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Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Van Manh, Nguyen,Ann, Jihyae,Kim, Eunhye,Cui, Minghua,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.12
<P><B>Abstract</B></P> <P>Glutamyl cyclase (QC) is a promising therapeutic target because of its involvement in the pathogenesis of Alzheimer’s disease. In this study, we developed novel QC inhibitors that contain 3-aminoalkyloxy-4-methoxyphenyl and 4-aminoalkyloxyphenyl groups to replace the previously developed pharmacophore. Several potent inhibitors were identified, showing IC<SUB>50</SUB> values in a low nanomolar range, and were further studied for <I>in vitro</I> toxicity and <I>in vivo</I> activity. Among these, inhibitors <B>51</B> and <B>53</B> displayed the most potent Aβ<SUB>N3pE−40</SUB>-lowering effects in <I>in vivo</I> acute model with reasonable BBB penetration, without showing cytotoxicity and <I>h</I>ERG inhibition. The molecular modeling analysis of <B>53</B> indicated that the salt bridge interaction and the hydrogen bonding in the active site provided a high potency. Given the potent activity and favorable BBB penetration with low cytotoxicity, we believe that compound <B>53</B> may serve as a potential candidate for anti-Alzheimer’s agents.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Ngo, Van T.H.,Hoang, Van-Hai,Tran, Phuong-Thao,Ann, Jihyae,Cui, Minghua,Park, Gyungseo,Choi, Sun,Lee, Jiyoun,Kim, Hee,Ha, Hee-Jin,Choi, Kwanghyun,Kim, Young-Ho,Lee, Jeewoo Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.5
<P><B>Abstract</B></P> <P>Pyroglutamate-modified amyloid β peptides (pGlu-Aβ) are highly neurotoxic and promote the formation of amyloid plaques. The pGlu-Aβ peptides are generated by glutaminyl cyclase (QC), and recent clinical studies indicate that QC represents an alternative therapeutic target to treat Alzheimer’s disease (AD). We have previously developed a series of QC inhibitors with an extended pharmacophoric scaffold, termed the Arg-mimetic D-region. In the present study, we focused on the structure activity relationship (SAR) of analogues with modifications in the D-region and evaluated their biological activity. Most compounds in this series exhibited potent activity in vitro, and our SAR analysis and the molecular docking studies identified compound <B>202</B> as a potential candidate because it forms an additional hydrophobic interaction in the <I>h</I>QC active site. Overall, our study provides valuable insights into the Arg-mimetic pharmacophore that will guide the design of novel QC inhibitors as potential treatments for AD.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Nguyen, Van Hong,Meghani, Nilesh M.,Amin, Hardik H.,Tran, Thao T.D.,Tran, Phuong H.L.,Park, Chulhun,Lee, Beom-Jin Elsevier 2018 Colloids and Surfaces B Vol.170 No.-
<P><B>Abstract</B></P> <P>Albumin is the most abundant protein in blood, and is the most frequently identified protein in the protein corona of nanoparticles (NPs). Thus, albumin plays an important role in modulating NPs’ physicochemical properties and bioavailability. In this study, the effect of bovine serum albumin (BSA) on gelatin-oleic nanoparticles’ (GONs) physicochemical properties and cellular uptake were evaluated. Coumarin-6 was used as indicator to track the cellular uptake of GONs. The binding of BSA onto the GON surface increased the size, slightly reduced the negative net charge of the GON, and improved GON stability. The presence of BSA in cell culture media reduced the cellular uptake of BSA-uncoated GONs on human embryonic kidney cells 293 (HEK 293) and human adenocarcinoma alveolar basal epithelial cells (A549) in the media without FBS addition. Pre-coated BSA corona decreased cellular uptake of GONs in A549 cells in the media, with and without supplemented with 10% fetal bovine serum (FBS) but drastically increased cellular uptake on HEK 293 cells. BSA could be used to modulate protein corona as an endogenous ligand in NP design simply by mixing or incubating BSA with NPs before in vivo administration to inhibit or induce cellular uptake in specific cell types.</P> <P><B>Highlights</B></P> <P> <UL> <LI> BSA adsorption increase GON size, reduced GON zeta potential and stabilized GONs. </LI> <LI> A lower cellular uptake of intact GONs was observed at a higher BSA concentration. </LI> <LI> BSA pre-coated GON modified cellular uptake of GONs in complete media. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Hoang, Van-Hai,Ngo, Van T. H.,Cui, Minghua,Manh, Nguyen Van,Tran, Phuong-Thao,Ann, Jihyae,Ha, Hee-Jin,Kim, Hee,Choi, Kwanghyun,Kim, Young-Ho,Chang, Hyerim,Macalino, Stephani Joy Y.,Lee, Jiyoun,Choi, S American Chemical Society 2019 Journal of medicinal chemistry Vol.62 No.17
