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检索条件"任意字段=第11届世界华人药物化学研讨会（ISCMC2018）"

共 414 条记录，以下是291-300 订阅

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Engineering enzymes as protein drugs by computational simulations and QM/MM calculations on the catalytic reaction mechanisms

Engineering enzymes as protein drugs by computational simula...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiaoqin Huang Wenli Wang Zhonglian Cao Wei Fu Center for Research Computing Center for Theoretical Biological PhysicsRice University Department of Medicinal Chemistry School of PharmacyFudan University

Protein/enzyme drugs have become more visible as an important class of medicines serving patients in need of new therapies. Besides the obvious advantages of protein enzyme drugs over chemical drugs（*** side effects）,more matured protein enzyme engineering technologies also help drug developers finely tune the desirable functional features of the interested protein/enzyme,while maintaining the product safety and/or efficacy. In order to engineer a novel enzyme mutant as potent and specific treatment,scientists have to first understand how the enzyme catalyzes the transformation of the substrate to the product,i.e.,the mechanisms of the catalytic *** then,researchers can perform mechanism-based designs of novel *** simulations can also be performed to improve the desirable functions,*** thermostability of the enzyme mutant These are also the biggest challenges in the current design of enzyme *** this talk,we will discuss some new computational strategies and methods（***-temperature simulations,QM/MM calculations） of how to improve enzyme thermostability and catalytic efficiency,by sharing our successful and ongoing stories of typical enzymes like butyrylcholinesterase,cocaine esterase,and uricase.

关键词： enzyme drug QM/MM methods high-temperature simulations catalytic efficiency

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Bouchardatine analogue alleviates NASH in mice via activating AMPK through blunting ATP synthase activity

Bouchardatine analogue alleviates NASH in mice via activatin...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yong Rao Yuting Lu Chan Li Qinqin Song Yaohao Xu Zhao Xu Yutao Hu Hong Yu Lin Gao Lianquan Gu Jiming Ye Zhishu Huang Institute of Medicinal Chemistry School of Pharmaceutical SciencesSun Yat-sen University Lipid Biology and Metabolic Disease Laboratory School of Health and Biomedical SciencesRMIT University

Non-alcoholic steatohepatitis(NASH) is pathologically characterized by hepatic steatosis(first hit)and its accompanied oxidative stress or ER stress[1].Currently,we examined a newly synthesized compound(R17) for the treatment of NASH and its molecular mode of action[2].Administration of R17(20 mg/kg,i.p.) significantly reversed HF-induced hepatic steatosis,inflammation,liver injury and fibrosis without indication of adverse *** studies revealed that R17 was able to reduce hepatic steatosis from both lipogenesis and fatty acid *** liver protective effects were associated with the inhibition of ER stress and oxidative ***,R17 treatment activated LKB1-AMPK pathway by blunting the activity of ATP *** together,our findings suggest that R17 may be a potential new drug for NASH via a new mechanism of activating the LKB1-AMPK axis.

关键词： NASH lipotoxicity inflammation metabolic stress AMPK

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Discovery of selective P300 inhibitors for cancer therapy

Discovery of selective P300 inhibitors for cancer therapy

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Zigao Yuan Qinsheng Sun Cunlong Zhang Chun Guo Yuyang Jiang Shenzhen Kivita Innovative Drug Discovery Institute Department of Pharmaceutical Engineering Shengyang Pharmaceutical University Graduate School at Shenzhen Tsinghua University

The paralogous P300 and CBP catalyze acetylation of histories as well as other epigenetic proteins and transcription factors,thereby regulating the expression of diverse genes controlling basic cellular processes,including proliferation,differentiation,and homeostasis.P300 and CBP have been pursued as potential therapeutic targets for many disease,especially ***,current inhibitors of P300/CBP histone acetyltransferase（HAT） domains lack potency and selectivity,and none has yet made it into clinical trials. Besides,the HAT domain and its two flanking domains in P300 and CBP show 86%amino acid residue identity,leading to a challenge for developing selective P300 or CBP inhibitors. We have constructed a series of novel HAT inhibitors,some of which potently inhibited P300（IC50 <0.5 μM） and did not affect *** inhibitors could be useful toolkits to decipher specific biological functions of P300,and to validate draggability of P300 as an antitumor *** further biological evaluations of our compounds are ongoing.

