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Plk1-Targeted Small Molecule Inhibitors: Mo-lecular Basis for Their Potency and Specificity
Ravichandran N. Murugan,박정은,김은희,신송엽,정재준,Kyung S Lee,방정규 한국분자세포생물학회 2011 Molecules and cells Vol.32 No.3
Members of polo-like kinases (collectively, Plks) have been identified in various eukaryotic organisms and play pivotal roles in cell proliferation. They are characterized by the presence of a distinct region of homology in the C-terminal noncatalytic domain, called polo-box domain (PBD). Among them, Plk1 and its functional homologs in other organisms have been best characterized because of its strong association with tumorigenesis. Plk1 is overexpressed in a wide spectrum of cancers in humans, and is thought to be an attractive anti-cancer drug target. Plk1 offers, within one molecule, two functionally different drug targets with distinct properties-the N-terminal catalytic domain and the C-terminal PBD essential for targeting the catalytic activity of Plk1 to specific subcellular locations. In this review, we focused on discussing the recent development of small-molecule and phosphopeptide inhibitors for their potency and specificity against Plk1. Our effort in understanding the binding mode of various inhibitors to Plk1 PBD are also presented.
Ahn, Mija,Murugan, Ravichandran N.,Shin, Song Yub,Kim, Eunjung,Lee, Jun Hyuck,Kim, Hak Jun,Bang, Jeong Kyu Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
Until now, few groups reported the antifreeze activity of cyclic glycopeptides; however, the tedious synthetic procedure is not amenable to study the intensive structure activity relationship. A series of N-linked cyclic glycopeptoids and glycopeptide have been prepared to evaluate antifreeze activity as a function of peptide backbone cyclization and methyl stereochemical effect on the rigid Thr position. This study has combined the cyclization protocol with solid phase peptide synthesis and obtained significant quantities of homogeneous cyclic glycopeptide and glycopeptoids. Analysis of antifreeze activity revealed that our cyclic peptide demonstrated RI activity while cyclic glycopeptoids showed no RI activity. These results suggest that the subtle changes in conformation and Thr orientation dramatically influence RI activity of N-linked glycopeptoids.
Mija Ahn,Ravichandran N. Murugan,신송엽,Eunjung Kim,Jun Hyuck Lee,김학준,Jeong-Kyu Bang 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
Until now, few groups reported the antifreeze activity of cyclic glycopeptides; however, the tedious synthetic procedure is not amenable to study the intensive structure activity relationship. A series of N-linked cyclic glycopeptoids and glycopeptide have been prepared to evaluate antifreeze activity as a function of peptide backbone cyclization and methyl stereochemical effect on the rigid Thr position. This study has combined the cyclization protocol with solid phase peptide synthesis and obtained significant quantities of homogeneous cyclic glycopeptide and glycopeptoids. Analysis of antifreeze activity revealed that our cyclic peptide demonstrated RI activity while cyclic glycopeptoids showed no RI activity. These results suggest that the subtle changes in conformation and Thr orientation dramatically influence RI activity of N-linked glycopeptoids
Kim, Tae-Sung,Park, Jung-Eun,Shukla, Anil,Choi, Sunho,Murugan, Ravichandran N.,Lee, Jin H.,Ahn, Mija,Rhee, Kunsoo,Bang, Jeong K.,Kim, Bo Y.,Loncarek, Jadranka,Erikson, Raymond L.,Lee, Kyung S. National Academy of Sciences 2013 PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF Vol.110 No.50
