One aspect of the present invention provides the MetAP2 inhibitor of polymeric conjugation. Although without being bound to any particular theory, it is believed that inhibit core that can provide the compound with more preferable than parent small molecule effect and excellent pharmacokinetic profiles via attachment as described herein coupling MetAP2. In one aspect of the invention, the MetAP2 inhibitor of the polymeric conjugation can be treated in the method for disease with what, which comprises to the MetAP2 inhibitor of the polymeric conjugation of subject with this need application therapeutically effective amount.本發明的一個方面提供了聚合物綴合的MetAP2抑制劑。儘管不受任何具體理論約束,據信,經由本文所述的連接物偶聯MetAP2抑制核心會提供具有比親本小分子更好效力和優良藥代動力學分布的化合物。在本發明的一個方面,所述聚合物綴合的MetAP2抑制劑可用於治療疾病的方法中,所述方法包括:給有此需要的受試者施用治療有效量的聚合物綴合的MetAP2抑制劑。