Search Results - "Kerekes, Angela D"

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…”
Get full text

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…”
Get full text

Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core by Yu, Tao, Tagat, Jayaram R, Kerekes, Angela D, Doll, Ronald J, Zhang, Yonglian, Xiao, Yushi, Esposite, Sara, Belanger, David B, Curran, Patrick J, Mandal, Amit K, Siddiqui, M. Arshad, Shih, Neng-Yang, Basso, Andrea D, Liu, Ming, Gray, Kimberly, Tevar, Seema, Jones, Jennifer, Lee, Suining, Liang, Lianzhu, Ponery, Samad, Smith, Elizabeth B, Hruza, Alan, Voigt, Johannes, Ramanathan, Lata, Prosise, Winifred, Hu, Mengwei

“…The imidazo-[1,2-a]-pyrazine (1) is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 μM). Lead…”
Get full text

Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor by Yu, Tao, Zhang, Yonglian, Kerekes, Angela D., Tagat, Jayaram R., Doll, Ronald J., Xiao, Yushi, Esposite, Sara, Hruza, Alan, Belanger, David B., Voss, Matthew, Rainka, Matthew P., Basso, Andrea, Liu, Ming, Liang, Lianzhu, Sui, Ning, Prelusky, Daniel, Rindgen, Diane, Zhang, Likang

“…[Display omitted] Imidazo-[1, 2-a]pyrazine 1 is a potent inhibitor of Aurora A and B kinase in vitro and is effective in in vivo tumor models, but has poor…”
Get full text

Aurora Kinase Inhibitors Based on the Imidazo[1,2-a]pyrazine Core: Fluorine and Deuterium Incorporation Improve Oral Absorption and Exposure by Kerekes, Angela D, Esposite, Sara J, Doll, Ronald J, Tagat, Jayaram R, Yu, Tao, Xiao, Yushi, Zhang, Yonglian, Prelusky, Dan B, Tevar, Seema, Gray, Kimberly, Terracina, Gaby A, Lee, Suining, Jones, Jennifer, Liu, Ming, Basso, Andrea D, Smith, Elizabeth B

“…Aurora kinases are cell cycle regulated serine/threonine kinases that have been linked to cancer. Compound 1 was identified as a potent Aurora inhibitor but…”
Get full text

Concise syntheses and HCV NS5B polymerase inhibition of (2′R)-3 and (2′S)-2′-ethynyluridine-10 and related nucleosides by Bennett, Frank, Buevich, Alexei V., Huang, Hsueh-Cheng, Girijavallabhan, Vinay, Kerekes, Angela D., Huang, Yuhua, Malikzay, Asra, Smith, Elizabeth, Ferrari, Eric, Senior, Mary, Osterman, Rebecca, Wang, Lingyan, Wang, Jun, Pu, Haiyan, Truong, Quang T., Tawa, Paul, Bogen, Stephane L., Davies, Ian W., Weber, Ann E.

“…[Display omitted] (2′R)-Ethynyl uridine 3, and its (2′S)-diastereomer 10, are synthesised in a divergent fashion from the inexpensive parent nucleoside. Both…”
Get full text

Structure Reassignment of the Fungal Metabolite TAEMC161 as the Phytotoxin Viridiol by Wipf, Peter, Kerekes, Angela D

“…Two-dimensional NMR analyses including HMBC, NOESY, and ROESY as well as 1D NOE experiments led to a reassignment of the structure of the recently identified…”
Get full text

An Allenic Pauson−Khand-Type Reaction:  A Reversal in π-Bond Selectivity and the Formation of Seven-Membered Rings by Brummond, Kay M, Chen, Hongfeng, Fisher, Kimberly D, Kerekes, Angela D, Rickards, Brenden, Sill, Peter C, Geib, Steven J

“…Treatment of alkynyl allenes with [Rh(CO)2Cl]2 results in a formal [2 + 2 + 1] cycloaddition reaction. This reaction occurs with complete regioselectivity for…”
Get full text

Chiral Nonracemic α-Alkylidene and α-Silylidene Cyclopentenones from Chiral Allenes Using an Intramolecular Allenic Pauson−Khand-Type Cycloaddition by Brummond, Kay M, Kerekes, Angela D, Wan, Honghe

“…We have successfully effected a transfer of chirality from a chiral nonracemic allene to an α-alkylidene and an α-silylidene cyclopentenone. The…”
Get full text

Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors by Meng, Zhaoyang, Kulkarni, Bheemashankar A., Kerekes, Angela D., Mandal, Amit K., Esposite, Sara J., Belanger, David B., Reddy, Panduranga Adulla, Basso, Andrea D., Tevar, Seema, Gray, Kimberly, Jones, Jennifer, Smith, Elizabeth B., Doll, Ronald J., Siddiqui, M. Arshad

“…Our continued effort toward the development of the imidazo[1,2-a]pyrazine scaffold as Aurora kinase inhibitors is described. Bioisosteric approach was applied…”
Get full text

Organometallic photonucleases: A novel class of DNA-cleaving agents by Mohler, Debra L, Dain, David R, Kerekes, Angela D, Nadler, William R, Scott, Tricia L

“…The first demonstration of DNA cleavage by an organic radical generated via homolysis of a metalalkyl bond in a Cp-metal complex is presented. Irradiation of…”
Get full text

SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors by Basso, Andrea D., Liu, Ming, Gray, Kimberly, Tevar, Seema, Lee, Suining, Liang, Lianzhu, Ponery, Abdul, Smith, Elizabeth B., Monsma, Frederick J., Yu, Tao, Zhang, Yonglian, Kerekes, Angela D., Esposite, Sara, Xiao, Yushi, Tagat, Jayaram R., Hicklin, Daniel J., Kirschmeier, Paul

“…Purpose Aurora kinases are required for orderly progression of cells through mitosis, and inhibition of these kinases by siRNA or small molecule inhibitors…”
Get full text

A new method for the preparation of alkynes from vinyl triflates by Brummond, Kay M., Gesenberg, Kirsten Dilzer, Kent, Joseph L., Kerekes, Angela D.

“…Treatment of vinyl triflates with lithium diisopropylamide results in the selective formation of alkynes in moderate to high yields. Treatment of vinyl…”
Get full text

Novel intramolecular aminohydroxylation toward the syntheses of 2′-amino-2′-ethynyl nucleosides by Huang, Yuhua, Bennett, Frank, Buevich, Alexei, Girijavallabhan, Vinay, Kerekes, Angela D., Huang, Hsueh-Cheng, Tawa, Paul, Bogen, Stephane L., Davies, Ian W.

“…[Display omitted] •Tertiary amino nucleoside via tethered aminohydroxylation.•Diastereospecificity.•Nucleosides bearing ethynyl/amino at the C2′ position…”
Get full text