76318-50-8Relevant academic research and scientific papers
COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF
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Page/Page column 173, (2019/01/21)
Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.
A novel class of tyrosine derivatives as dual 5-LOX and COX-2/mPGES1 inhibitors with PGE2 mediated anticancer properties
Puratchikody, Ayarivan,Umamaheswari, Appavoo,Irfan, Navabshan,Sinha, Shweta,Manju,Ramanan, Meera,Ramamoorthy, Gayathri,Doble, Mukesh
supporting information, p. 834 - 846 (2019/01/09)
Leukotriene and prostaglandin pathways are controlled by the enzymes, LOX and COX/mPGES1 respectively and are responsible for inflammatory responses. PGE2, produced by mPGES1, leads to the progression of inflammation as well as cancer. A series of 19 novel tyrosine derivatives are synthesized, characterized and tested against 5-LOX, in vitro, and production of PGE2, in HeLa cells. 6b-v and 6c-i, are found to possess maximum inhibitory action against 5-LOX and PGE2 production. The compound 6b-v is found to act by disrupting the redox cycle of the 5-LOX enzyme, and its activity is comparable to that of the commercial drug, Zileuton. The activity of the other compound 6c-i is comparable to a drug in clinical trials, Licofelone, and it has been found to inhibit the mRNA expression of mPGES1 predominantly. It also arrests the HeLa cells in the S and G2/M phases of the cell cycle indicating anticancer activity. Also, compounds, 6b-iv and 6b-viii inhibit both the LT & PG pathways in the inflammation cascade. Presence of iodine in the phenyl ring appears to favour the inhibition of 5-LOX whereas chlorine favours the inhibition of PGE2 production. These leads could be further optimized and developed as drugs against inflammation and cancer.
Tyrosine-derived stimuli responsive, fluorescent amino acids
Cheruku, Pradeep,Huang, Jen-Huang,Yen, Hung-Ju,Iyer, Rashi S.,Rector, Kirk D.,Martinez, Jennifer S.,Wang, Hsing-Lin
, p. 1150 - 1158 (2015/03/04)
A series of fluorescent unnatural amino acids (UAAs) bearing stilbene and meta-phenylenevinylene (m-PPV) backbone have been synthesized and their optical properties were studied. These novel UAAs were derived from protected diiodo-l-tyrosine using palladi
Iodination of aromatic residues in peptides by reaction with IPy2BF4
Barluenga, Jose,Garcia-Martin, Miguel A.,Gonzalez, Jose M.,Clapes, Pere,Valencia, Gregorio
, p. 1505 - 1506 (2007/10/03)
A simple and straightforward approach to selectively iodinate Tyr residues on peptides using IPy2BF4 is described which is compatible with Met residues on the side chain; preliminary studies reveal that the method is also suitable to
