874162-99-9Relevant academic research and scientific papers
Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library
Bingham, Patrick,Burke, Benjamin J.,Chen, Qiuxia,Cheng, Xuemin,Deng, Ya-Li,Dou, Dengfeng,Feng, Junli,Gallego, Gary M.,Gehring, Michael R.,Grant, Stephan K.,Greasley, Samantha,Harris, Anthony R.,Kung, Pei-Pei,Maegley, Karen A.,Meier, Jordan,Meng, Xiaoyun,Montano, Jose L.,Morgan, Barry A.,Naughton, Brigitte S.,Palde, Prakash B.,Paul, Thomas A.,Richardson, Paul,Sakata, Sylvie,Shaginian, Alex,Sonnenburg, William K.,Stewart, Albert E.,Subramanyam, Chakrapani,Timofeevski, Sergei,Wan, Jinqiao,Yan, Wen
supporting information, p. 1175 - 1184 (2020/07/04)
Two novel compounds were identified as Naa50 binders/inhibitors using DNA-encoded technology screening. Biophysical and biochemical data as well as cocrystal structures were obtained for both compounds (3a and 4a) to understand their mechanism of action. These data were also used to rationalize the binding affinity differences observed between the two compounds and a MLGP peptide-containing substrate. Cellular target engagement experiments further confirm the Naa50 binding of 4a and demonstrate its selectivity toward related enzymes (Naa10 and Naa60). Additional analogs of inhibitor 4a were also evaluated to study the binding mode observed in the cocrystal structures.
Novel chemotactic For-Met-Leu-Phe-OMe (fMLF-OMe) analogues based on Met residue replacement by 4-amino-proline scaffold: Synthesis and bioactivity
Torino, Domenica,Mollica, Adriano,Pinnen, Francesco,Feliciani, Federica,Spisani, Susanna,Lucente, Gino
experimental part, p. 251 - 259 (2011/03/19)
cis-(2S,4S) 4-Amino-proline (cAmp) and trans-(2S,4R) 4-amino-proline (tAmp) residues, bearing N-For or N-Boc substituents at the two amino groups, have been incorporated into the potent chemotactic agent fMLF-OMe in place of the N-terminal native (S)-methionine to give the analogues 17a-19a and 17b-19b. The new ligands have been examined for their activity (chemotaxis, superoxide anion production and lysozyme release) on human neutrophils as agonists and antagonists. Compounds 19a and 19b, bearing two N-For groups at the proline scaffold, are active and selective chemoattractants. The ligand 18b, containing N-For at the 4-amino group of the N-Boc-tAmp residue, exhibits significant chemotactic antagonism. The influence of the different substitution at the N-terminal position of the new analogues is discussed.
Design and synthesis of photoaffinity-labeling ligands of the L-prolyl-L-leucylglycinamide binding site involved in the allosteric modulation of the dopamine receptor
Fisher, Abigail,Mann, Amandeep,Verma, Vaneeta,Thomas, Nancy,Mishra, Ram K.,Johnson, Rodney L.
, p. 307 - 317 (2007/10/03)
Pro-Leu-Gly-NH2 (PLG), in addition to its endocrine effects, possesses the ability to modulate dopamine 02 receptors within the central nervous system. However, the precise binding site of PLG is unknown. Potential photoaffinity-labeling ligand
