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- 1opl (8,297 bytes)
2: ...l basis for the auto-inhibition of c-Abl tyrosine kinase==
5: ... Molecule of the Month] feature on ''Src Tyrosine Kinase'' by David S. Goodsell is [https://dx.doi.org/10...
13: ...of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskelet...
26: ... the catalytic activity of Abl, but not that of c-Src.
28: ...al basis for the autoinhibition of c-Abl tyrosine kinase.,Nagar B, Hantschel O, Young MA, Scheffzek K, Vea... - 1xba (8,024 bytes)
2: ==Crystal structure of apo syk tyrosine kinase domain==
10: ...s phosphorylated by SYK include VAV1, PLCG1, PI-3-kinase, LCP2 and BLNK. Initially identified as essential...
23: ...gid structure of the nonspecific, natural product kinase inhibitor staurosporine.
25: ...g is revealed by the structure of spleen tyrosine kinase.,Atwell S, Adams JM, Badger J, Buchanan MD, Feil ...
32: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 1xbb (8,299 bytes)
2: ==Crystal structure of the syk tyrosine kinase domain with Gleevec==
11: ...s phosphorylated by SYK include VAV1, PLCG1, PI-3-kinase, LCP2 and BLNK. Initially identified as essential...
24: ...gid structure of the nonspecific, natural product kinase inhibitor staurosporine.
26: ...g is revealed by the structure of spleen tyrosine kinase.,Atwell S, Adams JM, Badger J, Buchanan MD, Feil ...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 1xbc (8,212 bytes)
2: ==Crystal structure of the syk tyrosine kinase domain with Staurosporin==
11: ...s phosphorylated by SYK include VAV1, PLCG1, PI-3-kinase, LCP2 and BLNK. Initially identified as essential...
24: ...gid structure of the nonspecific, natural product kinase inhibitor staurosporine.
26: ...g is revealed by the structure of spleen tyrosine kinase.,Atwell S, Adams JM, Badger J, Buchanan MD, Feil ...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 2g1t (8,305 bytes)
2: ...rc-like Inactive Conformation in the Abl Tyrosine Kinase Domain==
13: ...of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskelet...
26: ...formations is a characteristic feature of the Abl kinase domain.
28: ...rc-like inactive conformation in the abl tyrosine kinase domain.,Levinson NM, Kuchment O, Shen K, Young MA...
35: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 2g2f (8,336 bytes)
2: ...rc-like Inactive Conformation in the Abl Tyrosine Kinase Domain==
13: ...of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskelet...
26: ...formations is a characteristic feature of the Abl kinase domain.
28: ...rc-like inactive conformation in the abl tyrosine kinase domain.,Levinson NM, Kuchment O, Shen K, Young MA...
35: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 2g2h (8,278 bytes)
2: ...rc-like Inactive Conformation in the Abl Tyrosine Kinase Domain==
13: ...of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskelet...
26: ...formations is a characteristic feature of the Abl kinase domain.
28: ...rc-like inactive conformation in the abl tyrosine kinase domain.,Levinson NM, Kuchment O, Shen K, Young MA...
35: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 2g2i (8,206 bytes)
2: ...rc-like Inactive Conformation in the Abl Tyrosine Kinase Domain==
13: ...of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskelet...
26: ...formations is a characteristic feature of the Abl kinase domain.
28: ...rc-like inactive conformation in the abl tyrosine kinase domain.,Levinson NM, Kuchment O, Shen K, Young MA...
35: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 1iep (7,187 bytes)
2: ==CRYSTAL STRUCTURE OF THE C-ABL KINASE DOMAIN IN COMPLEX WITH STI-571.==
11: ... NEDD9. Phosphorylates multiple receptor tyrosine kinases and more particularly promotes endocytosis of EG...
24: ...or inactive), whereas STI-571 requires a specific inactive conformation of Abl.
26: ...x with the small molecule inhibitors PD173955 and imatinib (STI-571).,Nagar B, Bornmann WG, Pellicena P, Sch...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 1opk (6,666 bytes)
2: ...l basis for the auto-inhibition of c-Abl tyrosine kinase==
11: ... NEDD9. Phosphorylates multiple receptor tyrosine kinases and more particularly promotes endocytosis of EG...
24: ... the catalytic activity of Abl, but not that of c-Src.
26: ...al basis for the autoinhibition of c-Abl tyrosine kinase.,Nagar B, Hantschel O, Young MA, Scheffzek K, Vea...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 2f4j (8,815 bytes)
2: ...b-Resistant Abl Mutant in Complex with the Aurora Kinase Inhibitor VX-680==
13: ...of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskelet...
