Table 6.

In vivo histone protein acetylation in CLL patient cells following depsipeptide treatment



Relative increase in H4 acetylation, % before treatment

Relative increase in H3 acetylation, % before treatment

Relative HDAC enzyme activity, % before treatment

Maximum reduction in lymphocyte count, %
Patient no.
4 h after treatment
24 h after treatment
4 h after treatment
24 h after treatment
4 h after treatment
24 h after treatment
1   260   170   240   800   26.0   52.5   45  
2   630   440   460   370   19.4   64.1   76  
3   200   230   240   410   30.6   45.3   61  
4   390   770   510   330   16.2   86.8   59  
5   800   270   440   260   24.2   58.3   50  
6   340   240   260   100   37.5   66.2   50  
7
 
300
 
200
 
630
 
390
 
36.2
 
80.2
 
62
 


Relative increase in H4 acetylation, % before treatment

Relative increase in H3 acetylation, % before treatment

Relative HDAC enzyme activity, % before treatment

Maximum reduction in lymphocyte count, %
Patient no.
4 h after treatment
24 h after treatment
4 h after treatment
24 h after treatment
4 h after treatment
24 h after treatment
1   260   170   240   800   26.0   52.5   45  
2   630   440   460   370   19.4   64.1   76  
3   200   230   240   410   30.6   45.3   61  
4   390   770   510   330   16.2   86.8   59  
5   800   270   440   260   24.2   58.3   50  
6   340   240   260   100   37.5   66.2   50  
7
 
300
 
200
 
630
 
390
 
36.2
 
80.2
 
62
 

Data are shown as percentage relative to the pretreatment sample in each case, set at 100%. Increases of H3 and H4 acetylation of at least 100% more than the pretreatment sample (ie, 200% before treatment or greater) are considered to meet the MEPD criteria.

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