SAP 61 Inhibitors

Chemical inhibitors of SAP 61 can be categorized based on their mechanism of action in targeting the spliceosome, the complex responsible for the removal of introns from pre-mRNA. Pladienolide B and its derivative E7107 are potent inhibitors that bind to the spliceosome, resulting in the disruption of splicing. Given that SAP 61 is an integral component of the spliceosome, the inhibition of the spliceosome assembly and function by these compounds directly impedes the role of SAP 61 in mRNA splicing. Similarly, Isoginkgetin, Madrasin, and Herboxidiene target the spliceosome, thereby inhibiting its assembly and function. These compounds exert their inhibitory effects by preventing the proper formation and activity of the spliceosome, leading to the inhibition of the function of SAP 61 which is critical in the splicing process. Spliceostatin A, like the aforementioned chemicals, also exerts its inhibitory effects on the spliceosome, which in turn results in the inhibition of SAP 61 activity as it is unable to fulfill its role in the absence of a functional spliceosome.

Further, Meayamycin, FR901464, and Pladienolide D bind to the spliceosome, inhibiting its function and thus the splicing process where SAP 61 is involved. The inhibition of SAP 61 by these chemicals is due to their ability to disrupt the normal splicing cycle which is essential for the processing of pre-mRNA into mature mRNA. Tetrocarcin A and Thailanstatin A also have an inhibitory effect on the spliceosome, and therefore on the function of SAP 61. By preventing the spliceosome from carrying out its role in mRNA splicing, these inhibitors directly contribute to the inhibition of SAP 61, which is vital for the splicing mechanism.