关键词： P300 CBP Selectivity Synthetic lethality Bioactivity evaluation

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Synthesis and bioactivity investigation of the individual components of cyclic lipopeptide antibiotics

Synthesis and bioactivity investigation of the individual co...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Along Cui Xinxin Hu Jie Jin Hong Yi Zhaojin Zhong Shuo Zhang Xiukun Wang Xuefu You Zhuorong Li Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences & Peking Union Medical College

In this paper,twenty-six natural individual polymyxin components and a new derivative S2 were synthesized[1],and their differences in efficiency and toxicity have been *** all of the synthesized components showed very strong activity against both susceptible and resistant strains of ***,***,***,and *** toxicities were obviously different between the components.A subset of components were tested for acute and renal toxicities in *** E2,E2-Val,A2,M2,D2,and S2 showed obviously lower renal cytotoxicities and acute toxicities than polymyxins B and *** in vivo nephrotoxicity of E2,M2,and S2 were similar to that of polymyxin ***,compound S2 with four positive charges could simultaneously increase the efficiency and decrease the *** SAR and toxicity studies indicated that further structural modification could concentrate on polymyxin S rather than the previous lead compound polymyxin B with five positive *** results also indicated that S2 could be a new drug candidate.

关键词： individual polymyxin component synthesize bioactivity evaluation SAR and toxicity

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Synthesis and structure-activity relationship study of sulfonamides as novel potent H5N1 inhibitors

Synthesis and structure-activity relationship study of sulfo...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yongshi Yu Shuwen Wu Haibing Zhou School of Pharmaceutical Sciences Wuhan University College of Life Sciences Wuhan University

H5 N1 virus is one subtype of influenza A virus,which belongs to the orthomyxoviridae *** of higher mortality（about 60%） compared with other subtypes,H5 N1 virus is a big threat to human health and *** our previous work,the SAR and molecular modeling studies indicate that the heteroaromatic moiety and sulfur atom play significant roles in the anti-H5 N1 activity,however,the long linker of compound 1 limits it efficiently filling the hydrophobic cavity of M2 proteinHerein,we designed and synthesized benzenesulfonamide derivatives by shortening the linker length,reserving the sulfur atom,replacing carboxamide moiety by sulfonamide moiety and introducing cyano side chain in the meanwhile（Figure 1）.Finally,we found compound 2 h exhibited excellent EC value of 0.006 μM against H5 N1 virus compared with reference drug amantadine（0.435 μM） in MDCK *** mechanism studies are still going on in our laboratory and will be reported in due course.

关键词： Sulfonamides H5N1 virus M2 protein H5N1 Inhibitors

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Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio) propanamide(CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of abl mutants includin

Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(tr...

引用

第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xuesong Liu Jing Liu High Magnetic Field Laboratory Key Laboratory of High Magnetic Field and Ion Beam Physical BiologyHefei Institutes of Physical ScienceChinese Academy of Sciences University of Science and Technology of China

Starting from axitinib a type I inhibitor,which has been reported to overcome ABL-T315 I mutant induced resistance,through a structure guided drug design approach and binding mode switch strategy,we have discovered a potent type Ⅱ ABL inhibitor CHMFL-ABL-121,which significantly improved the inhibitory activity against ABL wt and a broad spectrum of mutants including the most prevalent imatinib-resistant gatekeeper mutant T315 ***-ABL-121 potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type Ⅱ inactive conformation and inhibited the proliferation of the established CML cell lines with GI at single digit *** cellular context,CHMFL-ABL-121 strongly affected BCR-ABL mediated signaling pathways and induced apoptosis by arresting cell cycle into G0/G1 phase.

关键词： axitinib ABL type Ⅱ gatekeeper mutant

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ASC26,a Selective ABCB1 inhibitor reverses ABCB1-mediated drug resistance in cancer cells

ASC26,a Selective ABCB1 inhibitor reverses ABCB1-mediated dr...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Tiantian Qin Dongxiao Yang Xueyan Zhang Leilei Li Weihua Liu Junfeng Huo Xiaoli Shi Cong Wang Hongmin Liu School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation Zhengzhou University

Multidrug resistance is the major cause of chemotherapy failure in *** of ATP-binding cassette subfamily B member 1(ABCB1) plays an important role in multidrug resistance by transporting various anticancer agents out of cancer *** this study,we investigated the effect of a novel steroidal derivative,ASC26 on ABCB1-overexpressing cell *** found that ASC26 could significantly enhance the efficacy of chemotherapeutic drugs in ABCB1 over-expressing cancer cells at non-toxic *** addition,ASC26 remarkably increased the intracellular accumulation of paclitaxel and rhodamine 123 by inhibiting the efflux function of ***,ASC26 did not alter the expression level or the subcellular location of ABCB1 *** conclusion,these findings indicated that ASC26 is a ABCB1 inhibitor,which could significantly reverse ABCB1-mediated MDR by competitively inhibiting the drug efflux function of ABCB1,other than down-regulating the protein expression of ABCB1.

