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Sökning: WFRF:(Li Jianghong) > (2018) > Discovery of Highly...

  • Zhao, XinGuangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China.;Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China.;Univ Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA. (författare)

Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses

  • Artikel/kapitelEngelska2018

Förlag, utgivningsår, omfång ...

  • 2018-05-25
  • American Chemical Society (ACS),2018
  • printrdacarrier

Nummerbeteckningar

  • LIBRIS-ID:oai:DiVA.org:kth-232630
  • https://urn.kb.se/resolve?urn=urn:nbn:se:kth:diva-232630URI
  • https://doi.org/10.1021/acs.jmedchem.8b00042DOI

Kompletterande språkuppgifter

  • Språk:engelska
  • Sammanfattning på:engelska

Ingår i deldatabas

Klassifikation

  • Ämneskategori:ref swepub-contenttype
  • Ämneskategori:art swepub-publicationtype

Anmärkningar

  • QC 20180730
  • Influenza pandemic is a constant major threat to public health caused by influenza A viruses (IAVs). IAVs are subcategorized by the surface proteins hemagglutinin (HA) and neuraminidase (NA), in which they are both essential targets for drug discovery. While it is of great concern that NA inhibitor oseltamivir resistant strains are frequently identified from human or avian influenza virus, structural and functional characterization of influenza HA has raised hopes for new antiviral therapies. In this study, we explored a structure-activity relationship (SAR) of pinanamine-based antivirals and discovered a potent inhibitor M090 against amantadine-resistant viruses, including the 2009 H1N1 pandemic strains, and oseltamivir-resistant viruses. Mechanism of action studies, particularly hemolysis inhibition, indicated that M090 targets influenza HA and it occupied a highly conserved pocket of the HA(2) domain and inhibited virus-mediated membrane fusion by "locking" the bending state of HA(2) during the conformational rearrangement process. This work provides new binding sites within the HA protein and indicates that this pocket may be a promising target for broad-spectrum anti-influenza A drug design and development.

Ämnesord och genrebeteckningar

Biuppslag (personer, institutioner, konferenser, titlar ...)

  • Li, RunfengGuangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China. (författare)
  • Zhou, YangAlbaNova Univ Ctr, Royal Inst Technol KTH, Sch Biotechnol, Div Theoret Chem & Biol, SE-10044 Stockholm, Sweden. (författare)
  • Xiao, MengjieGuangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China.;Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China. (författare)
  • Ma, ChunlongUniv Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA.;Univ Arizona, BIO5 Inst, Tucson, AZ 85721 USA. (författare)
  • Yang, ZhongjinGuangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China. (författare)
  • Zeng, ShaogaoChinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China. (författare)
  • Du, QiulingGuangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China. (författare)
  • Yang, ChunguangGuangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China. (författare)
  • Jiang, HaimingGuangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China. (författare)
  • Hu, YanmeiUniv Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA.;Univ Arizona, BIO5 Inst, Tucson, AZ 85721 USA. (författare)
  • Wang, KefengGuangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China. (författare)
  • Mok, Chris Ka PunGuangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China.;Univ Hong Kong, HKU Li Ka Shing Fac Med, Sch Publ Hlth, HKU Pasteur Res Pole, 5 Sassoon Rd, Hong Kong, Peoples R China. (författare)
  • Sun, PingGuangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China. (författare)
  • Dong, JianghongChinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China. (författare)
  • Cui, Wei (författare)
  • Wang, JunUniv Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA.;Univ Arizona, BIO5 Inst, Tucson, AZ 85721 USA. (författare)
  • Tu, YaoquanKTH,Teoretisk kemi och biologi(Swepub:kth)u1kuh2ie (författare)
  • Yang, ZifengGuangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China. (författare)
  • Hu, WenhuiGuangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China.;Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China. (författare)
  • Guangzhou Med Univ, Sch Pharmaceut Sci, Key Lab Mol Target & Clin Pharmacol, State Key Lab Resp Dis, Guangzhou 511436, Guangdong, Peoples R China.;Guangzhou Med Univ, Affiliated Hosp 5, Guangzhou 511436, Guangdong, Peoples R China.;Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Guangzhou 510530, Guangdong, Peoples R China.;Univ Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA.Guangzhou Med Univ, Guangzhou Inst Resp Hlth, Affiliated Hosp 1, Natl Clin Res Ctr Resp Dis,State Key Lab Resp Dis, Guangzhou 510120, Guangdong, Peoples R China. (creator_code:org_t)

Sammanhörande titlar

  • Ingår i:Journal of Medicinal Chemistry: American Chemical Society (ACS)61:12, s. 5187-51980022-26231520-4804

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