1 similar to that of the AGC kinase inhibitor
balanol.
2 ence and absence of the AGC kinase inhibitor
balanol.
3 Balanol,
a fungal metabolite consisting of four rings, p
4 The selectivity of
balanol among human GRKs is assessed.
5 A number of
balanol analogs in which the perhydroazepine moiety is r
6 A series of
balanol analogs in which the perhydroazepine ring and th
7 In general, these acyclic
balanol analogs were found to be highly selective for PK
8 The
balanol analogues serve to test the model and to highlig
9 Here, we characterize three
balanol analogues that inhibit cyclic 3',5'-adenosine mo
10 The PKA C subunit appears to tolerate
balanol analogues with D-ring modifications; PKC does no
11 We have characterized the effects of
balanol and 10"-deoxybalanol in intact cells to determin
12 Western analysis shows that both
balanol and 10"-deoxybalanol reduce phosphorylation of c
13 extensive complementary interactions between
balanol and conserved cAPK residues.
14 Both
balanol and the Takeda compounds induce a slight closure
15 e of the catalytic subunit of PKA (cPKA) and
balanol as a guide, we have analyzed and compared the di
16 indicates considerable diversity of the ATP/
balanol-
binding sites of protein kinases within familial
17 Balanol,
but not 10"-deoxybalanol, inhibits phosphorylat
18 ilar to that of the cPKA-balanol complex and
balanol can be a useful lead compound for developing eff
19 d interfaces are similar to that of the cPKA-
balanol complex and balanol can be a useful lead compoun
20 In addition,
balanol congeners inhibit PKA and PKC with the specifici
21 m is used to calculate binding affinities of
balanol derivatives, H-series inhibitors, and ATP analog
22 BIRB796, Tarceva, NU6102, Gleevec, SB203580,
balanol,
H89, PP1).
23 on linker in which the carboxamide moiety of
balanol had been replaced by a methylene group.
24 ses, a 2.1 A resolution crystal structure of
balanol in complex with cAMP-dependent protein kinase (c
25 ponse element-luciferase reporter construct,
balanol inhibits the induction of luciferase activity by
26 Balanol is a natural product inhibitor exhibiting low na
27 Balanol is a potent inhibitor of cyclic AMP-dependent pr
28 Our data demonstrate that
balanol is a potent inhibitor of PKA and PKC in several
29 The fungal metabolite
balanol is a potent inhibitor of protein kinase A (PKA)
30 Balanol is a potent protein kinase C (PKC) inhibitor tha
31 We propose that
balanol is a protean structure that may be modified to p
32 s with a reduced polar character compared to
balanol itself.
33 Balanol'
s pattern of interactions indicates considerable
34 To elucidate
balanol'
s specific inhibitory effects and provide a basi
35 ding (K(i) approximately 4 nM); congeners of
balanol show specificity for PKA over PKC.
36 analysis approach was applied to the ligand
balanol to develop a pharmacophoric model for searching
37 We tested the capacity of
balanol to inhibit representative serine- and threonine-
38 in kinase C (PKC) inhibitory natural product
balanol which bear modified benzophenone subunits are de