ライフサイエンスコーパス: ispinesib

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1 results from the phase II clinical benchmark ispinesib.

2 her as a single agent or in combination with Ispinesib.

3 to define the mechanism of KSP inhibition by ispinesib.

4 This series also binds in the presence of Ispinesib, a known anticancer KSP inhibitor in phase I/I

5 Our data show that ispinesib alters the ability of KSP to bind to microtubu

6 sin Eg5 against the potent second-generation ispinesib analogue SB743921 (1), a phase I/II clinical c

7 -metabolizing enzymes and hERG compared with ispinesib and SB-743921, which is important given the li

8 s comparable to the Phase II drug candidates ispinesib and SB-743921.

9 83 and MLN8237), Wee1 kinase (MK-1775), KSP (ispinesib), and tubulin (taxanes, vinca alkaloids), are

10 us binding implying existence of a novel non-Ispinesib binding pocket within KSP.

11 Mutations that attenuate Ispinesib binding to KSP in vitro have been identified,

12 ormational changes that occur in response to ispinesib binding.

13 graphy to identify a new structure of an Eg5-ispinesib complex and have combined this with transient

14 Our results demonstrate that ispinesib-induced structural changes in L5 from Eg5 lead

15 Ispinesib is the first potent, highly specific small-mol

16 e development and, in the clinical candidate ispinesib, moderate hERG and CYP inhibition.

17 he wild-type KSP motor domain as well as two ispinesib mutants (D130V and A133D) identified to confer

18 consistent with the physiological effect of ispinesib on cells, which is to prevent KSP-driven mitot

19 One triphenylbutanamine analogue and ispinesib possess very good bioavailability (51% and 45%

20 nstrate direct binding of these compounds to Ispinesib-resistant mutants (D130V, A133D, and A133D + D

21 ormation and corresponding models of the two ispinesib-resistant mutants.

22 e could be a productive strategy for eluding Ispinesib-resistant tumors.

23 Ispinesib (SB-715992), a potent and selective inhibitor

24 A comparison of ispinesib to monastrol, another small-molecule inhibitor

25 nd A133D) identified to confer resistance to ispinesib treatment.

26 ATP-uncompetitive inhibitors, monastrol and ispinesib, we report here the results of thermal denatur

27 mber of small molecule inhibitors, including ispinesib, which is being used in clinical trials in pat

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