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Pyrrole-Based Macrocyclic Small-Molecule Inhibitors That Target Oocyte Maturation
Gunasekaran, Pethaiah,Lee, So-Rim,Jeong, Seung-Min,Kwon, Jeong-Woo,Takei, Toshiki,Asahina, Yuya,Bang, Geul,Kim, Seongnyeon,Ahn, Mija,Ryu, Eun Kyung,Kim, Hak Nam,Nam, Ki-Yub,Shin, Song Yub,Hojo, Hirono Wiley - V C H Verlag GmbH & Co. KGaA 2017 CHEMMEDCHEM Vol.12 No.8
<P>Polo-like kinase1 (PLK1) plays crucial roles in various stages of oocyte maturation. Recently, we reported that the peptidomimetic compound AB103-8, which targets the polo box domain (PBD) of PLK1, affects oocyte meiotic maturation and the resumption of meiosis. However, to overcome the drawbacks of peptidic compounds, we designed and synthesized a series of pyrrole-based small-molecule inhibitors and tested them for their effects on the rates of porcine oocyte maturation. Among them, the macrocyclic compound (E/Z)-3-(2,16-dioxo-19-(4-phenylbutyl)-3,19-diazabicyclo[15.2.1]icosa-1(20),6,17-trien-3-yl)propyl dihydrogen phosphate (4) showed the highest inhibitory activity with enhanced inhibition against embryonic blastocyst formation. Furthermore, the addition of this compound to culture media efficiently blocked the maturation of porcine and mouse oocytes, indicating its ability to penetrate the zona pellucida and cell membrane. We investigated mouse oocytes treated with compound 4, and the resulting impairment of spindle formation confirmed PLK1 inhibition. Finally, molecular modeling studies with PLK1 PBD also confirmed the presence of significant interactions between compound 4 and PLK1 PBD binding pocket residues, including those in the phosphate, tyrosine-rich, and pyrrolidine binding pockets. Collectively, these results suggest that the macrocyclic compound 4 may serve as a promising template for the development of novel contraceptive agents.</P>
Fabrication of planar junctions in Graphene sheets using Focused Ion Beam
Gunasekaran Venugopal,Sang-Jae Kim 대한기계학회 2008 대한기계학회 춘추학술대회 Vol.2008 No.5
In this paper we present about fabrication of planar-type structures in thinner graphite sheets (thickness ~ 300 ㎚) using focused ion beam (FIB). We have studied temperature dependent transport characterization for these planar-type structures. Highly oriented pyrolytic graphite (HOPG) is a periodical stack of two dimensional (2-D) graphite sheets along the c-axis. The interlayers of graphite are loosely bonded each other with weak Van der waals forces. We describe a technique for preparing micronscale graphite sheets out of bulk graphite, method of electrical ohmic contacts and fabrication of planar-type structures in graphite sheet using focused ion beam (FIB). We also report the temperature dependence transport characteristics for several sizes of planar-type structures patterned in graphite flakes. We have observed semiconducting behavior and a small drop in resistance during the temperature down to 30 K. This paper will further describe the current (Ⅰ) - voltage (Ⅴ) characteristics for those planar structures.
Gunasekaran Gopalakrishnan,Raja Kalayarasan,Senthil Gnanasekaran,Biju Pottakkat 한국간담췌외과학회 2020 Annals of hepato-biliary-pancreatic surgery Vol.24 No.4
Backgrounds/Aims: Additional surgical procedures are often required in patients with chronic pancreatitis (CP) related complications. The present study aims to analyze the type of additional procedures required in patients who underwent Frey’s procedure (Frey’s plus) and to compare the short-term outcomes and quality of life with patients who underwent only Frey’s procedure. Methods: Retrospective analysis of a prospectively maintained database of patients who underwent surgery for CP between January 2012 and February 2018 and completed at least one year of follow-up. Patients who underwent non-Frey’s surgical procedures were excluded. Clinical parameters, postoperative pain relief (using Izbicki pain score) and functioning scale score (EORTC QLQ C30) of patients who underwent Frey’s plus procedure and only Frey’s procedure were compared. Results: Of the 146 patients who underwent surgery for CP during the study period, 100 patients (Frey’s procedure–68, Frey’s plus procedure–32) were included in this study. Roux-en-Y hepaticojejunostomy was the commonly performed additional procedure (n=12). The demographic and clinical parameters were comparable, except for more patients with jaundice (28.1% vs. 2.9%, p=0.01) and prolonged operative time (374.6 mins vs. 326.3 mins, p=0.01) in Frey’s plus group. However, there was no significant difference in mean intraoperative blood loss, postoperative morbidity or duration of hospital stay. At median (range) follow up of 34 (12-86) months, there was no significant difference in the pain control and quality of life between two groups. Conclusions: Frey’s plus procedure for chronic pancreatitis can be safely performed wherever indicated without adversely affecting the postoperative outcome or quality of life.
Temperature Dependence of Planar-type Graphite Structures
Gunasekaran Venugopal,Sang-Jae Kim 한국물리학회 2009 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.55 No.3
We have characterized the temperature dependence of the transport behavior for planar-type structures along ab-plane fabricated in micron-scale graphite layers. The planar-type structures of graphite layers were fabricated by using a focused ion beam (FIB) etching method. In-plane areas of 10 μm × 10 μm, 6 μm × 5 μm, 6 μm × 2 μm, and 1 μm × 1 μm exhibit semi-conducting behaviors which is contradictory to conventional metallic behavior of graphite flakes and show a small drop in resistance around 49 K. The origin of this effect is suspected from Ga+ ion damage during FIB fabrication. The fabricated planar-type structures show a transition in the current (I) - voltage (V) curves from diode-like characteristics around 30 K to an Ohmic behavior around 300 K. We have characterized the temperature dependence of the transport behavior for planar-type structures along ab-plane fabricated in micron-scale graphite layers. The planar-type structures of graphite layers were fabricated by using a focused ion beam (FIB) etching method. In-plane areas of 10 μm × 10 μm, 6 μm × 5 μm, 6 μm × 2 μm, and 1 μm × 1 μm exhibit semi-conducting behaviors which is contradictory to conventional metallic behavior of graphite flakes and show a small drop in resistance around 49 K. The origin of this effect is suspected from Ga+ ion damage during FIB fabrication. The fabricated planar-type structures show a transition in the current (I) - voltage (V) curves from diode-like characteristics around 30 K to an Ohmic behavior around 300 K.
Fabrication and Characteristics of Submicron Stacked-Junctions on Thin Graphite Flakes
Venugopal, Gunasekaran,Kim, Sang-Jae American Scientific Publishers 2011 Journal of Nanoscience and Nanotechnology Vol.11 No.2
<P>We report on the fabrication and transport characteristics of submicron-size stacks along c-axis of thin graphite flakes. The stacks were fabricated using a three-dimensional focused-ion-beam (FIB) etching technique. The stack with in-plane area A of 0.5 microm2 showed nonlinear concave-like I-V characteristics even at 300 K; however the stack with A of > 0.5 microm2 were shown an ohmic-like I-V characteristic at 300 K for both low and high-current biasing. It turned into nonlinear characteristics when the temperature goes down. The in-plane area dependence of stack capacitance were discussed and the observed capacitance of stack with A of 0.5 microm2 is smaller than the capacitance of stack with A of 1 microm2 which causes the nonlinear I-V characteristics in stack with A of 0.5 microm2 even at 300 K.</P>