公开(公告)号：US20210317090A1

公开(公告)日：2021-10-14

申请号：US17272436

申请日：2019-08-30

申请人： University of Central Florida Research Foundation, Inc. ,  Terrey Pines Institute for Molecular Studies

发明人： Otto PHANSTIEL, IV ,  Chelsea MASSARO ,  Jenna THOMAS ,  Adel NEFZI

IPC分类号： C07D241/04 ,  A61K45/06 ,  A61K31/337

摘要： Novel compounds are described which decrease the intracellular levels of leucine and methionine. Treatment with these amino acid depletion agents affects many metabolic and life processes which rely upon methionine, leucine and their derivatives. Methionine depletion not only inhibits protein synthesis, but also polyamine biosynthesis and significantly reduces intracellular pools of the native polyamines, spermidine and spermine. Since methionine restriction has been shown to mimic caloric restriction in life extension studies across multiple species, these compounds are also expected to extend lifespan by limiting methionine supply.

公开(公告)号：US20230364057A1

公开(公告)日：2023-11-16

申请号：US18139681

申请日：2023-04-26

申请人： THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES ,  UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.

发明人： Fenfei LENG ,  Eddy ALFONSO ,  Zifang DENG ,  Adel NEFZI ,  Kyle ROHDE

IPC分类号： A61K31/404 ,  A61K31/196 ,  A61K31/5377 ,  A61K31/427 ,  A61K31/519 ,  A61K31/428 ,  A61K31/429 ,  A61K31/41 ,  A61K31/433 ,  A61K31/513 ,  A61K31/366 ,  A61K31/443 ,  A61K31/635 ,  A61K31/496 ,  A61K31/24 ,  A61K31/164 ,  A61K31/426 ,  A61K31/48 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/381 ,  A61K31/498 ,  A61K31/195 ,  A61K31/352 ,  A61K31/7076 ,  A61K31/4178 ,  A61K31/192 ,  A61K31/473 ,  A61K31/517 ,  A61K31/4745 ,  A61K31/502 ,  A61K31/345 ,  A61K31/422 ,  A61K31/4436 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/197 ,  A61K31/137 ,  A61K31/45 ,  A61K31/15 ,  A61K31/4402 ,  A61K31/136 ,  A61K31/4245 ,  A61K31/351 ,  A61K31/437 ,  A61K31/47 ,  A61K31/122 ,  A61K31/365 ,  A61K31/438 ,  A61K31/436 ,  A61K31/515 ,  A61K31/53 ,  A61K31/357 ,  A61K31/4162 ,  A61K31/538 ,  A61P31/04

CPC分类号： A61K31/404 ,  A61K31/122 ,  A61K31/136 ,  A61K31/137 ,  A61K31/15 ,  A61K31/164 ,  A61K31/192 ,  A61K31/195 ,  A61K31/196 ,  A61K31/197 ,  A61K31/24 ,  A61K31/345 ,  A61K31/351 ,  A61K31/352 ,  A61K31/357 ,  A61K31/365 ,  A61K31/366 ,  A61K31/381 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  A61K31/433 ,  A61K31/436 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4402 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/45 ,  A61K31/47 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/48 ,  A61K31/496 ,  A61K31/498 ,  A61K31/502 ,  A61K31/513 ,  A61K31/515 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/635 ,  A61K31/7076 ,  A61P31/04

摘要： The subject invention provides fluorophore-quencher nucleic acid molecules comprising relaxed or supercoiled DNA molecules, and their use in rapid and efficient high-throughput screening (HTS) assays to screen and identify compounds that inhibit DNA gyrases. These compounds can be used as antibiotics for treating bacterial infections, especially, multidrug resistant bacterial infections.