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apratastat

structure in first source

Also Known As:

4-((4-(2-butynyloxy)phenyl)sulfonyl)-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide; TMI 005; TMI-005; TMI-1

Networked: 7 relevant articles (1 outcomes, 0 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Oxazines: 9
    - Morpholines: 6
      - apratastat: 7

Experts

1.	Brockhoff, Gero: 1 article (05/2021)
2.	Bronger, Holger: 1 article (05/2021)
3.	Dreyer, Tobias F: 1 article (05/2021)
4.	Ortmann, Olaf: 1 article (05/2021)
5.	Teoman, Attila: 1 article (05/2021)
6.	Wege, Anja Kathrin: 1 article (05/2021)
7.	Fang, Xianjun: 1 article (10/2020)
8.	He, Tianhai: 1 article (10/2020)
9.	Ma, Yibao: 1 article (10/2020)
10.	Mukherjee, Abir: 1 article (10/2020)

Related Diseases

1.	Experimental Arthritis 04/01/2004 - "In vivo, TMI-1 is highly effective in reducing clinical severity scores in mouse prophylactic collagen-induced arthritis (CIA) at 5, 10, and 20 mg/kg p.o. "
2.	Rheumatoid Arthritis 04/01/2011 - "Even though the dosage provided adequate exposure to inhibit TNF-α release, apratastat was not efficacious in rheumatoid arthritis (RA). " 11/01/2006 - "Drug evaluation: apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis." 01/01/2012 - "The thiomorpholine hydroxamate compound TMI-1 has been previously designed to inhibit metalloproteinase activity for the treatment of rheumatoid arthritis. " 11/01/2006 - "Wyeth Research was developing apratastat (TMI-005), one in a series of dual TNFalpha-converting enzyme and matrix metalloprotease-13 inhibitors, for the potential treatment of inflammation, especially rheumatoid arthritis. "
3.	Neoplasms (Cancer) 05/18/2021 - "TMI-1 and GI254023X caused a reduced shedding of CX3CL1 and of HER2 in vitro but without effects on tumor cell proliferation or viability. " 01/01/2012 - "We tested the effect of TMI-1 on luminal, basal and ERBB2-overexpressing breast tumor cell lines and on MMTV-ERBB2/neu tumor evolution. "
4.	Cystic Kidney Diseases (Cystic Kidney Disease) 09/01/2014 - "Using Western blotting, an enzyme activity assay, and a growth factor-shedding assay in the presence or absence of the specific ADAM17 inhibitor TMI-005, we show that increased expression and activation of ADAM17 in the cystic kidney and in collecting duct epithelial cells originating from the Ift88°(rpk) mice (designated as PKD cells) lead to constitutive shedding of several growth factors, including heparin-binding EGF-like growth factor (HB-EGF), amphiregulin, and transforming growth factor-α (TGF-α). "
5.	Ovarian Neoplasms (Ovarian Cancer) 10/01/2020 - "Inactivation of ADAM17, a disintegrin and metalloproteinase, with a specific inhibitor TMI-1 or by shRNA knockdown prevented ovarian cancer cells from releasing TNF-α protein in response to LPA, indicating that LPA-mediated TNF-α production relies on both transcriptional upregulations of the TNF-α gene and the activity of ADAM17, the membrane-associated TNF-α-converting enzyme. "

Related Drugs and Biologics

1.	Enzymes
2.	Metalloproteases (Metalloproteinases)
3.	Amphiregulin
4.	Heparin-binding EGF-like Growth Factor (HB-EGF)
5.	Matrix Metalloproteinase Inhibitors
6.	Intercellular Signaling Peptides and Proteins (Growth Factors)
7.	Small Interfering RNA (siRNA)
8.	Disintegrins
9.	Transforming Growth Factors (Transforming Growth Factor)
10.	Tumor Necrosis Factor-alpha (Tumor Necrosis Factor)