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Inverse Agonists at $A_1$ Adenosine Receptors in Rat Cerebral Cortex (흰쥐의 뇌의$A_1$ 아데노신 수용체에 작용하는 역효현제에 관한 연구)

  • Park, Kyung-Sun;Yang, Wan-Suk;Kim, Kyung-Hwan
    • The Korean Journal of Pharmacology
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    • v.32 no.1
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    • pp.23-29
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    • 1996
  • According to the traditional receptor model, competitive antagonists share with agonists the ability to bind to a common site on receptors, but they are different from agonist in that they cannot trigger the biological response-i.e., they lack intrinsic efficacy. Recent findings extend the model by indicating that not all antagonists display an intrinsic efficacy of zero but that some display 'inverse agonism'. In the present study we studied the inverse agonism at $A_1$ adenosine receptors in membranes prepared from rat cerebral cortex. Eight commercially available $A_1$ adenosine receptor antagonists (CGS-15943, ADPX, CPT, DPCPX, DPX, N-0840, PACPX and 8-PT) were screened for inverse agonism by measuring the extent of $[^{35}S]guanosine-5'-({\gamma}-thio)$ triphosphate $([^{35}S]GTP_{\gamma}S)$ binding to G proteins. The agonist-induced stimulation of $[^{35}S]GTP_{\gamma}S$ bindings was completely blocked in the presence of $A_1$ adenosine receptor antagonists. Under optimal conditions, two types of antagonists could be distinguished. Seven antagonists including DPCPX decreased the basal $[^{35}S]GTP_{\gamma}S$ binding in the absence of agonist, displaying inverse agonist activity. One (CGS-15943) had no effect on the basal bindings. N-ethylmaleimide treatment reduced the basal bindings as well as agonist-mediated stimulation of $[^{35}S]GTP_{\gamma}S$ bindings, indicating that a substantial amount of this binding reflects an activated state of the C proteins. In good agreement with these findings, 0.1 mM GTP decreased the apparent affinity of the receptors for the agonist PIA, increased that for DPCPX, and had no effect on that for CGS-15943.

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The Effect of Herding Behavior and Perceived Usefulness on Intention to Purchase e-Learning Content: Comparison Analysis by Purchase Experience (무리행동과 지각된 유용성이 이러닝 컨텐츠 구매의도에 미치는 영향: 구매경험에 의한 비교분석)