26: ... The avoidance of the innermost cavity of the Abl kinase domain by VX-680 and the specific recognition of ...
28: ...b-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.,Young MA, Shah NP, Chao LH, See...
35: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 2oiq (6,055 bytes)
2: ...Src kinase domain in complex with the cancer drug imatinib.==
11: ...lustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates...
24: ...nce between different inactive states is a key to imatinib binding.
26: c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermody...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - SandboxPKA (24,333 bytes)
3: ...ctor-independent cell growth. It also affects the Src/Pax/Fak/Rac pathway. This affects the cytoskeleto...
4: ...l molecule inhibitors of BCR-Abl that bind to the kinase domain can be used to treat CML <ref>PMID:1215402...
11: ...have been well studied. Like others, the abelson kinase incorporates a highly conserved bi-lobed structur...
13: ...d by an SH3 domain, an SH2 domain, and a tyrosine kinase domain. The C-terminal half of c-Abl includes bin...
17: ... group in the N-terminal domain of c-Abl tyrosine kinase' scene='SandboxPKA/Abl1/4'> - 3el7 (6,069 bytes)
2: ==Crystal structure of c-Src in complex with pyrazolopyrimidine 3==
11: ...lustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates...
24: ...on the differential selectivity of Imatinib for c-Src and Abl.
26: Small molecule recognition of c-Src via the Imatinib-binding conformation.,Dar AC, Lopez MS, Shokat KM...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 3el8 (6,065 bytes)
2: ==Crystal structure of c-Src in complex with pyrazolopyrimidine 5==
11: ...lustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates...
24: ...on the differential selectivity of Imatinib for c-Src and Abl.
26: Small molecule recognition of c-Src via the Imatinib-binding conformation.,Dar AC, Lopez MS, Shokat KM...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 3g6g (6,561 bytes)
2: ...-Src and Abl by compounds that recognize inactive kinase conformations==
11: ...lustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates...
24: ...mpounds block the growth of Ba/F3 cells harboring imatinib-resistant BCR-ABL mutants, including the Thr315Il...
26: ...-Src and Abl by compounds that recognize inactive kinase conformations.,Seeliger MA, Ranjitkar P, Kasap C,...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - 3g6h (6,458 bytes)
2: ==Src Thr338Ile inhibited in the DFG-Asp-Out conformati...
11: ...lustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates...
24: ...mpounds block the growth of Ba/F3 cells harboring imatinib-resistant BCR-ABL mutants, including the Thr315Il...
26: ...-Src and Abl by compounds that recognize inactive kinase conformations.,Seeliger MA, Ranjitkar P, Kasap C,...
33: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]] - Nilotinib (3,614 bytes)
6: * Drug Class: Receptor Tyrosine Kinase (Especially, PDGFR, KIT & BCR-Abl) Inhibitor
8: * Expected Sales in Combination with [[Imatinib]]: $5 Billion
9: ...tion BCR-Abl inhibitor designed to work against [[Imatinib]] resistant CML. Recent studies have revealed tha...
13: ...69, stabilizing the inhibited conformation of the kinase.<ref>doi:10.1107/S0907444906047287</ref><ref>PMID...
22: {{:Tyrosine Kinase Inhibitor Pharmacokinetics}} - Bcr-Abl and Imatinib (STI571 or Gleevec) (24,297 bytes)
1: ... group in the N-terminal domain of c-Abl tyrosine kinase (PDB code [[1opk]])' scene='SandboxPKA/Abl1/4'>
2: ...ctor-independent cell growth. It also affects the Src/Pax/Fak/Rac pathway. This affects the cytoskeleto...
3: ...l molecule inhibitors of BCR-Abl that bind to the kinase domain can be used to treat CML <ref>PMID:1215402...
5: See also [[Imatinib]] and [[BCR-Abl Inhibitors]]
10: ...have been well studied. Like others, the abelson kinase incorporates a highly conserved bi-lobed structur... - 2xyn (5,531 bytes)
2: ==HUMAN ABL2 IN COMPLEX WITH AURORA KINASE INHIBITOR VX-680==
11: ...des during infection. Pathogens can highjack ABL2 kinase signaling to reorganize the host actin cytoskelet...
14: ... of the DFG motif intermediate between active and inactive conformations, that may also serve as a template ...
16: ...ctures of ABL-Related Gene (ABL2) in Complex with Imatinib, Tozasertib (VX-680), and a Type I Inhibitor of t...
23: *[[Tyrosine kinase 3D structures|Tyrosine kinase 3D structures]]
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