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Avadomide
Avadomide (CC-122) is an experimental cereblon E3 ligase modulator, or thalidomide analog (molecular glue A molecular glue is a type of small molecule that modulates protein–protein interactions in cells by enhancing the affinity between proteins. These compounds can induce novel interactions between proteins (type I) or stabilize pre-existing one ...) that was discovered and studied by Celgene to see if it was effective against cancer. The deuterated S-enantiomer, SP-3164 (DRX-164) is in development at Salarius Pharmaceuticals. References {{reflist Cereblon E3 ligase modulators Drugs developed by Bristol Myers Squibb Glutarimides Quinazolinones Anilines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Molecular Glue
A molecular glue is a type of small molecule that modulates protein–protein interactions in cells by enhancing the affinity between proteins. These compounds can induce novel interactions between proteins (type I) or stabilize pre-existing ones (type II), offering an alternative strategy to traditional drug discovery. Molecular glues have shown promise in targeting proteins previously considered "undruggable" by conventional methods. They work through various mechanisms, such as promoting protein degradation or inhibiting protein function, and are being studied for potential use in treating cancer, neurodegenerative disorders, and other diseases. Unlike PROTACs, which are rationally designed heterobifunctional molecules that contain two covalently linked ligands that bind respectively to a target protein and an E3 ligase, molecular glues are small, monofunctional compounds typically discovered serendipitously through screening or chance observations. Mechanism of action ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cereblon E3 Ligase Modulator
Cereblon E3 ligase modulators, also known as immunomodulatory imide drugs (IMiDs), are a class of immunomodulatory drugs (drugs that adjust immune responses) containing an imide group. The IMiD class includes thalidomide and its analogues (lenalidomide, pomalidomide, mezigdomide and iberdomide). These drugs may also be referred to as 'Cereblon modulators'. Cereblon (CRBN) is the protein targeted by this class of drugs. The name "IMiD" alludes to both "IMD" for "immunomodulatory drug" and the forms ''imide'', '' imido-'', '' imid-'', and '' imid''. The development of analogs of thalidomide was precipitated by the discovery of the anti-angiogenic and anti-inflammatory properties of the drug yielding a new way of fighting cancer as well as some inflammatory diseases after it had been banned in 1961. The problems with thalidomide included teratogenic side effects, high incidence of other adverse reactions, poor solubility in water and poor absorption from the intestines. In 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thalidomide
Thalidomide, sold under the brand names Contergan and Thalomid among others, is an oral administered medication used to treat a number of cancers (e.g., multiple myeloma), graft-versus-host disease, and many skin disorders (e.g., complications of leprosy such as skin lesions). Updated as required. Thalidomide has been used to treat conditions associated with HIV: aphthous ulcers, HIV-associated wasting syndrome, diarrhea, and Kaposi's sarcoma, but increases in HIV viral load have been reported. Common side effects include sleepiness, rash, and dizziness. Severe side effects include tumor lysis syndrome, blood clots, and peripheral neuropathy. Thalidomide is a known human teratogen and carries an extremely high risk of severe, life-threatening birth defects if administered or taken during pregnancy. It causes skeletal deformities such as Amelia (birth defect), amelia (absence of legs and/or arms), absence of bones, and phocomelia (malformation of the limbs). A single dose of t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cereblon E3 Ligase Modulators
Cereblon is a protein that in humans is encoded by the ''CRBN'' gene. The gene that encodes the cereblon protein is found on the human chromosome 3, on the short arm at position p26.3 from base pair 3,190,676 to base pair 3,221,394. CRBN orthologs are highly conserved from plants to humans. Function Ubiquitination and role in development Cereblon forms an E3 ubiquitin ligase complex with damaged DNA binding protein 1 (DDB1), cullin-4A (CUL4A), and regulator of cullins 1 (ROC1). This complex ubiquitinates a number of other proteins and marks them for degradation via the proteasome. Through a mechanism which has not been completely elucidated, this ubiquitination results in reduced levels of fibroblast growth factor 8 (FGF8) and fibroblast growth factor 10 (FGF10). FGF8 in turn regulates a number of developmental processes, such as limb and auditory vesicle formation. The net result is that this ubiquitin ligase complex is important for limb outgrowth in embryos. In ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs Developed By Bristol Myers Squibb
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinazolinones
Quinazolinone is a heterocyclic chemical compound, a quinazoline with a carbonyl group in the C4N2 ring. Two isomers are possible: 2-quinazolinone and 4-quinazolinone, with the 4-isomer being the more common. These compounds are of interest in medicinal chemistry. File:2-Quinazolinone.png, 2-Quinazolinone File:4-Quinazolinone.png, 4-Quinazolinone Synthesis Common routes to quinazolines involve condensation of amides to anilines with ortho nitrile, carboxylic acids and amides. Derivatives Quinazolinone drugs that function as hypnotic/sedatives, methaqualone (Quaalude) for example, usually contain a 4-quinazolinone core with a 2-substituted phenyl group at nitrogen atom 3. See also * Idelalisib (Zydelig) * Cloroqualone * SL-164 (Dicloqualone) * Diproqualone * Etaqualone * Mebroqualone * Mecloqualone * Methylmethaqualone * Nitromethaqualone References {{Chemical classes of psychoactive drugs Quinazolinones, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
