Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Karen Ackermann"'
Autor:
Kenichi Nomoto, Kuan-Chun Huang, Donna Kolber-Simonds, Natalie C. Twine, George A. Moniz, Paul Chang, Jue-lon Shie, Jingzang Tao Miu, Karen Ackermann, Zhihong Chen, Sharon McGonigle, Jiayi Wu
Publikováno v:
Oncotarget
Impact Journals/National Center for Biotechnology Information (U.S.)
Impact Journals/National Center for Biotechnology Information (U.S.)
Inhibition of Poly(ADP-ribose) Polymerase1 (PARP1) impairs DNA damage repair, and early generation PARP1/2 inhibitors (olaparib, niraparib, etc.) have demonstrated clinical proof of concept for cancer treatment. Here, we describe the development of t
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:3073-3078
Compounds in which cysteine of the tetrapeptide CVFM has been replaced with a phenolic benzyl substituent inhibit farnesylation of H-ras protein by farnesyl transferase (FTase). In the most potent inhibitors (e.g., 5-chloro-2-hydroxybenzyl-VFM, IC 50
Autor:
James J. Kowalczyk, Ana Maria Garcia, Michael D. Lewis, Sharon L. Pinnow, Edmund M. Harrington, Karen Ackermann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2775-2780
Compounds in which cysteine and methionine have been linked by amino acids replacing the A1A2 portion of the CA1A2X box template inhibit farnesyl and geranylgeranyl transferases. The expected specificity for FTase over GGTase I is observed. A variety
Publikováno v:
Journal of Biological Chemistry. 268:18415-18418
The ras protooncogene is involved in regulation of cell growth. Mutations that activate the protein result in uncontrolled cell growth. Ras undergoes a series of posttranslational processing events, the first of which, farnesylation, is crucial for t
Autor:
Ana Maria Garcia, Edmund M. Harrington, Michael D. Lewis, Karen Ackermann, Xiaoning C. Sheng, Hu Yang
Publikováno v:
ChemInform. 30
Autor:
and Ana Maria Garcia, Michael D. Lewis, Edmund M. Harrington, Hu Yang, Xiaoning C. Sheng, Karen Ackermann
Publikováno v:
The Journal of organic chemistry. 64(1)
Syntheses of the potent sulfur-containing tetrapeptide mimetic farnesyl transferase inhibitors B956 (22) and B957 (23) are described. The two double bonds in 22 and 23 were constructed by application of iterative NHK and cuprate S(N)2' reactions. Nor
Autor:
Cheryl A. Rowell, James J. Kowalczyk, Michael D. Lewis, Celeste E. O'Connell, Ana Maria Garcia, Karen Ackermann
Publikováno v:
Chemicalpharmaceutical bulletin. 48(5)
CA 1 A 2 X peptidomimetics containing a modified proline at position A 2 were prepared and evaluated for their ability to inhibit farnesyltransferase (FTase) and geranylgeranyltransferase I (GGTase I) in enzymatic and cell-based assays. These compoun
Autor:
Karen Ackermann, Ana Maria Garcia, Michael D. Lewis, Cheryl A. Rowell, C.Eric Schwartz, Celeste E. O'Connell
Publikováno v:
Bioorganicmedicinal chemistry letters. 9(14)
A series of peptidomimetics based on a hydroxyproline scaffold was prepared and evaluated for inhibition of farnesyltransferase and geranylgeranyltransferase I in both enzymatic and cell-based assays. A number of analogs were potent and selective inh
Autor:
Sharon McGonigle, Karen Ackermann, Jiayi Wu, Karen TenDyke, Zhihong Chen, Kenichi Nomoto, George A. Moniz
Publikováno v:
Cancer Research. 72:4688-4688
E7449 is an orally bioavailable, potent, small molecule inhibitor of Poly(ADP-ribose) Polymerase (PARP)1 and PARP2. PARP1 is a key molecule in sensing and repairing single strand DNA breaks via the base excision repair (BER) pathway and may also play