Drug Discovery

antibody drug conjugate

ADC Cleavable Linker: Classification and Mechanism of Action

Antibody-drug conjugates (ADCs), as emerging anticancer drugs, can deliver highly cytotoxic molecules directly to cancer cells to kill them. ADC is a monoclonal antibody covalently bound to cytotoxic chemical substances […]

siRNA Design

Optimization of siRNA Design

The length of siRNA is 7-8 nm, the diameter is 2-3 nm, the molecular weight is 13-14 kDa, and it is hydrophilic. Therefore, unmodified and naked siRNA cannot passively cross […]

ADC targets

Nectin-4: A New Target of ADC

Overview of Nectin Nectin, a cell adhesion molecule belonging to the Immunoglobulin (Ig) superfamily, is a homologue of poliovirus receptor (PVR/CD155). It also known as poliovirus receptor-associated protein Receptor Related Protein (PVRL). […]

Peptide-drug Conjugate

Overview of Peptide-drug Conjugate

The concept of drug conjugates originated in the early 20th century. In 1910, Paul Ehrlich proposed the “Magic Bullet” theory, which aimed to describe the concept of a drug that […]

antibody drug conjugate

FDA Approved Antibody-Drug Conjugates (ADCs) By 2023

Antibody Drug Conjugate (ADC) is a complex formed by linking cytotoxic drugs to tumor-targeting monoclonal antibodies. It combines the characteristics of targeted drugs and chemotherapy drugs to achieve precise treatment. The concept […]

Telomere Targeting Chimera

Literature Interpretation (JACS): Telomere Targeting Chimera Enables Targeted Destruction of Telomeric Repeat-Binding Factor Proteins

Today I would like to share with you an article published in JACS titled “Telomere Targeting Chimera Enables Targeted Destruction of Telomeric Repeat-Binding Factor Proteins”. This article developed a nucleotide-based […]

drug discovery

Research Progress of Small Molecule Drugs Targeting PD-1/PD-L1

Immunotherapy, which uses immune pathways to treat cancer, is rapidly becoming an accepted cancer treatment after surgery, chemotherapy and radiation. Checkpoint blocking using monoclonal antibodies against cytotoxic T lymphocyte-associated protein […]

drug discovery

Advances in Research on Small Molecule Janus Kinase (JAK) Inhibitors

Janus kinases (JAKs) belong to the non-receptor tyrosine kinase family, and their JAK-STAT signaling pathway with signal transducers and activators of transcription (STAT) can affect cell proliferation, differentiation, apoptosis, and […]

lab experiment

FDA-approved small molecule kinase inhibitors-Part 3

Fostamatinib is the precursor drug of active metabolite R406. It is a Syk inhibitor with an IC50 value of 41 nM. It strongly inhibits Syk but does not inhibit Lyn. […]

drug research

FDA-approved small molecule kinase inhibitors-Part 2

Dabrafenib (GSK2118436) is a mutant BRAFV600-specific inhibitor, with an IC50 of 0.7 nM in cell-free assays. It shows 7-fold and 9-fold lower potency against B-Raf(wt) and c-Raf, respectively. Synthetic route: […]