• Title/Summary/Keyword: R-LIM

Search Result 3,379, Processing Time 0.031 seconds

3D QSAR Study on Pyrrolopyrimidines-Based Derivatives as LIM2 Kinase Inhibitors

  • Balasubramanian, Pavithra K.;Balupuri, Anand;Cho, Seung Joo
    • Journal of Integrative Natural Science
    • /
    • v.8 no.4
    • /
    • pp.285-292
    • /
    • 2015

  • LIM kinases belong to the serine/Threonine kinase family. The members of the LIM kinase (LIMK) family include LIMK 1 and 2 which are involved in the regulation of actin polymerisation and microtubule disassembly. LIMK1 was shown to be involved in cancer metastasis, while LIMK2 activation promotes cells cycle progression. Since LIMK2 plays a vital role in many disease conditions such as pulmonary hypertension, cancer and viral diseases, and till date there are not much selective inhibitors been reported, LIMK2 becomes an interesting therapeutic target among the kinases. 3D QSAR study was carried out on a series of pyrrolopyrimidines based derivatives as LIMK2 inhibitors. A reasonable CoMFA ($q^2$=0.888; ONC=3; $r^2$=0.974) with good statistical values was developed. The developed model was validated using 1000 runs of boostrapping and was found to be predictable. The results of CoMFA contour map analysis suggested that the bulky substitution at $R_4$ and $R_5$ position are highly desirable to increase the activity. Similarly, positive substitution at $R_3$ position is also required to increase the activity. It is also noted that bulky substitution at $R_1$ position must be avoided. Our results could provide valuable information to enhance the activity of the LIMK2 inhibitors and to design potent pyrrolopyrimidines derivatives.

  • https://doi.org/10.13160/ricns.2015.8.4.285 인용 PDF KSCI

FINITELY GENERATED G-PROJECTIVE MODULES OVER PVMDS

  • Hu, Kui;Lim, Jung Wook;Xing, Shiqi
    • Bulletin of the Korean Mathematical Society
    • /
    • v.57 no.3
    • /
    • pp.803-813
    • /
    • 2020

  • Let M be a finitely generated G-projective R-module over a PVMD R. We prove that M is projective if and only if the canonical map θ : M⨂R M∗ → HomR(HomR(M, M), R) is a surjective homomorphism. Particularly, if G-gldim(R) ⩽ ∞ and ExtiR(M, M) = 0 (i ⩾ 1), then M is projective.

  • https://doi.org/10.4134/BKMS.b190531 인용 PDF KSCI

Drug Resistance in Fish-Pathogenic Bacteria

  • Aoki, Takashi
    • Journal of fish pathology
    • /
    • v.6 no.1
    • /
    • pp.57-64
    • /
    • 1993

  • The properties and DNA structures of R plasmids differ depending on the species of the fish-pathogens Aeromonas hydrophila, A. salmonicida, Edwardsiella tarda, Enterococcus seriolicida, Pasteurella piscicida and Vibrio anguillarum. However, some R plasmids with the same resistance markers in similar DNA structures were found in A. hydrophila and E. tarda, as well as in A. hydrophila and A. salmonicida. R plasmids from V. anguillarum were classified into three groups according to their DNA structures. The first group was detected before 1977, the second from 1980 to 1983, and the third from 1989 to 1991. R plasmids have been retained within P. piscieida having the same DNA structures and detected at various locations and times. E. seriolicida strains carrying the same R plasmids, which were encoded with resistance to macrolide antibiotics(MLs), lincomycin(LIM), and TC, and to MLs, LIM, and CP. were distributed in yellowtail farms in various districts. The chloramphenicol-resistance(cat) gene of the R plasmids of P. piscicida was classified as CAT type I. The cat of the R plasmids of E, tarda. A. salmonicida was classified as type II. The cat of R plasmids of V. anguillarum was classified into two types. One type detected before 1977, was classified as CAT IV and the other type, detected after 1980, was classified as CAT II. Tetracycline-resistance (tet) V. anguillarum, isolated before 1977 and after 1981, was classified as Tet B and Tet G, respectively. The class D tet gene was widely distributed in R plasmids from fish-pathogens A. hydrophila, E. tarda, P. piscicida, and also V. anguillarum isolated after 1989.

  • PDF