Drug Discovery

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: […]

drug development

FDA-approved small molecule kinase inhibitors-Part 1

Kinase inhibitors can be divided into monoclonal antibodies (mAbs) and small molecule kinase inhibitors (SMKIs) based on their structure and size. Monoclonal antibodies have achieved great success in the development […]

PROTAC drug discovery

Metabolic Characteristics of PROTAC Drugs

1. Structural Characteristics of PROTAC PROTAC consists mainly of three key structures: on one side is the ligand structure targeting the Protein of Interest (POI); on the other side is […]

drugs

Marketed Nucleic Acid Drugs and Their Lipid Nano-Delivery Systems

Existing research shows that nucleic acids can be used for the treatment of neurological diseases, cardiovascular diseases, and cancer, as well as for the prevention of chronic and infectious diseases. […]

lab research

Emerging ADC Targets: B7-H3 and B7-H4

B7-H3 and B7-H4 are type I transmembrane proteins belonging to the B7 family. Their abnormal expression is associated with many diseases such as colon cancer, breast cancer, liver cancer, and […]

drugs

List of ADCs Targeting HER

Introduction to HER and ADCs Members of the human epidermal growth factor receptor (HER) family, including HER1 (EGFR), HER2, HER3, and HER4, play a core role in regulating cell proliferation, […]

drug discovery

The Forefront of Drug Discovery: Targeting RNA with Small Molecules

Pfizer’s mRNA vaccine for COVID has reignited the passion for using ribonucleic acid (RNA) as a therapeutic target. However, targeting RNA with small molecules is extremely challenging. RNA only has […]

Challenges of Oligonucleotide Drug Development

Challenges of Oligonucleotide Drug Development

The core technologies of oligonucleotide drug development include sequence design, synthesis and modification, isolation and purification, and delivery techniques. The production of oligonucleotide raw materials adopts solid-phase synthesis technology, with […]