113850-77-4Relevant articles and documents
Identification of inhibitors of UDP-galactopyranose mutaseviacombinatorialin situscreening
Fu, Jian,Fu, Huixiao,Xia, Yufen,N'Go, Inès,Cao, Jun,Pan, Weidong,Vincent, Stéphane P.
, p. 1818 - 1826 (2021)
Anin situscreening assay for UDP-galactopyranose mutase (UGM, an essential enzyme ofM. tuberculosiscell wall biosynthesis) has been developed to discover novel UGM inhibitors. The approach is based on the amide-forming reaction of an amino acid core with various cinnamic acids, followed by a direct fluorescence polarization assay to identify the best UGM binders without isolation and purification of the screened ligands. This assay allows us to perform one-pot high-throughput synthesis and screening of enzyme inhibitors in a 384-well plate format. UGM ligands were successfully identified by this technology and their inhibition levels were established from pure synthetic compoundsin vitroand in a whole cell antibacterial assay. This study provides a blueprint for designing enamide structures as new UGM inhibitors and anti-mycobacterial agents.
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 (1996)
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
X???X Halogen Bond-Induced Supramolecular Helices
Hao, Aiyou,Xing, Pengyao,Xu, Yunying
supporting information, (2021/11/30)
The halogen bond is the attractive interaction between the electrophilic region of a halogen atom and the nucleophilic region of another molecular entity, emerging as a favorable manner to manipulate supramolecular chirality in self-assemblies. Engineerin
Specific Inhibitor of Placental Alkaline Phosphatase Isolated from a DNA-Encoded Chemical Library Targets Tumor of the Female Reproductive Tract
Bassi, Gabriele,Cazzamalli, Samuele,Favalli, Nicholas,Manz, Markus G.,Neri, Dario,Onda, Yuichi,Pellegrino, Christian,Scheuermann, J?rg
supporting information, p. 15799 - 15809 (2021/11/16)
Placental alkaline phosphatase (PLAP) is an abundant surface antigen in the malignancies of the female reproductive tract. Nevertheless, the discovery of PLAP-specific small organic ligands for targeting applications has been hindered by ligand cross-reac
Electron-deficient p-benzoyl-l-phenylalanine derivatives increase covalent chemical capture yields for protein–protein interactions
Joiner, Cassandra M.,Breen, Meghan E.,Mapp, Anna K.
, p. 1163 - 1170 (2019/05/10)
The photoactivatable amino acid p-benzoyl-l-phenylalanine (pBpa) has been used for the covalent capture of protein–protein interactions (PPIs) in vitro and in living cells. However, this technique often suffers from poor photocrosslinking yields due to th
PENTAFLUOROPHOSPHATE DERIVATIVE, ITS USES AND AN APPROPRIATE MANUFACTURING METHOD
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Page/Page column 12, (2019/04/05)
The invention relates to a pentafluorophosphate derivative according to general formula (I): or a pharmaceutically acceptable salt or solvate thereof. Thereby, R1 and R2 denote independently from each other H or F; R3 denotes H, an optionally substituted C1-C10 alkyl, an optionally substituted C3-C10 cycloalkyl, or an optionally substituted C6-C20 aryl, wherein a hydrocarbon chain of the alkyl, the cycloalkyl or the aryl can be interrupted by one or more oxygen, sulfur and/or nitrogen atoms; and M denotes any cation; with the proviso that at least one of R1 and R2 denotes F, if R3 denotes H. The invention further relates to uses of such a pentafluorophosphate derivative and to an appropriate manufacturing method.
A Bifunctional Amino Acid Enables Both Covalent Chemical Capture and Isolation of in Vivo Protein–Protein Interactions
Joiner, Cassandra M.,Breen, Meghan E.,Clayton, James,Mapp, Anna K.
, p. 181 - 184 (2017/02/05)
In vivo covalent chemical capture by using photoactivatable unnatural amino acids (UAAs) is a powerful tool for the identification of transient protein–protein interactions (PPIs) in their native environment. However, the isolation and characterization of
A palladium and gold catalytic system enables direct access to O- and S-linked non-natural glyco-conjugates
Jeon, Min Ho,Mathew, Bijoy P.,Kuram, Malleswara Rao,Myung, Kyungjae,Hong, Sung You
supporting information, p. 11518 - 11524 (2016/12/18)
Here we report a straightforward cross-coupling method for the synthesis of non-natural glycoamino acids from alkyne-bearing monosaccharides and p-iodophenylalanine. Pd/Au-catalyzed Sonogashira coupling is tolerant to both O- and S-glycosides without any epimerization. In addition, no racemization of the amino acid was observed allowing direct access to the homogeneous glyco-conjugate in a single step. Notably, this Pd/Au catalytic system presents enhanced catalytic activity than conventional Pd/Cu and Pd-only platforms, and it further enables the convergent synthesis of glycodipeptides.
PROCESSES AND REAGENTS FOR MAKING DIARYLIODONIUM SALTS
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Paragraph 0433, (2014/05/08)
This disclosure relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated, iodinated, astatinated and radiofluorinated aromatic compounds.
Effect of the 4′-substituted phenylalanine moiety of sansalvamide A peptide on antitumor activity
Liu, Shouxin,Yang, Yihua,Zhao, Cuiran,Huang, Jing,Han, Chunyu,Han, Jianrong
, p. 463 - 467 (2014/04/17)
Eight sansalvamide A peptide analogues with 4′-fluoride, 4′-chloride, 4′-bromide, 4′-iodide, and 4′- methoxyphenylalanine moieties were synthesized. The effect of these para-substitutions of sansalvamide A peptide on their cytotoxicity was evaluated using HCT-116, MDA-MB-231, HT-29, HCT-15, K562, HeLa, and A549 cell lines. The 4′-methoxyphenylalanine analog of sansalvamide A peptide was found to be a promising antitumor agent.