行业新闻
关注特色分子砌块、偶联化学、工艺问题和材料选择相关内容
全部新闻
共 58 篇文章
Reported Phosphorylated ADC Linker and DAR Design
Conventional ADC development often starts with antigen binding, linker stability, and cytotoxic payload release. A phosphorylated payload concept changes the payload question. The reported payload is not framed as a classic cytotoxin; it is framed as a polar phosphorylated molecule intended to support an intracellular recognition hypothesis.
Reported MK-0616 Route Analysis Highlights Peptide Biocatalysis
The reported retrosynthetic map treats MK-0616 as a fragment-intensive macrocyclic peptide program, with multiple non-natural amino acid building blocks that must be controlled before final assembly. That architecture shifts the development question from simple peptide coupling to building-block access, stereochemical control, impurity management, and fragment supply reliability.
Reported TFA Cleavage Tactics for Cys S-tert-Butylation in SPPS
In Fmoc/tBu solid-phase peptide synthesis, cysteine can become vulnerable during final acidic cleavage because side-chain protecting groups and resin cleavage chemistry generate reactive tert-butyl species. Reported process-development work describes S-tert-butylated cysteine as an impurity formed when tert-butyl cations re-attack deprotected Cys thiols during the TFA cleavage step.
DHODH Inhibitor as ADC Payload: A Linker Chemistry Case Study
DHODH (dihydroorotate dehydrogenase) catalyzes the fourth step of de novo pyrimidine synthesis. BAY-2402234 is a Bayer-originated DHODH inhibitor reported in the paper with enzyme-level potency in the low-nanomolar range. As an ADC payload, it introduces a mechanism distinct from microtubule inhibitors and DNA-damaging agents: pyrimidine starvation.
Reported Coil-Tag Assembly for Site-Specific ADC Conjugation
The reported Coil-Tag concept pairs an engineered coiled-coil sequence on an antibody with a complementary payload-bearing peptide. For ADC teams, the important idea is architectural: antibody expression, peptide synthesis, aqueous assembly, and purification are described as separable development modules.
OPRD Paper Reports Fmoc Ene and Epoxide Impurity Controls
The reported ene and epoxide modifications are not side-chain-specific handling details; they are described on the fluorene core shared by Fmoc-protected amino acids. That matters because solid-phase peptide synthesis normally treats Fmoc as a temporary protecting group, while the modified cores were reported to behave differently under common deprotection and cleavage conditions.