关键词： multidrug resistance ABCB1 ASC26 drug efflux cancer

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Benzoselenazoles:highly selective estrogen receptor-beta agonists

Benzoselenazoles:highly selective estrogen receptor-beta ago...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Silong Zhang Xueke Peng Zhiye Hu Chune Dong Haibing Zhou School of Pharmaceutical Sciences Wuhan University

Estrogen receptor beta（ERβ） is a subtype of ER that plays important roles in the central nervous system（CNS） and the immune ***,an important nutritional trace element,is also known to be important for a wide array of health *** part of our long-term interest in the development of ER ligands with novel structures and activities in 2016,our group reported selenophenes as non-steroidal estrogen receptor ligands,which was the first example introducing selenium into ER ligands. Herein,to expand the application of selenium as a constituent part of ER ligands,we focused on monoaryl-substituted benzenes that were fused to five-membered ring ***,we decided to prepare benzoselenazoles because these followed the aryl diphenolic azole pharmacophore model that frequently led to ligands favored ERβ as well as raloxifene Most of the compounds showed good selectivity for ERβ in terms of binding affinity and had very weak affinity for *** particular,derivatives Sh and 5 j can be considered as the lead compounds（RBA of 5 h for ERβ is 24%,5 j affinity selectivity is over 50-fold）.And most of the active compounds act as ERβ agonists showing promising application in the selective activation of the ERβ.As such,they could be useful pharmacological probes to define the biological importance and physiological roles of ERβ.

关键词： estrogen receptor beta structure-activity relationship benzoselenazoles selectivity

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Design,synthesis and biological evaluation of novel benzothiazine derivatives as PI3Kδ/γ inhibitors

Design,synthesis and biological evaluation of novel benzothi...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jun Wei Dongyan Gu Yongzhou Hu Rong Sheng College of Pharmaceutical Sciences Zhejiang University

PI3 Kδ and PI3 Kγ play essential role in specific immune cell *** PI3 Kδ,PI3 Kγand dual PI3 Kδ/γ inhibitors have the potential for the treatment of hematological malignancies and inflammatory diseases. In our previous work,several benzodithiazine derivatives have been designed and synthesized as potent PI3 Kδ inhibitors,the further biological evaluation are in *** bioisosterism strategy,a new series of benzothiazine derivatives were designed to improve the PK profile with remained PI3 Kδ inhibitory *** in vitro biological assay revealed that almost all the new compounds exhibited moderate to potent PI3 Kδ inhibitory *** them,compound SV-14 exhibit excellent PI3 Kδ inhibitory activity with IC value of 6.2 *** interestedly,compound SV-18 demonstrated PI3 Kδ and PI3 Kγ inhibitory activities with IC values of 1.0 nM and 3.3 nM,*** further in vitro and in vivo PK evaluation on SV-14 and SV-18 showed that these two compounds possess better PK profiles than previous benzodithiazine analogues.

关键词： PI3K Benzothiazine Antitumor

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Discovery of novel phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library

Discovery of novel phenylalanine derivatives as potent HIV-1...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Gaochan Wu Lanlan Jing Dongwei Kang Xinyong Liu Peng Zhan Department of Medicinal Chemistry Key Laboratory of Chemical BiologyMinistry of EducationSchool of Pharmaceutical SciencesShandong University

HTV-l capsid（CA） is considered an important therapeutic target that is currently unexploited clinically .In this article,taking previously reported CA inhibitor PF-74 as lead compound,a total of 48 novel phenylalanine derivatives were rationally designed via scaffold hopping strategy and parallelly synthetized adopting Cu（I）-catalyzed alkyne-azide 1,3-dipolar cycloaddition（CuAAC） reaction .Subsequently,anti-HTV-l activity evaluation in MT-4 cells indicated that synthesized compounds WG16,WG19 and WG12 displayed remarkable activity against HTV-l NL4-3 strain with EC values of 4.33 ± 0.83 μM,6.65 ± 1.47 μM and 6.91 ± 2.43 μM,respectively,which were superior or comparable to PF-74(EC= 5.95 ± 1.32 μM).Furthermore,SPR binding assays,SARs analysis and molecular modeling studies illustrated valuable insights for further design of more potent phenylalanine analogues with potential therapeutic applications for HTV-l infection.

关键词： HIV-1 Capsid Drug design Click chemistry Compound library

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