  • Yoo, Chul-Woo;Kim, Yang-Jin;Moon, Jung-Hoon;Choe, Young-Chan
    • Asia pacific journal of information systems
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    • v.18 no.4
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    • pp.105-130
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    • 2008
  • Consumers of e-learning market differ from those of other markets in that they are replaced in a specific time scale. For example, e-learning contents aimed at highschool senior students cannot be consumed by a specific consumer over the designated period of time. Hence e-learning service providers need to attract new groups of students every year. Due to lack of information on products designed for continuously emerging consumers, the consumers face difficulties in making rational decisions in a short time period. Increased uncertainty of product purchase leads customers to herding behaviors to obtain information of the product from others and imitate them. Taking into consideration of these features of e-learning market, this study will focus on the online herding behavior in purchasing e-learning contents. There is no definite concept for e-learning. However, it is being discussed in a wide range of perspectives from educational engineering to management to e-business etc. Based upon the existing studies, we identify two main view-points regarding e-learning. The first defines e-learning as a concept that includes existing terminologies, such as CBT (Computer Based Training), WBT (Web Based Training), and IBT (Internet Based Training). In this view, e-learning utilizes IT in order to support professors and a part of or entire education systems. In the second perspective, e-learning is defined as the usage of Internet technology to deliver diverse intelligence and achievement enhancing solutions. In other words, only the educations that are done through the Internet and network can be classified as e-learning. We take the second definition of e-learning for our working definition. The main goal of this study is to investigate what factors affect consumer intention to purchase e-learning contents and to identify the differential impact of the factors between consumers with purchase experience and those without the experience. To accomplish the goal of this study, it focuses on herding behavior and perceived usefulness as antecedents to behavioral intention. The proposed research model in the study extends the Technology Acceptance Model by adding herding behavior and usability to take into account the unique characteristics of e-learning content market and e-learning systems use, respectively. The current study also includes consumer experience with e-learning content purchase because the previous experience is believed to affect purchasing intention when consumers buy experience goods or services. Previous studies on e-learning did not consider the characteristics of e-learning contents market and the differential impact of consumer experience on the relationship between the antecedents and behavioral intention, which is the target of this study. This study employs a survey method to empirically test the proposed research model. A survey questionnaire was developed and distributed to 629 informants. 528 responses were collected, which consist of potential customer group (n = 133) and experienced customer group (n = 395). The data were analyzed using PLS method, a structural equation modeling method. Overall, both herding behavior and perceived usefulness influence consumer intention to purchase e-learning contents. In detail, in the case of potential customer group, herding behavior has stronger effect on purchase intention than does perceived usefulness. However, in the case of shopping-experienced customer group, perceived usefulness has stronger effect than does herding behavior. In sum, the results of the analysis show that with regard to purchasing experience, perceived usefulness and herding behavior had differential effects upon the purchase of e-learning contents. As a follow-up analysis, the interaction effects of the number of purchase transaction and herding behavior/perceived usefulness on purchase intention were investigated. The results show that there are no interaction effects. This study contributes to the literature in a couple of ways. From a theoretical perspective, this study examined and showed evidence that the characteristics of e-learning market such as continuous renewal of consumers and thus high uncertainty and individual experiences are important factors to be considered when the purchase intention of e-learning content is studied. This study can be used as a basis for future studies on e-learning success. From a practical perspective, this study provides several important implications on what types of marketing strategies e-learning companies need to build. The bottom lines of these strategies include target group attraction, word-of-mouth management, enhancement of web site usability quality, etc. The limitations of this study are also discussed for future studies.

Patterns of Mediastinal Lymph Nodes Metastasis in Non-small Cell Lung Cancer according to the Primary Cancer Location (원발성 비소세포성 폐암의 폐엽에 따른 종격동 림프절 전이 양상)

  • Lee, Kyo-Sean;Song, Sang-Yun;Ryu, Sang-Woo;Na, Kook-Ju
    • Journal of Chest Surgery
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    • v.41 no.1
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    • pp.68-73
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    • 2008
  • Background: The presence of infiltrated mediastinal lymph nodes is a crucial factor for the prognosis of lung cancer. The aim of our study is to investigate the pattern of metastatic non-small cell lung cancer that spreads to the mediastinal lymph nodes, in relation to the primary tumor site, in patients who underwent major lung resection with complete mediastinal lymph node dissection. Material and Method: We retrospectively. studies 293 consecutive patients [mean age $63.0{\pm}8.3$ years (range $37{\sim}88$) and 220 males (75.1%)] who underwent major lung resection due to non-small cell lung cancer from January 1998 to December 2005. The primary tumor and lymph node status was classified according to the international TNM staging system reported by Mountain. The histologic type of the tumors was determined according to the WHO classification. Fisher's exact test was used; otherwise the chi-square test of independence was employed. A p-value < 0.05 was considered significant. Result: Lobectomy was carried out in 180 patients, bilobectomy in 50, sleeve lobectomy in 10 and pnemonectomy in 53. The pathologic report revealed 124 adenocarcinomas, 138 squamous-cell tumors, 14 adenosquamous tumors, 1 carcinoid tumor, 8 large cell carcinomas, 1 carcinosarcoma, 2 mucoepidermoid carcinomas and 5 undifferentiated tumors. The TNM stage was IA in 51 patients, IB in 98, IIB in 41, IIIA in 71, IIIB in 61 and IV in 6. 25.9 % of the 79 patients had N2 tumor. Most common infiltrated mediastinal lymph node was level No.4 in the right upper lobe, level No. 4 and 5 in the left upper lobe and level No. 7 in the other lobes, but no statistically significant difference was observed. Thirty-six patients (12.3%) presented with skip metastasis to the mediastinum. Conclusion: Mediastinal lymph node dissection is necessary for accurately determining the pTNM stage. It seems that there is no definite way that non-small cell lung cancer spreads to the lymphatics, in relation to the location of the primary cancer. Further, skip metastasis to the mediastinal lymph nodes was present in 12.3% of our patients.