<P>Centrosomes play an important role in various cellular processes, including spindle formation and chromosome segregation. They are composed of two orthogonally arranged centrioles, whose duplication occurs only once per cell cycle. Accurate control of centriole numbers is essential for the maintenance of genomic integrity. Although it is well appreciated that polo-like kinase 4 (Plk4) plays a central role in centriole biogenesis, how it is recruited to centrosomes and whether this step is necessary for centriole biogenesis remain largely elusive. Here we showed that Plk4 localizes to distinct subcentrosomal regions in a temporally and spatially regulated manner, and that Cep192 and Cep152 serve as two distinct scaffolds that recruit Plk4 to centrosomes in a hierarchical order. Interestingly, Cep192 and Cep152 competitively interacted with the cryptic polo box of Plk4 through their homologous N-terminal sequences containing acidic-alpha-helix and N/Q-rich motifs. Consistent with these observations, the expression of either one of these N-terminal fragments was sufficient to delocalize Plk4 from centrosomes. Furthermore, loss of the Cep192- or Cep152-dependent interaction with Plk4 resulted in impaired centriole duplication that led to delayed cell proliferation. Thus, the spatiotemporal regulation of Plk4 localization by two hierarchical scaffolds, Cep192 and Cep152, is critical for centriole biogenesis.</P>
안미자,신송엽,김은주,강신원,김은희,류은경,정재준,Ravichandran N. Murugan,안용해,손호익,방정규 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.9
Antimicrobial peptides have recently gained the much attention because of their ability to make defense system from attacking bacterial infections. Drosocin has been considered as very attractive antibiotic agents because of low toxicity against human erythrocytes and active at the low concentration. We have studied the structureactivity relationship of a glycopeptide drosocin focused on the N-acetyl-D-galactoside at Thr^11 residue. Based on the radial diffusion assay, we found that the acetylation of carbohydrate moiety increased the antimicrobial activity and the Pro^10, present in the middle of drosocin plays an important role in the antimicrobial activity. Our results provide a good lead compound for further studies on the design of drosocin-based analogues targeting glyco linked Thr site.
Ahn, Mi-Ja,Sohn, Ho-Ik,Nan, Yong Hai,Murugan, Ravichandran N.,Cheong, Chae-Joon,Ryu, Eun-Kyoung,Kim, Eun-Hee,Kang, Shin-Won,Kim, Eun-Joo,Shin, Song-Yub,Bang, Jeong-Kyu Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.9
Antimicrobial peptides have recently gained the much attention because of their ability to make defense system from attacking bacterial infections. Drosocin has been considered as very attractive antibiotic agents because of low toxicity against human erythrocytes and active at the low concentration. We have studied the structureactivity relationship of a glycopeptide drosocin focused on the N-acetyl-D-galactoside at $Thr^{11}$ residue. Based on the radial diffusion assay, we found that the acetylation of carbohydrate moiety increased the antimicrobial activity and the $Pro^{10}$, present in the middle of drosocin plays an important role in the antimicrobial activity. Our results provide a good lead compound for further studies on the design of drosocin-based analogues targeting glyco linked Thr site.
Some congruence properties for -regular partitions, where l ∈ {4, 8, 13, 17, 19, 25, 40, 55}
P. Murugan,V. S. Veena,S. N. Fathima 장전수학회 2023 Proceedings of the Jangjeon mathematical society Vol.26 No.2
Some congruence properties for -regular partitions, where l ∈ {4, 8, 13, 17, 19, 25, 40, 55}
I. Dinaharan,N. Murugan 대한금속·재료학회 2012 METALS AND MATERIALS International Vol.18 No.1
A variety of ceramic particles is added to aluminum alloys to produce aluminum matrix composites (AMCs). Establishing the joining procedure for AMCs is an essential requirement prior to extending their applications. Friction stir welding (FSW) is an emerging solid state welding which eliminates all the defects associated with fusion welding of AMCs. An attempt has been made to friction stir weld AA6061/ ZrB2 in-situ composite. A four factor, five level central composite rotatable design has been used to minimize the number of exper-iments. The four factors considered are tool rotational speed, welding speed, axial force and weight percentage of ZrB2. A mathematical model has been developed incorporating the FSW process parameters to predict the ultimate tensile strength (UTS) and FS process is optimized using generalized reduced gradient method (GRG) to maximize the UTS. The effect of process parameters on UTS was analyzed. It was observed that the process parameters independently influence the UTS over the entire range studied in this work.