Inhibitor

Future Trends in the Development of GLP-1 Receptor Agonists

Future Trends in the Development of GLP-1 Receptor Agonists

Glucagon-like peptide-1 (GLP-1) is an incretin hormone secreted by intestinal L cells in response to dietary intake. Within minutes after a meal, GLP-1 is released from the L cells in the […]

Definition and Difference of Inhibitor, Activator, Agonist, Antagonist, Reverse Agonist, Blocker

Inhibitor, Activator, Agonist, Antagonist, Reverse Agonist, Blocker: Definition and Difference

For a drug to exert its effect, it must bind to the corresponding target. Drug targets mainly include enzymes, receptors, ion channels, hormones, and cytokines. Small molecules that bind to […]

reversible-inhibitor

What is reversible inhibitor?

Covalent inhibitors generally refer to irreversible covalent inhibitors; however, in detailed studies, they can be divided into irreversible covalent inhibitors (ICIs) and reversible covalent inhibitors (RCIs). Advantages of covalent inhibitors […]

CD137/4-1BB combination therapy

Two Paths of Second-Generation 4-1BB Agonists

CD137/4-1BB combination therapy

Review of Popular Targets

Review of Popular Targets

In recent years, antibody therapies (including traditional antibodies and nano-antibodies) have become an important means of treating a wide range of human malignant diseases, and more than 100 antibody therapies […]

Design Ideas for FDA-Approved Small Molecule Drugs in the third quarter of 2023

Design Ideas for FDA-Approved Small Molecule Drugs in the third quarter of 2023

FDA approved the marketing of 14 drugs in the third quarter of 2023, including 6 small molecule drugs. This article mainly focuses on the drug design ideas of small molecule drugs, hoping […]

Covalent Inhibitors

Covalent Inhibitors Targeting Undruggable Protein

With the rise of genomics and proteomics, many clinically significant targets have been discovered in human diseases. However, a relatively small proportion of traditional druggable targets exists, and many targets […]

drug

A Brief Discussion on ALK Inhibitors

In 2007, Japanese professors firstly discovered ALK rearrangement and identified the fusion of ALK and EML4 in non-small cell lung cancer specimens. EML4 can promote the activation of ALK kinase […]

Cancer

Summary of Kinase Inhibitors | CDK2 and Its Inhibitors

CDKs belong to the serine/threonine protein kinase family, and their kinase activity requires binding to cyclins. Abnormalities in CDKs have been reported to cause proliferation, genomic and chromosomal instability that […]

The Development of Small-molecule Inhibitors Targeting CD47

The Development of Small-molecule Inhibitors Targeting CD47

Abstract Immunotherapy has become an indispensable part of cancer treatment. A pivotal phagocytosis checkpoint, named cluster of differentiation 47 (CD47), which functions as a ‘don’t eat me’ signal to protect […]