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Sridevi Muppala,Pavan Kumar Gudlavalleti,Sreenu Pagidoju,Kodandarami Reddy Malireddy,Sateesh Kumar Puligandla,Premalatha Dasari (사)한국식물생명공학회 2020 JOURNAL OF PLANT BIOTECHNOLOGY Vol.47 No.1
In maize, immature embryos (IEs) are highly regenerative explants most suitable for producing high frequencies of plantlet regeneration in vitro. Apart from media, explants, and hormones, genotypic variation also influences in vitro characters to a great extent. In the present study, IEs were used to study the distinctive effect of variation of size/stage and hormones in different genotypes on five in vitro characters viz., frequency of callus induction, growth rate of total callus, frequency of E. callus induction, and volume and number of regenerated plantlets. LS medium with different concentrations of 2,4-D (0.5, 1.5, 2.5, 4.0 and 5.0 mg/L) were used to study the former four in vitro characters, and medium with 6-benzylaminopurine and kinetin (0.5 mg/L, each) was used for plantlet regeneration. IEs of 1.0, 1.5, 2.0, 2.5 and 3.0 mm in size were isolated from four inbred lines viz., NM74C, NM81A, NM5883 and NM5884. Two-way ANOVA revealed that explant size and genotypes, as well as hormonal concentrations showed significant effects on in vitro characters. Two millimeter IEs were found to be suitable for in vitro cultures. LS medium with 1.5 mg/L 2,4-D and LS with BAP and Kn (0.5 mg/L, each) were found to be the best hormonal concentrations for callus induction, maintenance, and regeneration, respectively. Among the four genotypes, NM81A and NM5883 yielded more non-embryogenic and Type I E. calli. In contrast, NM74C and NM5884 yielded more highly regenerative Type II calli. Inbred line NM5884 was found to be the best among these four genotypes.
Muppala, Sridevi,Gudlavalleti, Pavan Kumar,Pagidoju, Sreenu,Malireddy, Kodandarami Reddy,Puligandla, Sateesh Kumar,Dasari, Premalatha The Korean Society of Plant Biotechnology 2020 식물생명공학회지 Vol.47 No.1
In maize, immature embryos (IEs) are highly regenerative explants most suitable for producing high frequencies of plantlet regeneration in vitro. Apart from media, explants, and hormones, genotypic variation also influences in vitro characters to a great extent. In the present study, IEs were used to study the distinctive effect of variation of size/stage and hormones in different genotypes on five in vitro characters viz., frequency of callus induction, growth rate of total callus, frequency of E. callus induction, and volume and number of regenerated plantlets. LS medium with different concentrations of 2,4-D (0.5, 1.5, 2.5, 4.0 and 5.0 mg/L) were used to study the former four in vitro characters, and medium with 6-benzylaminopurine and kinetin (0.5 mg/L, each) was used for plantlet regeneration. IEs of 1.0, 1.5, 2.0, 2.5 and 3.0 mm in size were isolated from four inbred lines viz., NM74C, NM81A, NM5883 and NM5884. Two-way ANOVA revealed that explant size and genotypes, as well as hormonal concentrations showed significant effects on in vitro characters. Two millimeter IEs were found to be suitable for in vitro cultures. LS medium with 1.5 mg/L 2,4-D and LS with BAP and Kn (0.5 mg/L, each) were found to be the best hormonal concentrations for callus induction, maintenance, and regeneration, respectively. Among the four genotypes, NM81A and NM5883 yielded more non-embryogenic and Type I E. calli. In contrast, NM74C and NM5884 yielded more highly regenerative Type II calli. Inbred line NM5884 was found to be the best among these four genotypes.
Jin, Cheng Hua,Krishnaiah, Maddeboina,Sreenu, Domalapally,Subrahmanyam, Vura B.,Rao, Kota S.,Lee, Hwa Jeong,Park, So-Jung,Park, Hyun-Ju,Lee, Kiho,Sheen, Yhun Yhong,Kim, Dae-Kee American Chemical Society 2014 Journal of medicinal chemistry Vol.57 No.10
<P>A series of 2-substituted-4-([1,2,4]triazolo[1,5-<I>a</I>]pyridin-6-yl)-5-(6-methylpyridin-2-yl)imidazoles was synthesized and evaluated to optimize a prototype inhibitor of TGF-β type I receptor kinase (ALK5), <B>6</B>. Combination of replacement of a quinoxalin-6-yl moiety of <B>6</B> with a [1,2,4]triazolo[1,5-<I>a</I>]pyridin-6-yl moiety, insertion of a methyleneamino linker, and a <I>o</I>-F substituent in the phenyl ring markedly increased ALK5 inhibitory activity, kinase selectivity, and oral bioavailability. The <B>12b</B> (EW-7197) inhibited ALK5 with IC<SUB>50</SUB> value of 0.013 μM in a kinase assay and with IC<SUB>50</SUB> values of 0.0165 and 0.0121 μM in HaCaT (3TP-luc) stable cells and 4T1 (3TP-luc) stable cells, respectively, in a luciferase assay. Selectivity profiling of <B>12b</B> using a panel of 320 protein kinases revealed that it is a highly selective ALK5/ALK4 inhibitor. Pharmacokinetic study with <B>12b</B>·HCl in rats showed an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng × h/mL and maximum plasma concentration (<I>C</I><SUB>max</SUB>) of 1620 ng/mL. Rational optimization of <B>6</B> has led to the identification of a highly potent, selective, and orally bioavailable ALK5 inhibitor <B>12b</B>.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2014/jmcmar.2014.57.issue-10/jm500115w/production/images/medium/jm-2014-00115w_0012.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm500115w'>ACS Electronic Supporting Info</A></P>
Dae-Kee, Kim,Hua Jin, Chung,Krishnaiah, Maddeboina,Sreenu, Domalapally,Kota Sudhakar, Rao,Subrahmanyam, Vura BaJa,Chui-Yong, Park,jee-Yeon, Son,Yhun Yhong, Sheen 이화여자대학교 약학연구소 2012 藥學硏究論文集 Vol.- No.22
A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles 14a-d, 15a-d, 17a, 17b, 18a-d, 19a, and 19b has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 2-[3-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-pyrazol-1-yl]-N-phenylethanethioamide (18a) inhibited ALK5 phosphorylation with an IC(50) value of 0.013 μM and showed 80% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.