Search Results - "HA, SOOKHEE N."

Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design by Alleyne, Candice, Amin, Rupesh P, Bhatt, Bhavana, Bianchi, Elisabetta, Blain, J. Craig, Boyer, Nicolas, Branca, Danila, Embrey, Mark W, Ha, Sookhee N, Jette, Kelli, Johns, Douglas G, Kerekes, Angela D, Koeplinger, Kenneth A, LaPlaca, Derek, Li, Nianyu, Murphy, Beth, Orth, Peter, Ricardo, Alonso, Salowe, Scott, Seyb, Kathleen, Shahripour, Aurash, Stringer, Joseph R, Sun, Yili, Tracy, Rodger, Wu, Chengwei, Xiong, Yusheng, Youm, Hyewon, Zokian, Hratch J, Tucker, Thomas J

“…Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the…”
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Platensimycin and Platencin Congeners from Streptomyces platensis by Zhang, Chaowei, Ondeyka, John, Herath, Kithsiri, Jayasuriya, Hiranthi, Guan, Ziqiang, Zink, Deborah L, Dietrich, Lisa, Burgess, Bruce, Ha, Sookhee N, Wang, Jun, Singh, Sheo B

“…Platensimycin (1a) and platencin (2) are inhibitors of FabF and FabF/H bacterial fatty acid synthase. The discovery of natural congeners is an approach that…”
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A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5 by O'Brien, Julie A, Lemaire, Wei, Chen, Tsing-Bau, Chang, Raymond S L, Jacobson, Marlene A, Ha, Sookhee N, Lindsley, Craig W, Schaffhauser, Hervé J, Sur, Cyrille, Pettibone, Douglas J, Conn, P Jeffrey, Williams, Jr, David L

“…We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely…”
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A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain by O'Brien, Julie A, Lemaire, Wei, Wittmann, Marion, Jacobson, Marlene A, Ha, Sookhee N, Wisnoski, David D, Lindsley, Craig W, Schaffhauser, Hervé J, Rowe, Blake, Sur, Cyrille, Duggan, Mark E, Pettibone, Douglas J, Conn, P Jeffrey, Williams, Jr, David L

“…We found that N-[4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl]-2-hydroxybenzamide (CPPHA), is a potent and selective positive allosteric…”
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A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors by Tucker, Thomas J, Embrey, Mark W, Alleyne, Candice, Amin, Rupesh P, Bass, Alan, Bhatt, Bhavana, Bianchi, Elisabetta, Branca, Danila, Bueters, Tjerk, Buist, Nicole, Ha, Sookhee N, Hafey, Mike, He, Huaibing, Higgins, John, Johns, Douglas G, Kerekes, Angela D, Koeplinger, Kenneth A, Kuethe, Jeffrey T, Li, Nianyu, Murphy, BethAnn, Orth, Peter, Salowe, Scott, Shahripour, Aurash, Tracy, Rodger, Wang, Weixun, Wu, Chengwei, Xiong, Yusheng, Zokian, Hratch J, Wood, Harold B, Walji, Abbas

“…Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the…”
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Synthesis and biological evaluation of platensimycin analogs by SHEN, Hong C, DING, Fa-Xiang, TATA, James R, HAMMOND, Milton L, MACCOSS, Malcolm, COLLETTI, Steven L, SINGH, Sheo B, PARTHASARATHY, Gopalakrishnan, SOISSON, Stephen M, HA, Sookhee N, XUN CHEN, KODALI, Srinivas, JUN WANG, DORSO, Karen

“…Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could…”
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Molecular Simulations Identify Binding Poses and Approximate Affinities of Stapled α‑Helical Peptides to MDM2 and MDMX by Morrone, Joseph A, Perez, Alberto, Deng, Qiaolin, Ha, Sookhee N, Holloway, M. Katharine, Sawyer, Tomi K, Sherborne, Bradley S, Brown, Frank K, Dill, Ken A

“…Traditionally, computing the binding affinities of proteins to even relatively small and rigid ligands by free-energy methods has been challenging due to large…”
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Isolation, structure and biological activities of platencin A2–A4 from Streptomyces platensis by Zhang, Chaowei, Ondeyka, John, Dietrich, Lisa, Gailliot, Francis P., Hesse, Michelle, Lester, Michael, Dorso, Karen, Motyl, Mary, Ha, Sookhee N., Wang, Jun, Singh, Sheo B.

“…Natural products serve as a great reservoir for chemical diversity and are the greatest source for antibacterial agents. Recent discoveries of platensimycin…”
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Synthesis and evaluation of N-[(1 S,2 S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists by Du, Wu, Jewell, James P., Lin, Linus S., Colandrea, Vincent J., Xiao, Jing C., Lao, Julie, Shen, Chun-Pyn, Bateman, Thomas J., Reddy, Vijay B.G., Ha, Sookhee N., Shah, Shrenik K., Fong, Tung M., Hale, Jeffrey J., Hagmann, William K.

