PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 33922533-8 2021 Here, we tested the effect of the ADAM17 inhibitor GW280264X in combination with cisplatin on ovarian cancer cells in 2D and 3D. GW280264X 51-60 ADAM metallopeptidase domain 17 Homo sapiens 34-40 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 ADAM metallopeptidase domain 17 Homo sapiens 47-51 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 ADAM metallopeptidase domain 10 Homo sapiens 63-69 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 C-X3-C motif chemokine ligand 1 Homo sapiens 149-155 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 C-X3-C motif chemokine ligand 1 Homo sapiens 168-174 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 C-X3-C motif chemokine ligand 1 Homo sapiens 168-174 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 ADAM metallopeptidase domain 10 Homo sapiens 261-267 12714508-5 2003 The hydroxamate GW280264X, capable of blocking TACE as well as ADAM10, proved to be an effective inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage in CX3CL1-expressing ECV-304 cells (CX3CL1-ECV-304), whereas GI254023X, preferentially blocking ADAM10 but not TACE, reduced the constitutive cleavage only. GW280264X 16-25 ADAM metallopeptidase domain 17 Homo sapiens 276-280 30826330-8 2019 Thus, recent progress has identified the "sheddase" activity of ADAMs as a viable target and the development of GW280264X is an experimental ADAM17 inhibitor. GW280264X 112-121 ADAM metallopeptidase domain 17 Homo sapiens 141-147 19432809-6 2009 This release was inhibited by the metalloproteinase inhibitor batimastat; however, ADAM10/ADAM17 inhibitor GW280264X only partially affected shedding activity. GW280264X 107-116 ADAM metallopeptidase domain 10 Homo sapiens 83-89 19432809-6 2009 This release was inhibited by the metalloproteinase inhibitor batimastat; however, ADAM10/ADAM17 inhibitor GW280264X only partially affected shedding activity. GW280264X 107-116 ADAM metallopeptidase domain 17 Homo sapiens 90-96 15215246-5 2004 The hydroxamate GW280264X, which is capable of blocking TACE and the closely related disintegrin-like metalloproteinase 10 (ADAM10), effectively inhibited both spontaneous and PMA-inducible cleavage of IL-15Ralpha, whereas GI254023X, which preferentially blocks ADAM10, was ineffective. GW280264X 16-25 a disintegrin and metallopeptidase domain 17 Mus musculus 56-60 15215246-5 2004 The hydroxamate GW280264X, which is capable of blocking TACE and the closely related disintegrin-like metalloproteinase 10 (ADAM10), effectively inhibited both spontaneous and PMA-inducible cleavage of IL-15Ralpha, whereas GI254023X, which preferentially blocks ADAM10, was ineffective. GW280264X 16-25 a disintegrin and metallopeptidase domain 10 Mus musculus 124-130 15215246-5 2004 The hydroxamate GW280264X, which is capable of blocking TACE and the closely related disintegrin-like metalloproteinase 10 (ADAM10), effectively inhibited both spontaneous and PMA-inducible cleavage of IL-15Ralpha, whereas GI254023X, which preferentially blocks ADAM10, was ineffective. GW280264X 16-25 interleukin 15 receptor, alpha chain Mus musculus 202-213 15215246-5 2004 The hydroxamate GW280264X, which is capable of blocking TACE and the closely related disintegrin-like metalloproteinase 10 (ADAM10), effectively inhibited both spontaneous and PMA-inducible cleavage of IL-15Ralpha, whereas GI254023X, which preferentially blocks ADAM10, was ineffective. GW280264X 16-25 a disintegrin and metallopeptidase domain 10 Mus musculus 262-268 33045304-6 2021 Increased MICA shedding was prevented by the ADAM inhibitor GW280264X, rendering BCSC as sensitive to gammadeltaTc cytotoxicity as NSC. GW280264X 60-69 MHC class I polypeptide-related sequence A Homo sapiens 10-14 29662625-11 2018 Inhibition of ADAM17 with either GW280264X or the anti-ADAM17 antibody D1 (A12) as well as silencing of ADAM17 by siRNA selectively reduced AREG release. GW280264X 33-42 ADAM