参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
[EN] MACROCYCLIZATION OF PEPTIDOMIMETICS<br/>[FR] MACROCYCLISATION DE PEPTIDOMIMÉTIQUES
申请人：UNIV WARWICK
公开号：WO2019186174A1
公开（公告）日：2019-10-03
The invention provides an improved method of macrocyclization of peptidomimetics, as measured by isolated yields and product distribution, which comprises substitution of one or more of the backbone amide C=O bonds with a turn-inducing motif. The method is general with enhancements seen across a range of ring sizes (e.g. tri-, tetra-, penta- and hexapeptides). Specifically, the invention provides a peptidomimetic macrocycle comprising a carbonyl bioisosteric turn-inducing element having the structure: (I) wherein X is a heteroatom; and wherein R1 to R6 are each independently selected from alkyl, aryl, heteroaryl and H.
[EN] MODULATORS OF C3A RECEPTORS<br/>[FR] MODULATEURS DES RÉCEPTEURS C3A
申请人：UNIV QUEENSLAND
公开号：WO2013067578A1
公开（公告）日：2013-05-16
Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
D-amino acid dehydrogenase and method of making D-amino acids
申请人：Rozzell J. David
公开号：US20080182972A1
公开（公告）日：2008-07-31
Polypeptides capable of catalyzing the reductive amination of a 2-ketoacid to its corresponding D-amino acid are provided. The polypeptides can be prepared by mutagenesis of, e.g., a diaminopimelate dehydrogenase. Also provided is a method of making a D-amino acid using a catalytically active polypeptide, wherein a 2-ketoacid is allowed to contact the polypeptide in the presence of a nicotinamide cofactor and ammonia or an ammonia source.
Proguanil has been found to have rapid and effective killing activity against a variety of disease-causing micro-organisms. For example, when applied topically, proguanil is particularly effective against
Propionibacterium acnes
, a bacteria that causes acne;
Corynebacterium minutissimum
, a bacteria that causes erythrasma,
Gardnerella vaginalis
, a bacteria that causes vaginosis;
Trichomonas vaginalis
, a protozoan that causes trichomoniasis and
C. albicans
, a fungus (a form of yeast).
Novel therapeutic agents that modulate enzymatic processes
申请人：——
公开号：US20040023290A1
公开（公告）日：2004-02-05
Novel multi-binding compounds are disclosed that modulate enzymatic processes. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to an enzyme, enzyme substrate or enzyme cofactor thereby modulating the biological processes/functions thereof.