<P>Alzheimer’s disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor <B>1</B>, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogues, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational analysis of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.</P> [FIG OMISSION]</BR>
Hoang, Van-Hai,Tran, Phuong-Thao,Cui, Minghua,Ngo, Van T. H.,Ann, Jihyae,Park, Jongmi,Lee, Jiyoun,Choi, Kwanghyun,Cho, Hanyang,Kim, Hee,Ha, Hee-Jin,Hong, Hyun-Seok,Choi, Sun,Kim, Young-Ho,Lee, Jeewoo American Chemical Society 2017 Journal of medicinal chemistry Vol.60 No.6
<P>Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of beta-amyloid peptides (pGlu-A beta) and thus may participate in the pathogenesis of Alzheimer's disease (AD). We designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, A beta 3E-42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 significantly reduced the brain concentrations of pyroform A beta and total A beta and restored cognitive functions. This potent A beta-lowering effect was achieved by incorporating an additional binding region into our previously established pharmacophoric model, resulting in strong-interactions with the carboxylate group of Glu327 in the QC binding site. Our study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.</P>
Social Optimization Strategy in Unobserved Queueing Systems in Cognitive Radio Networks
Do, C. T.,Tran, N. H.,Mui Van Nguyen,Choong Seon Hong,Sungwon Lee IEEE 2012 IEEE communications letters Vol.16 No.12
<P>We study a noncooperative game problem for queueing control in the Cognitive Radio (CR) system where selfish Secondary User's (SU) data packets (a.k.a. 'customers' in this work) are served by a CR base station (a.k.a. 'server'). The scenario is modeled as an M/M/1 queueing game with server breakdowns where each customer wants to optimize their benefit in a selfish distributed manner. We first show that the game has an inefficient unique Nash Equilibrium (NE). In order to improve the outcome efficiency, we propose an appropriate admission fee that can be easily implemented at the server. We then show that the social welfare at the equilibrium point can be coincided the social welfare of the socially optimal strategy.</P>
Efficacy and Tolerability of Ich Nieu Khang Dietary Supplement for Overactive Bladder
Hoan M. Vu,Van T. H. Tran,Huy Q. Hoang,Bo Han,Ba X. Hoang 한국식품영양과학회 2023 Journal of medicinal food Vol.26 No.4
This study aims to assess the effectiveness and safety of plant-derived food supplement Ich Nieu Khang (INK) as a dietary supplement for overactive bladder (OAB) symptoms. A total of 50 patients 18–80 years of age with the diagnosis and symptoms of the OAB were enrolled in the study and followed up for 30 days. The INK treatment efficacy, in terms of changes in nocturnal and day-time urination frequency, urination incontinence episodes, level of OAB symptoms according to Homma's OABSS scale, sleep quality according to Pittsburg Sleep Quality Index (PSQI), and possible side effects of the INK phytotherapy, was evaluated. INK significantly improved all OAB symptoms scores with a reduction of average nocturia from 4.06 ± 1.53 to 1.14 ± 0.94, the daily average urination urgency from 7.67 ± 5.00 to 5. 82 ± 3.70, the daily average frequency of urination from 9.96 ± 4.04 to 8.00 ± 3.70, weekly average incontinence of urination from 0.92 ± 1.56 to 0.60 ± 1.02, and OABSS Homma's score decreased from 9.31 ± 1.44 to 6.8 ± 2.21. INK phytotherapy also resulted in sleep quality improvement by PSQI score decreasing from 13.11 ± 1.33 to 10.54 ± 2.21. There were no adverse effects and abnormalities in paraclinical parameters with INK therapy. The results of our study suggest that INK dietary supplement is effective and safe phytotherapy for patients with primary OAB symptoms within 30 days of treatment. Larger control clinical trials are warranted to confirm our findings and promote wider use of INK for OAB and possible other age-related urination disorders.