Parameterization and Application of a Forest Landscape Model by Using National Forest Inventory and Long Term Ecological Research Data (국가산림자원조사와 장기생태연구 자료를 활용한 산림경관모형의 모수화 및 적용성 평가)

  • Cho, Wonhee;Lim, Wontaek;Kim, Eun-Sook;Lim, Jong-Hwan;Ko, Dongwook W.
    • Korean Journal of Agricultural and Forest Meteorology
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    • v.22 no.3
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    • pp.215-231
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    • 2020
  • Forest landscape models (FLMs) can be used to investigate the complex interactions of various ecological processes and patterns, which makes them useful tools to evaluate how environmental and anthropogenic variables can influence forest ecosystems. However, due to the large spatio-temporal scales in FLMs studies, parameterization and validation can be extremely challenging when applying to new study areas. To address this issue, we focused on the parameterization and application of a spatially explicit forest landscape model, LANDIS-II, to Mt. Gyebang, South Korea, with the use of the National Forest Inventory (NFI) and long-term ecological research (LTER) site data. In this study, we present the followings for the biomass succession extension of LANDIS-II: 1) species-specific and spatial parameters estimation for the biomass succession extension of LANDIS-II, 2) calibration, and 3) application and validation for Mt. Gyebang. For the biomass succession extension, we selected 14 tree species, and parameterized ecoregion map, initial community map, species growth characteristics. We produced ecoregion map using elevation, aspect, and topographic wetness index based on digital elevation model. Initial community map was produced based on NFI and sub-alpine survey data. Tree species growth parameters, such as aboveground net primary production and maximum aboveground biomass, were estimated from PnET-II model based on species physiological factors and environmental variables. Literature data were used to estimate species physiological factors, such as FolN, SLWmax, HalfSat, growing temperature, and shade tolerance. For calibration and validation purposes, we compared species-specific aboveground biomass of model outputs and NFI and sub-alpine survey data and calculated coefficient of determination (R2) and root mean square error (RMSE). The final model performed very well, with 0. 98 R2 and 8. 9 RMSE. This study can serve as a foundation for the use of FLMs to other applications such as comparing alternative forest management scenarios and natural disturbance effects.

Studies on the Function of the Rv2435c Gene of the Mycobacterium bovis BCG (Mycobacterium bovis BCG Rv2435c 유전자의 기능에 대한 연구)

  • Lee Seung-Sil;Bae Young-Min
    • Journal of Life Science
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    • v.15 no.3 s.70
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    • pp.415-422
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    • 2005
  • library of the mutants was prepared by transposon mutagenesis of the Mycobacterium bovis BCG. We screened this library for the resistance to an anti-tuberculosis antibiotic, PA-824. Most of the mutants resistant to the PA-824 were not able to synthesize the coenzyme $F_{420}$ which is normally produced by the wild type M. bovis BCG strains. HPLC analysis of the cellular extract showed that one of those mutants which lost the ability to synthesize $F_{420}$ still produced F0. The insertion site of the transposon in this mutant was determined by an inverse PCR and the transposon was found to be inserted in the Rv2435c open reading frame (ORF). Rv2435c ORF is predicted to encode an 80.3 kDa protein. Rv2435c protein appears to be bound to the cytoplasmic membrane, its N-terminal present in the periplasm and C-terminal in the cytoplasm. The C-terminal portion of this protein is highly homologous with the adenylyl cyclases of both prokaryotes and eukaryotes. There are 15 ORFs which have homology with the class III AC proteins in the genome of the M. tuberculosis and M. bovis. Two of those, Rv1625c and Rv2435c, are highly homologous with the mammalian ACs. We cloned the cytoplasmic domain of the Rv2435c ORF and expressed it with six histidine residues attached on its C-terminal in Escherichia coli to find out if this protein is a genuine AC. Production of that protein in E. coli was proved by purifying the histidine-tagged protein by using the Ni-NTA resin. This protein, however, failed to complement the cya mutation in E. coli, indicating that this protein lacks the AC activity. All of the further attempts to convert this protein to a functional AC by a mutagenesis with UV or hydroxylamine, or construction of several different fusion proteins with Rv1625c failed. It is, therefore, possible that Rv2435c protein might affect the conversion of F0 to $F_{420}$ not by synthesizing cAMP but by some other way.

