Research Topics

Hideaki Kakeya


Affiliation: Kyoto University
Country: Japan


  1. Ozaki T, Sugiyama R, Shimomura M, Nishimura S, Asamizu S, Katsuyama Y, et al. Identification of the common biosynthetic gene cluster for both antimicrobial streptoaminals and antifungal 5-alkyl-1,2,3,4-tetrahydroquinolines. Org Biomol Chem. 2019;: pubmed publisher
    ..Differences in the oxidation states of the products result in a distinct cyclization mode to yield 5aTHQs and STAMs. ..
  2. Takahashi N, Hayashi K, Nakagawa Y, Furutani Y, Toguchi M, Shiozaki Sato Y, et al. Development of an anti-hepatitis B virus (HBV) agent through the structure-activity relationship of the interferon-like small compound CDM-3008. Bioorg Med Chem. 2019;27:470-478 pubmed publisher
    ..In addition, the half-life period of 11 was dramatically improved in both mouse and human hepatic microsomes (T1/2, >120 min versus 58.2 min in mouse, and >120 min versus 34.1 min in human, for 11 and 1, respectively). ..
  3. Ishikawa F, Tanabe G, Kakeya H. Activity-Based Protein Profiling of Non-ribosomal Peptide Synthetases. Curr Top Microbiol Immunol. 2018;: pubmed publisher
  4. Nishimura S, Tokukura M, Ochi J, Yoshida M, Kakeya H. Balance between exocytosis and endocytosis determines the efficacy of sterol-targeting antibiotics. Chem Biol. 2014;21:1690-9 pubmed publisher
    ..We propose that exocytosis and endocytosis respectively supply and internalize the specific plasma membrane domains recognized by sterol-targeting antibiotics. ..
  5. Lu S, Nishimura S, Hirai G, Ito M, Kawahara T, Izumikawa M, et al. Saccharothriolides A-C, novel phenyl-substituted 10-membered macrolides isolated from a rare actinomycete Saccharothrix sp. Chem Commun (Camb). 2015;51:8074-7 pubmed publisher
    ..Saccharothriolide B (2) exhibited cytotoxicity against human tumor cell lines HeLa and HT1080. ..
  6. Kakeya H. Natural products-prompted chemical biology: phenotypic screening and a new platform for target identification. Nat Prod Rep. 2016;33:648-54 pubmed publisher
    ..In addition, the development of two new platforms, 5-sulfonyl tetrazole-based and thiourea-modified amphiphilic lipid-based probe technologies, to identify the cellular targets of these molecules is also discussed. ..
  7. Ishikawa F, Suzuki T, Dohmae N, Kakeya H. A Multiple-Labeling Strategy for Nonribosomal Peptide Synthetases Using Active-Site-Directed Proteomic Probes for Adenylation Domains. Chembiochem. 2015;16:2590-4 pubmed publisher
    ..This method provides a new option for the direct detection, functional analysis, and high-resolution identification of low-abundance active NRPS enzymes in native proteomic environments. ..
  8. Ishikawa F, Kakeya H. A Competitive Enzyme-Linked Immunosorbent Assay System for Adenylation Domains in Nonribosomal Peptide Synthetases. Chembiochem. 2016;17:474-8 pubmed publisher
    ..These studies indicate that the ELISA technique can accelerate the discovery of small-molecule inhibitors of the A-domains with new scaffolds that perturb the production of NRPS-related virulence factors. ..
  9. Sugiyama R, Nishimura S, Ozaki T, Asamizu S, Onaka H, Kakeya H. Discovery and Total Synthesis of Streptoaminals: Antimicrobial [5,5]-Spirohemiaminals from the Combined-Culture of Streptomyces nigrescens and Tsukamurella pulmonis. Angew Chem Int Ed Engl. 2016;55:10278-82 pubmed publisher
    ..This work shows the application of microbes as reservoirs for a range of chemical scaffolds. ..

More Information


  1. Yasuda Y, Arakawa T, Nawata Y, Shimada S, Oishi S, Fujii N, et al. Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors. Bioorg Med Chem. 2015;23:1776-87 pubmed publisher
    ..These results revealed 1-ethylpyrazole-3-carboxamide as a novel scaffold to develop promising anti-cancer drugs targeting the HIF-1 signaling pathway. ..
  2. Kanoh N, Itoh S, Fujita K, Sakanishi K, Sugiyama R, Terajima Y, et al. Asymmetric Total Synthesis of Heronamides?A-C: Stereochemical Confirmation and Impact of Long-Range Stereochemical Communication on the Biological Activity. Chemistry. 2016;22:8586-95 pubmed publisher