metallopeptidase domain 17 Homo sapiens 14-20 28264989-5 2017 With respect to the inhibitor profile, we found that ADAM9 was inhibited by the hydroxamate-based metalloprotease inhibitors marimastat, TAPI-2, BB94, GM6001 and GW280264X, and by 10 nM of the tissue inhibitor of metalloproteinases (TIMP)-3, but not by up to 20 nM of TIMP-1 or -2. GW280264X 162-171 ADAM metallopeptidase domain 9 Homo sapiens 53-58 22367719-3 2012 In vitro, endotoxin-mediated induction of endothelial permeability and IL-8-induced transmigration of neutrophils through human microvascular endothelial cells required ADAM17 as shown by inhibition with GW280264X or shRNA-mediated knockdown. GW280264X 204-213 C-X-C motif chemokine ligand 8 Homo sapiens 71-75 22367719-3 2012 In vitro, endotoxin-mediated induction of endothelial permeability and IL-8-induced transmigration of neutrophils through human microvascular endothelial cells required ADAM17 as shown by inhibition with GW280264X or shRNA-mediated knockdown. GW280264X 204-213 ADAM metallopeptidase domain 17 Homo sapiens 169-175 22367719-6 2012 Induced vascular permeability, oedema formation, release of TNF-alpha and IL-6 and pulmonary leukocyte recruitment were all markedly reduced by GW280264X or endothelial adam17-knockout. GW280264X 144-153 tumor necrosis factor Homo sapiens 60-69 22367719-6 2012 Induced vascular permeability, oedema formation, release of TNF-alpha and IL-6 and pulmonary leukocyte recruitment were all markedly reduced by GW280264X or endothelial adam17-knockout. GW280264X 144-153 interleukin 6 Homo sapiens 74-78 21111811-6 2011 GW280264X that targets both ADAM10 and ADAM17 blocked IL-6-induced proliferation and ERK1/2 phosphorylation with same potency as GM6001. GW280264X 0-9 ADAM metallopeptidase domain 10 Homo sapiens 28-34 21111811-6 2011 GW280264X that targets both ADAM10 and ADAM17 blocked IL-6-induced proliferation and ERK1/2 phosphorylation with same potency as GM6001. GW280264X 0-9 ADAM metallopeptidase domain 17 Homo sapiens 39-45 21111811-6 2011 GW280264X that targets both ADAM10 and ADAM17 blocked IL-6-induced proliferation and ERK1/2 phosphorylation with same potency as GM6001. GW280264X 0-9 interleukin 6 Homo sapiens 54-58 21111811-6 2011 GW280264X that targets both ADAM10 and ADAM17 blocked IL-6-induced proliferation and ERK1/2 phosphorylation with same potency as GM6001. GW280264X 0-9 mitogen-activated protein kinase 3 Homo sapiens 85-91 19455579-7 2009 Inhibition of ADAM10 activity by the hydroxamate-based inhibitors GI254023X and GW280264X resulted in a significant decrease in the mean axonal length. GW280264X 80-89 ADAM metallopeptidase domain 10 Rattus norvegicus 14-20 18305178-7 2008 Addition of the MP inhibitors GM6001, TNF-alpha-converting enzyme inhibitor 2, or GW280264X strongly reduced selenium-induced L-selectin shedding, indicating a MP-dependent mechanism. GW280264X 82-91 selectin L Homo sapiens 126-136 16227584-3 2005 Spontaneous and inducible Axl cleavage was inhibited by the broad-spectrum metalloproteinase inhibitor GM6001 and by hydroxamate GW280264X, which is capable of blocking ADAM10 and ADAM17. GW280264X 129-138 AXL receptor tyrosine kinase Mus musculus 26-29 16227584-3 2005 Spontaneous and inducible Axl cleavage was inhibited by the broad-spectrum metalloproteinase inhibitor GM6001 and by hydroxamate GW280264X, which is capable of blocking ADAM10 and ADAM17. GW280264X 129-138 a disintegrin and metallopeptidase domain 10 Mus musculus 169-175 16227584-3 2005 Spontaneous and inducible Axl cleavage was inhibited by the broad-spectrum metalloproteinase inhibitor GM6001 and by hydroxamate GW280264X, which is capable of blocking ADAM10 and ADAM17. GW280264X 129-138 a disintegrin and metallopeptidase domain 17 Mus musculus 180-186 15777180-7 2005 By contrast, the compound did not affect the PMA-induced shedding, which was only blocked by GW280264X, a potent inhibitor of ADAM17. GW280264X 93-102 ADAM metallopeptidase domain 17 Homo sapiens 126-132