A Study on the Screening of the Novel Genes Associated with Lysosomal Trafficking and Mutation Detection in Fibroblasts of the Patients with Mucolipidosis type II and III (리소좀 교통 이상을 초래하는 뮤코지방증 2형과 3형 환자의 섬유아세포를 이용한 신규 유전자 탐색 및 돌연변이에 대한 연구)

  • Song, Seng Mi;Chang, Soo Hee;Paik, Kyung Hoon;Jin, Dong-Kyu
    • Journal of The Korean Society of Inherited Metabolic disease
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    • v.5 no.1
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    • pp.65-75
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    • 2005
  • Purpose: To understand genetic differences and similarities between mucolipidosis and control. Methods: Using the fibroblast of the mucolipidosis II and control, forward and reverse subtracted libraries were constructed. Among these clones, we investigated mutations in the GNPTA (MGC4170) gene, which codes for the ${\alpha}/{\beta}$ subunits of phosphotransferase, and in the GNPTAG gene, which codes for the ${\gamma}$ subunits in 5 Korean patients with mucolipidosis type II or IIIA. Result: Several differentially expressed cDNAs were cloned and their sequences were determined. Mutation analysis of the interested gene, GNPTA was performed and we identified 7 mutations in the GNPTA gene, but none in the GNPTAG gene. The mutations in type II patients included p.Q104X(c.310C>T), p.R1189X(c.3565C>T), p.S1058X(c.3173C>G), p.W894X(c.2681G>A) and p.H1158fsX15(c.3474_3475delTA), all of which are non-sense or frame shift mutations. However, a splicing site mutation, IVS13+1G>A (c.2715+1G>A) was detected along with a non-sense or a frame shift mutation (p.R1189X or p.E858fsX3(c.2574_2575delGA)) in two mucolipidosis type IIIA patients. Conclusion: This report shows that mutations in the GNPTA gene coding for the ${\alpha}{\beta}$subunits of phosphotransferase, and not mutations in the GNPTAG gene, account for most of mutations found in Korean patients with mucolipidosis type II or IIIA.

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A Study on Light Condition between Pinus densiflora and Quercus variabilis Natural Mixed Forest Stands by Using the Hemispherical Photo Method (수관사진법을 이용한 소나무-굴참나무 천연림에 있어서의 광 조건 연구)

