 |
A 18F-radiolabeled analogue of CGS 27023A as a potential agent for assessment of matrix-metalloproteinase activity in vivo.
Topics: Drug Delivery Systems; Enzyme Activation; Feasibility Studies; Fluorine Radioisotopes; Hydroxamic Acids; Isotope Labeling; Matrix Metalloproteinases; Pyrazines; Radiopharmaceuticals; Sulfonamides | 2007 |
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET.
Topics: Animals; Enzyme Activation; Female; Fluorine Radioisotopes; Humans; Hydroxamic Acids; Ligands; Male; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Mice; Mice, Inbred C57BL; Positron-Emission Tomography; Pyrazines; Radiopharmaceuticals; Stereoisomerism; Structure-Activity Relationship; Sulfonamides; Tissue Distribution | 2007 |
The role of collagenases in experimental pulmonary fibrosis.
Topics: Administration, Oral; Animals; Bleomycin; Bronchoalveolar Lavage Fluid; Collagenases; Gelatin; Hydroxamic Acids; Hydroxyproline; Immunoblotting; Male; Matrix Metalloproteinase Inhibitors; Mice; Mice, Inbred ICR; Protease Inhibitors; Pulmonary Fibrosis; Pyrazines; Sulfonamides | 2008 |
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
Topics: Amino Acids; Animals; Brain Edema; Disease Models, Animal; Drug Design; Gelatinases; Humans; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Microsomes, Liver; Middle Cerebral Artery; Molecular Structure; Pyrazines; Rats; Stereoisomerism; Structure-Activity Relationship; Sulfonamides | 2008 |
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 1. Design, synthesis, and lead identification.
Topics: Animals; Drug Design; Gelatinases; Humans; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Microsomes, Liver; Molecular Structure; Pyrazines; Rats; Structure-Activity Relationship; Sulfonamides | 2008 |
Matrix metalloproteinase inhibitor, MMI270 (CGS27023A) inhibited hematogenic metastasis of B16 melanoma cells in both experimental and spontaneous metastasis models.
Topics: Animals; Hydroxamic Acids; Lung Neoplasms; Male; Matrix Metalloproteinase Inhibitors; Melanoma, Experimental; Mice; Neoplasm Metastasis; Protease Inhibitors; Pyrazines; Sulfonamides | 2008 |
A new 18F-labelled derivative of the MMP inhibitor CGS 27023A for PET: radiosynthesis and initial small-animal PET studies.
Topics: Animals; Fluorine Radioisotopes; Hydroxamic Acids; Matrix Metalloproteinase Inhibitors; Mice; Mice, Inbred C57BL; Positron-Emission Tomography; Protease Inhibitors; Pyrazines; Sulfonamides | 2009 |
Effects of novel semiselective matrix metalloproteinase inhibitors on ex vivo cardiac structure-function.
Topics: Animals; Coronary Circulation; Hydroxamic Acids; Male; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Myocardial Contraction; Myocardial Stunning; Oligopeptides; Pyrazines; Pyridones; Pyrones; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Sulfonamides | 2009 |
Synthesis and evaluation of a novel hydroxamate based fluorescent photoprobe for imaging of matrix metalloproteinases.
Topics: Carbocyanines; Cell Line, Tumor; Enzyme Inhibitors; Fluorescent Dyes; Humans; Hydroxamic Acids; Ligands; Matrix Metalloproteinase Inhibitors; Matrix Metalloproteinases; Molecular Imaging; Polyethylene Glycols; Protein Biosynthesis; Pyrazines; Sulfonamides; Transcription, Genetic | 2009 |
Probing water-protein contacts in a MMP-12/CGS27023A complex by nuclear magnetic resonance spectroscopy.
Topics: Humans; Hydroxamic Acids; Matrix Metalloproteinase 12; Matrix Metalloproteinase Inhibitors; Nitrogen Isotopes; Nuclear Magnetic Resonance, Biomolecular; Protease Inhibitors; Protein Conformation; Pyrazines; Sulfonamides; Water | 2012 |
Matrix metalloproteinase-driven endochondral fracture union proceeds independently of osteoclast activity.
Topics: Animals; Bone Density Conservation Agents; Clodronic Acid; Collagenases; Diphosphonates; Femoral Fractures; Fracture Healing; Humans; Hydroxamic Acids; Imidazoles; Male; Matrix Metalloproteinase Inhibitors; Osteoclasts; Osteoprotegerin; Pyrazines; Rats; Rats, Wistar; Recombinant Proteins; Sulfonamides; Time Factors; Zoledronic Acid | 2013 |
Expression of catalytically active matrix metalloproteinase-1 in dermal fibroblasts induces collagen fragmentation and functional alterations that resemble aged human skin.
Topics: Actins; Adenoviridae; Adult; Aged, 80 and over; Cell Shape; Cells, Cultured; Collagen Type I; Dermis; Enzyme Activation; Fibroblasts; Gene Expression Regulation, Enzymologic; HEK293 Cells; Humans; Hydroxamic Acids; Matrix Metalloproteinase 1; Models, Biological; Pyrazines; RNA, Small Interfering; Skin Aging; Sulfonamides; Temperature; Time Factors; Transfection; Young Adult | 2013 |
New matrix metalloproteinase inhibitors based on γ-fluorinated α-aminocarboxylic and α-aminohydroxamic acids.
Topics: Binding Sites; Carboxylic Acids; Halogenation; Humans; Hydrogen Bonding; Hydroxamic Acids; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Matrix Metalloproteinase Inhibitors; Models, Molecular; Molecular Structure; Protein Binding; Protein Conformation; Pyrazines; Sulfonamides | 2015 |
Developing an Antibody-Drug Conjugate Approach to Selective Inhibition of an Extracellular Protein.
Topics: Animals; Antibodies, Monoclonal, Murine-Derived; Cell Line; Enzyme Assays; Fluorometry; Humans; Hydroxamic Acids; Immunoconjugates; Matrix Metalloproteinase 9; Mice; Protease Inhibitors; Protein Binding; Pyrazines; Sulfonamides | 2019 |