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Xiyan Hou,Hyuk Woo Lee,Dilip K. Tosh,Long Xuan Zhao,Lak Shin Jeong 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
Improved syntheses of potent and selective A3 adenosine receptor agonists, Cl-IB-MECA and thio-Cl-IB-MECA were accomplished from cheap stating material, D-ribose. New synthetic methods were found to be superior to old methods from the viewpoint of use of cheap starting material, number of steps, and overall yields.
Molecular Design and Engineering of Phosphopeptide Ligands to Target Lung Cancer Polo-like Kinase
Xiyan Yu,Yanwen Li,Ying Lou,Tong Wang 한국생물공학회 2017 Biotechnology and Bioprocess Engineering Vol.22 No.2
Polo-like kinase (Plk) plays a central role in centrosome cycle and is closely associated with the oncogenesis of lung cancer. The protein consists of a catalytic kinase domain (KD) and a regulatory polo-box domain (PBD); either direct inhibition of the KD’s catalytic activity or indirect disruption of the PBD–substrate interaction can be used to potentially suppress the pathological activation of lung cancer Plk. Here, we reported a successful molecular design and engineering of phosphopeptide ligands to target Plk PBD domain by integrating in silico modeling and in vitro assay. In the procedure, a helical peptide segment hps was derived from dimerization interface of the complex crystal structure of domain dimer using bioinformatics approach, which was then used as sequence template to generate potent phosphopeptide binders of Plk PBD domain in terms of a systematic residue mutation profile. Fluorescence anisotropy assays were conducted to substantiate the findings and conclusions obtaining from the molecular engineering. Consequently, three helical phosphopeptides, including the native hps and its two mutants hps-m1 and hps-m2, were successfully designed that can independently rebind to Plk PBD domain with a moderate or high affinity (Kd = 127, 26, and 5 μM, respectively). These peptide ligands can be considered as potent self-competitors to disrupt PBD dimerization in lung cancer metastasis. Structural and energetic analysis revealed that hydrophobic forces and van der Waals contacts confer strong stability for domain–peptide complex system, while hydrogen bonds and electrostatic interactions contribute specificity and selectivity to the complex recognition.
Hou, Xiyan,Lee, Hyuk-Woo,Tosh, Dilip K.,Zhao, Long Xuan,Jeong, Lak-Shin 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10
Improved syntheses of potent and selective $A_3$ adenosine receptor agonists, CI-IB-MECA and thio-CI-IB-MECA were accomplished from cheap stating material, D-ribose. New synthetic methods were found to be superior to old methods from the viewpoint of use of cheap starting material, number of steps, and overall yields.
Hou, Xiyan,Majik, MaheshS.,Kim, Kyunglim,Pyee, Yuna,Lee, Yoonji,Alexander, Varughese,Chung, Hwa-Jin,Lee, Hyuk Woo,Chandra, Girish,Lee, Jin Hee,Park, Seul-gi,Choi, Won Jun,Kim, Hea Ok,Phan, Khai,Gao, Z American ChemicalSociety 2012 Journal of medicinal chemistry Vol.55 No.1
<P>Truncated <I>N</I><SUP>6</SUP>-substituted-4′-oxo-and 4′-thioadenosine derivatives with C2 or C8 substitutionwere studied as dual acting A<SUB>2A</SUB> and A<SUB>3</SUB> adenosinereceptor (AR) ligands. The lithiation-mediated stannyl transfer andpalladium-catalyzed cross-coupling reactions were utilized for functionalizationof the C2 position of 6-chloropurine nucleosides. An unsubstituted6-amino group and a hydrophobic C2 substituent were required for highaffinity at the hA<SUB>2A</SUB>AR, but hydrophobic C8 substitutionabolished binding at the hA<SUB>2A</SUB>AR. However, most of synthesizedcompounds displayed medium to high binding affinity at the hA<SUB>3</SUB>AR, regardless of C2 or C8 substitution, and low efficacyin a functional cAMP assay. Several compounds tended to be full hA<SUB>2A</SUB>AR agonists. C2 substitution probed geometrically throughhA<SUB>2A</SUB>AR docking was important for binding in order of hexynyl> hexenyl > hexanyl. Compound <B>4g</B> was the most potentligand acting dually as hA<SUB>2A</SUB>AR agonist and hA<SUB>3</SUB>AR antagonist, which might be useful for treatment of asthma or otherinflammatory diseases.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jmcmar/2012/jmcmar.2012.55.issue-1/jm201229j/production/images/medium/jm-2011-01229j_0013.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/jm201229j'>ACS Electronic Supporting Info</A></P>
Static Anomaly Detection Framework for Android-based Mobile Phones
Honge Ren,Xiyan Xu,Jian Zhang,Yali Chen 보안공학연구지원센터 2016 International Journal of Security and Its Applicat Vol.10 No.12
With the rapid development of wireless communication, mobile network, and embedded system technologies, android-based mobile devices show a number of useful functions and then they are attacked by hackers for obtaining some useful information. In this paper, an efficient static anomaly detection framework is shown for android-based mobile phones to improve their security. The proposed framework uses support vector machine to perform the anomaly detection and exploits the cloud computing platform to reduce the impact on android-based mobile phones. Experimental results show that the proposed framework is better than existing anomaly detection frameworks in terms of the detection precision and the detection time.
Cheng Chen,Xulong Yuan,Xiyan Liu,Jianjun Dang 대한조선학회 2019 International Journal of Naval Architecture and Oc Vol.11 No.1
In this paper, the oblique water-entry impact of a vehicle with a disk cavitator is studied experimentally and numerically. The effectiveness and accuracy of the numerical simulation are verified quantitatively by the experiments in this paper and the data available in the literature. Then, the numerical model is used to simulate the hydrodynamic characteristics and flow patterns of the vehicle under different entry conditions, and the axial force is found to be an important parameter. The influences of entry angle, entry speed and cavitator area on the axial force are studied. The variation law of the force coefficient and the dimensionless penetration distance at the peak of the axial force are revealed. The research conclusions are beneficial to engineering calculations on the impact force of a vehicle with a disk cavitator over a wide range of water-entry parameters.