An approach for the generation of secondary structure specific abzymes
摘要:
Secondary structure specific recognition of substrates by enzymes is ubiquitous. In this letter, we describe an approach to incorporate this recognition element into abzymes,
A compound of formula (I), or a pharmaceutically acceptable salt thereof:
The compound is used in pharmaceutical compositions and in a method of treatment of a disease or medical condition which benefits from inhibition of gap junction activity by administering to a subject suffering from such disease or condition.
[EN] PEGYLATED CARFILZOMIB COMPOUNDS<br/>[FR] COMPOSÉS DE CARFILZOMIB PÉGYLÉS
申请人:AMGEN INC
公开号:WO2017205392A1
公开(公告)日:2017-11-30
The present invention provides polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts thereof, of Formula I wherein R1, R2, linker, PEG, n and o are as defined herein. The invention also provides methods of making and using these compounds to treat cancer, and particularly to treat hematological malignancies including multiple myeloma.
We report a selective ruthenium catalyzed reduction of tertiary amides on the side chain of Fmoc-Gln-OtBu derivatives, leading to innovative unnatural α,β or γ-amino acids functionalized with tertiary amines. Rapid and scalable, this process allowed us to build a library of basic unnatural aminoacids at the gram-scale and directly usable for liquid- or solid-phase peptide synthesis. The diversity
我们报道了选择性钌催化的Fmoc-Gln-O t Bu衍生物侧链上的叔酰胺还原,导致创新的用叔胺官能化的非天然α,β或γ-氨基酸。快速且可扩展,该过程使我们能够建立克级的基本非天然氨基酸文库,并可直接用于液相或固相肽合成。可用叔胺的多样性使我们能够调节所得氨基酸的物理化学性质,例如碱性或疏水性。
The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein are capable of inhibiting all three of CT-L, T-L, and PGPH activities of proteasomes, and are useful in treating various conditions or diseases associated with proteasomes.