PCAF

Cytokines such as TNFa and IL-1 3, acting via NF-kB, can induce histone acetylation in both a time- and concentration-dependent manner. Upon DNA binding, NF-kB recruits transcriptional coactivators such as CREB binding protein (CBP) and p300/CBP-associated factor (PCAF). 

Cohen HY, Lavu S, Bitterman KJ, Hekking B, Imahiyerobo TA, Miller C, Frye R, Ploegh H, Kessler BM, Sinclair DA (2004) Acetylation of the C terminus of Ku70 by CBP and PCAF controls Bax-mediated apoptosis. Mol Cell 13(5) 627-638... 

Several small molecule modulators (SMM) of p300 and PCAF have been developed (Varier et al, 2004). Recently, the first naturally occurring HAT inhibitor anacardic acid was isolated from cashew nut shell liquid, which inhibits the HAT activity of both p300 and PCAF very effectively (Balasubramanyam et al, 2003). By using anacardic acid as a synthon, an amide derivative of anacardic acid, CTPB, has been synthesized, which is the only known small molecule activator of any histone acetyltransferase, in this case, p300. However, cells are impermeable or... 

Lachner M, O Carroll D, Rea S, Mechtler K Jenuwein T (2001) Methylation of histone H3 lysine 9 creates a binding site for HPl proteins. Nature 410 116-120 Lau OD, Kundu TK, Soccio RE, Ait-Si-Ali S, KhaUl EM, Vassilev A, Wolffe AP, Nakatani Y, Roeder RG, Cole PA (2000) HATs off selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell 5 589-595... 

Dorr A, Kiermer V, Pedal A, Rackwitz HR, HenUein P, Schubert U, Zhou MM, Verdin E, Ott M (2002) Transcriptional synergy between Tat and PCAF is dependent on the binding of acetylated Tat to the PCAF bromodomain. EMBO J 21 2715-2723... 

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