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43 articles in total
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.
Stepwise Disulfide Bond Construction in Peptides: Orthogonal Protection Meets Regioselective Folding
When a peptide carries two, three, or four disulfide bonds, the question is not whether cysteines can be oxidized — it is whether they pair correctly. Orthogonal protection answers this by assigning each cysteine pair a protecting group removable under conditions that leave the others intact. The most widely used group in Fmoc-SPPS is trityl (Trt), which cleaves with 1–5% TFA and is the default for single-disulfide peptides. But Trt alone cannot support regioselective multi-disulfide assembly.
Reported SPPS Resin Selection Criteria for Peptide Process Work
For a peptide process team, resin selection is a design decision made before the first coupling cycle. The reported selection model starts with the C-terminal functional group needed after cleavage, then checks whether the sequence raises risks such as diketopiperazine formation, racemization, steric hindrance, poor swelling, or a need for protected fragments.
Generative AI Meets Peptide Chemistry: How ApexGO Frames Peptide Lead Optimization
Antimicrobial resistance continues to drive interest in peptide-based antibiotics as an alternative to conventional small molecules. However, optimizing peptide leads for activity, selectivity, and stability can require repeated synthesis, purification, and assay cycles. Each round consumes time and material, limiting how many candidates can be explored experimentally.