【摘 要】
：
Human CD38 is a dual-functional protein that acts not only as a receptor but also as a signaling enzyme,catalyzing the formation of Ca2+ messenger molecules,cyclic ADP-ribose(cADPR),ADPR and nicotinic
【机 构】
：
State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking Univer
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Human CD38 is a dual-functional protein that acts not only as a receptor but also as a signaling enzyme,catalyzing the formation of Ca2+ messenger molecules,cyclic ADP-ribose(cADPR),ADPR and nicotinic acid adenine dinucleotide phosphate.Ablation of the CD38 gene in mice causes multiple physiological defects,including impaired oxytocin release,that result in altered social behavior.The role of CD38 in human physiology and pathology makes it a novel potential pharmacological target.H2 is the currently best noncovalent inhibitor of CD38,so we synthesized a series of H2 derivatives to analyze the structure-activity relationships and found two compounds exhibiting considerable inhibition of the NADase activity of CD38.This study provides an available reference for design of novel noncovalent inhibitors of CD38.
其他文献
Robust strategies to rapidly access compound libraries featuring high levels of structural complexity,skeletal diversity and drug-likeness for drug discovery remain in urgent demand.We propose a highl
Introduction of fluorine in organic molecules constitutes a great interest in pharmaceuticals.It can change chemical and physical properties of molecules due to the great stability of C-F bond and lip
Recently,3-iodo-4-phenoxypyridinone derivatives (IOPYs) were identified as a novel class of highly potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with superior activity against both w
Pyrimidines have been recognized as important heterocyclic compounds due to their diverse biological activities such as HIV-1 inhibitor,antimalarial,antibacterial,anticancer,analgesic,cardiovascular,a
There were several strategies enhancing permeation of gancyclovir (GCV) into the retinal and corneal tissues.These approaches could lead to significant improvement in therapeutic options and efficacy,
Large-conductance calcium-activated potassium channels(BK channels),widely expressed in various cells and tissues of mammals except myocardial cells,responding to two distinct physiological stimuli,i.
Taxoids remain a subject of research for the design of novel anticancer drugs and much more complete knowledge of their interaction with microtubules.1-DeoxybaccatinⅥ 1 possessing the typical tetracyc
The zinc-dependent and calcium-containing family of endopeptidascs called matrix metalloproteinases (MMPs) play a crucial role in the degradation of extracellular matrix (ECM) and tissue remodeling.Of
In recent years,butenolides have gained much attention due to their extensive biological activities and flexible synthetic strategies.Numerous studies have been dedicated to molecular design,synthetic
Histamine H3 receptor(H3R) is a presynaptic GPCR receptor regulating the synthesis and release of histamine as well as other important neurotransmitters,such as ACh,5-HT and DA.Development of H3R anta