  • Chung Dong-Jun;Kim Young-Chai
    • Korean Journal of Agricultural and Forest Meteorology
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    • v.1 no.2
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    • pp.127-134
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    • 1999
  • This study was performed to obtain the basic data to present rational silvicultural tending plan. It makes these widely distributed pine-oak mixed stand and each of pure stand in middle province on object of this study and do comparative analysis of light condition about stand parameter and natural regeneration according to each slope(north, west and south) conditions of location in central part of South Korea. Sample plots for pine-oak mixed stand and pine and oak pure stand were established on each of southern, northern and western slopes based upon site and growth conditions of the slope. Sample plot was a circle of 0.05ha with a diameter of 25.24 m. A sample plot has between 30 and 40 tree in it. Total 23 sample plots were established; 9 pure pine stands, 8 pine-oak mixed stands. and 6 pure oak stands across lower, middle, upper parts of slopes. Relative light intensity within a stand was' measured by crown- photo(fish-eye lens; 180$^{\circ}$) system through fish-eye lens and by comparing each plot with the denuded through PAR-sensor. The crown closure ratio of pure pine stand (75%) shows much lower than that of mixed stand (90.9%) and pure oak stand (93%). The relative light intensity within a stand showed an opposite result. The crown closure of mixed stands tended to become gradually low as the slope moves from the north to the south, but the relative light Intensity within the stand tended to rise. By analyzing the relationship between the relative light intensity within a stand and stand parameter, light intensity within a stand tended to decrease as the diameter and N/ha increase. Number of oak seedlings and light intensity within a stand is in a straight-line regression relation. In particular, the number of oak seedlings was the highest in mixed stands on the southern slope. But no single pine seedling was found. The unfavorable conditions of l0cm thick litter layer and low relative light intensity in a stand (ranging between 4% and 8%) is considered to prevent pine seeds from germinating.

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Interannual and Seasonal Variations of Water Quality in Terms of Size Dimension on Multi-Purpose Korean Dam Reservoirs Along with the Characteristics of Longitudinal Gradients (우리나라 다목적댐 인공호들의 규모에 따른 연별.계절별 수질변이 및 상.하류간 종적구배 특성)

  • Han, Jeong-Ho;Lee, Ji-Yeoun;An, Kwang-Guk
    • Korean Journal of Ecology and Environment
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    • v.43 no.2
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    • pp.319-337
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    • 2010
  • Major objective of this study was to determine interannual and seasonal water quality along with characteristics of longitudinal gradients along the reservoir axis of the riverine zone (Rz)-to-lacustrine zone (Lz). Water quality dataset of five years during 2003~2007 used here were obtained from Ministry of Environment, Korea and ten physical, chemical and biological parameters were analyzed in the study. Similarity analysis, based on moropho-hydrological variables of reservoir surface area, watershed area, total inflow, and outflow, showed that the reservoirs were categorized as three groups of large-dam reservoirs (Chungju Reservoir, Daecheong Reservoir and Soyang Reservoir), mid-size reservoirs (Andong Reservoir, Yongdam Reservoir, Juam Reservoir and Hapcheon Reservoir), and small-size reservoirs (Hoengseong Reservoir and Buan Reservoir). According to the data comparison of high-flow year (2003) vs. lowflow year (2005), dissolved oxygen (DO), pH, biological oxygen demand (BOD), suspended solids (SS), total nitrogen (TN), total phosphorus (TP), chlorophyll-a (CHL) and electrical conductivity (EC) declined along the longitudinal axis of Rz to Lz and water transparency, based on Secchi depth (SD), increased along the axis. These results indicate that transparency was a function of Values of pH, DO, SS, SD, and EC at each site were greater in the low-flow year (2005) than the high-flow year (2003), whereas values of BOD, COD, TN, TP and CHL were greater in the high-flow year (2003). When values of TN, TP, CHL and SD in nine reservoirs were compared in the three zones of Rz, Tz, and Lz, values of TN, TP and CHL declined along longitudinal gradients and SD showed the opposite due to the sedimentation processes from the water column. Values of TN were not statistically correlated with TP values. The empirical linear models of TP-CHL and CHL-SD showed significant (p<0.05, $R^2$>0.04). In the mid-size reservoirs, the variation of CHL was explained ($R^2$=0.2401, p<0.0001, n=239) by the variation of TP. The affinities in the correlation analysis of mid-size reservoirs were greater in the CHL-SD model than any other empirical models, and the CHL-SD model had an inverse relations. In the meantime, water quality variations was evidently greater in Daecheong Reservoir than two reservoirs of Andong Reservoir and Hoengseong Reservoir as a result of large differences of water quality by long distance among Rz, Tz and Lz.