“…A series of N-[(1 S,2 S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamides were prepared by a divergent synthesis. Their…”
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Nodulisporic Acids D−F:  Structure, Biological Activities, and Biogenetic Relationships by Singh, Sheo B, Ondeyka, John G, Jayasuriya, Hiranthi, Zink, Deborah L, Ha, Sookhee N, Dahl-Roshak, Arlene, Greene, Joyce, Kim, Jennifer A, Smith, McHardy M, Shoop, Wesley, Tkacz, Jan S

“…Nodulisporic acids D, E, and F (7−12) are the newest members of a family of nontremorogenic indole-diterpenoids that are potent, orally bioavailable, antiflea…”
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Discovery of benzamides as potent human β3 adrenergic receptor agonists by Zhu, Cheng, Kar, Nam F., Li, Bing, Costa, Melissa, Dingley, Karen H., Di Salvo, Jerry, Ha, Sookhee N., Hurley, Amanda L., Li, Xiaofang, Miller, Randy R., Salituro, Gino M., Struthers, Mary, Weber, Ann E., Hale, Jeffrey J., Edmondson, Scott D.

“…[Display omitted] The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human…”
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Potent Kv1.3 inhibitors from correolide—modification of the C18 position by Bao, Jianming, Miao, Shouwu, Kayser, Frank, Kotliar, Andrew J., Baker, Robert K., Doss, George A., Felix, John P., Bugianesi, Randal M., Slaughter, Robert S., Kaczorowski, Gregory J., Garcia, Maria L., Ha, Sookhee N., Castonguay, Laurie, Koo, Gloria C., Shah, Kashmira, Springer, Marty S., Staruch, Mary Jo, Parsons, William H., Rupprecht, Kathleen M.

“…Correolide ( 1) was converted to a new series of tetracyclic Kv1.3 blockers 2. SAR for this class of compounds in two functional assays, Rb_Kv and human T cell…”
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Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder by Harper, Bart H., Wang, Liping, Zhu, Cheng, Kar, Nam F., Li, Bing, Moyes, Christopher R., Goble, Stephen D., Costa, Melissa, Dingley, Karen, Di Salvo, Jerry, Ha, Sookhee N., Hurley, Amanda, Li, Xiaofang, Miller, Randy R., Nagabukuro, Hiroshi, Salituro, Gino M., Smith, Sean, Struthers, Mary, Hale, Jeffrey J., Edmondson, Scott D., Berger, Richard

“…[Display omitted] The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β3-adrenergic receptor for the treatment of…”
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Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder by Harper, Bart H, Wang, Liping, Zhu, Cheng, Kar, Nam F, Li, Bing, Moyes, Christopher R, Goble, Stephen D, Costa, Melissa, Dingley, Karen, Di Salvo, Jerry, Ha, Sookhee N, Hurley, Amanda, Li, Xiaofang, Miller, Randy R, Nagabukuro, Hiroshi, Salituro, Gino M, Smith, Sean, Struthers, Mary, Hale, Jeffrey J, Edmondson, Scott D, Berger, Richard

“…The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β -adrenergic receptor for the treatment of overactive bladder…”
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Isolation, structure and biological activities of platencin A(2)-A(4) from Streptomyces platensis by Zhang, Chaowei, Ondeyka, John, Dietrich, Lisa, Gailliot, Francis P, Hesse, Michelle, Lester, Michael, Dorso, Karen, Motyl, Mary, Ha, Sookhee N, Wang, Jun, Singh, Sheo B

“…Natural products serve as a great reservoir for chemical diversity and are the greatest source for antibacterial agents. Recent discoveries of platensimycin…”
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Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA by Zhao, Zhijian, Wisnoski, David D., O’Brien, Julie A., Lemaire, Wei, Williams, David L., Jacobson, Marlene A., Wittman, Marion, Ha, Sookhee N., Schaffhauser, Herve, Sur, Cyrille, Pettibone, Doug J., Duggan, Mark E., Conn, P. Jeffrey, Hartman, George D., Lindsley, Craig W.

“…This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the…”
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Mini review on molecular modeling of P-glycoprotein (Pgp) by Ha, Sookhee N, Hochman, Jerome, Sheridan, Robert P

“…Membrane bound P-glycoprotein (Pgp) acts as an active transport pump. It plays a major role as a cause of multidrug resistance (MDR) and acts as a component of…”
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A Gly/Ala switch contributes to high affinity binding of benzoxazinone-based non-peptide oxytocin receptor antagonists by Hawtin, Stuart R., Ha, Sookhee N., Pettibone, Douglas J., Wheatley, Mark

“…Non-peptide antagonists of the oxytocin receptor (OTR) have been developed to prevent pre-term labour. The benzoxazinone-based antagonists L-371,257 and…”
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Binding modes of dihydroquinoxalinones in a homology model of bradykinin receptor 1 by Ha, Sookhee N., Hey, Pat J., Ransom, Rick W., Harrell, C. Meacham, Murphy, Kathryn L., Chang, Ray, Chen, Tsing-Bau, Su, Dai-Shi, Markowitz, M. Kristine, Bock, Mark G., Freidinger, Roger M., Hess, Fred J.

“…We report the first homology model of human bradykinin receptor B1 generated from the crystal structure of bovine rhodopsin as a template. Using an automated…”
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A revised potential-energy surface for molecular mechanics studies of carbohydrates by Ha, S N, Giammona, A, Field, M, Brady, J W

“…A revised CHARMM-type molecular mechanics potential-energy function has been developed for use in the dynamical simulation of simple carbohydrates in aqueous…”
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