Enhancement of the Thermostability of a Fibrinolytic Enzyme from Bacillus amyloliquefaciens CH51 (Bacillus amyloliquefaciens CH51이 생산하는 혈전용해효소의 열안정성 개선)

  • Kim, Jieun;Choi, Kyoung-Hwa;Kim, Jeong Hwan;Song, Young-Sun;Cha, Jaeho
    • Journal of Life Science
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    • v.23 no.1
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    • pp.15-23
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    • 2013
  • AprE51 from Bacillus amyloliquefaciens CH51 is a 27 kDa subtilisin-like protease with fibrinolytic activity. AprE51-6 showing increased catalytic activity was produced previously. To enhance the thermostability of AprE51-6, 2 residues, Gly-166 and Asn-218 based on B. subtilis subtilisin E were mutated by site-directed mutagenesis. The results of the mutational analysis showed that substitution of arginine for Gly-166 (AprE51-7) increased the fibrinolytic activity 1.8-fold. An N218S mutant (AprE51-8) also increased the fibrinolytic activity up to 4.5-fold in a fibrin plate assay. Purified AprE51-7 and AprE51-8 mutants had a 1.9- and a 2.5-fold higher $k_{cat}$, respectively, and a 2.1-1.9-fold lower $K_m$, respectively. This resulted in a 3.8- and a 4.7-fold increase in catalytic efficiency ($k_{cat}/K_m$), respectively, relative to that of wild-type AprE51. AprE51-8 had a broader pH range than AprE51-6 and nattokinase, especially at an alkaline pH value. In addition, AprE51-8 showed higher thermostability than AprE51-6 at $60^{\circ}C$. The half-lives of AprE51-7 and AprE51-8 at $50^{\circ}C$ were 21.5 and 27.3 min, respectively, which are 2.0 and 2.6 times longer, respectively, than that of the wild-type AprE51.

Deformation structures of the Jurassic Ogcheon granite and the Honam Shearing, Ogcheon Area, Korea (옥천지역 쥬라기 옥천화강암의 변형구조와 호남전단운동)

  • Kang, Ji-Hoon
    • The Journal of the Petrological Society of Korea
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    • v.19 no.1
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    • pp.19-30
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    • 2010
  • The Jurassic Daebo Ogcheon granite is distributed in the Ogcheon area which is located in the central part of the Ogcheon Belt, Korea. This paper newly examines the timing of Honam shearing on the basis of the petrofabric researches on the deformation structures of the Ogcheon granite. The structural shape of Ogcheon granite is mainly characterized by a wedge shaped of E-W trend and an elongate shape of ENE trend in geological map and by contacts parallel to the regional S1 foliation in the host Ogcheon supergroup. It indicates that the pluton was permittedly emplaced after the S1 formation. The main deformation structures are marked by a solid-state tectonic foliation of N-S trend, which passes through the contact of the pluton, and by an aplitic dyke of E-W trend, and by sinistral, NW and E-W oriented shear zones on the eastern border of the pluton. The petrofabric study on the main deformation structures suggests that the tectonic foliation and the aplitic dyke were formed by the Honam dextral strike-slip shearing of (N)NE trend at ca. $500{\sim}450^{\circ}C$ deformation temperature, and that the sinistral shear zones could be induced by the dextral rotation of the pluton from its original site of intrusion, that is, by the shear strain which is due to sliding of the pluton past the host rocks. The history of emplacement and deformation of the Ogcheon granite and the previous results on the timing of Honam shearing would be newly established and reviewed as follows. (1) Early~Middle Jurassic(187~170 Ma); intrusion of syntectonic foliated granite related to Early Honam shearing, (2) Middle Jurassic(175~166 Ma); main magmatic period of Jurassic granitoids, the permitted emplacement of the Ogcheon granite, (3) Middle~Late Jurassic(168~152 Ma); main cooling period of Jurassic granitoids, the deformation of the Ogcheon granite related to Late Honam shearing. Thus, this study proposes that the Honam shear movement would occur two times at least during 187~152 Ma (ca. 35 Ma) through the intertectonic phase of 175~166 Ma.