Zobrazeno 1 - 10
of 171
pro vyhledávání: '"Peter P. Roller"'
Autor:
Peter P. Roller, Zaneta Nikolovska-Coleska, Iestyn Lewis, Krzysztof Krajewski, Lian Li, Shaomeng Wang, Jeanne A. Stuckey, Haian Fu, Raymond Dingledine, Min Qui, Yuhong Du
Publikováno v:
ASSAY and Drug Development Technologies. 9:382-393
Forster (fluorescence) resonance energy transfer (FRET) and fluores- cence polarization (FP) are widely used technologies for monitoring bimolecular interactions and have been extensively used in high- throughput screening (HTS) for probe and drug di
Autor:
Peter P. Roller, Pao-Yi Huang, Eun-Gyung Cho, Sheau-Ling Lee, Dongeun Park, Robert B. Dickson
Publikováno v:
Mechanisms of Development. 127(1-2):82-95
The epithelial-derived, type II transmembrane serine protease matriptase, the mouse homologue of which is epithin, has been shown to be involved in epidermal differentiation, hair formation, and thymus function. We show in this study that epithin/mat
Autor:
Marc C. Nicklaus, Terrence R. Burke, Robert J. Fisher, Lakshman Bindu, Karen W. Worthy, Biaolin Yin, Sheng Jiang, Peter P. Roller, Chenzhong Liao
Publikováno v:
Bioorg Med Chem Lett
Blocking the interaction between phosphotyrosine (pTyr)-containing activated receptors and the Src homology 2 (SH2) domain of the growth factor receptor-bound protein 2 (Grb 2) is considered to be an effective and non-cytotoxic strategy to develop ne
Autor:
Ako Ohkubo, Nobutaka Fujii, Yoshimasa Inagaki, Akira Otaka, Peter P. Roller, Motoyoshi Nomizu, Takeyoshi Yamashita, Haruaki Yajima
Publikováno v:
International Journal of Peptide and Protein Research. 37:145-152
A new two-step deprotection/cleavage procedure for t-butoxycarbonyl (Boc) based solid phase peptide synthesis is reported. First the protective groups are removed from 4-(oxymethyl)-phenylacetamidomethyl (PAM) resin attached peptide with the weak har
Publikováno v:
Current Organic Chemistry. 12:1502-1542
Autor:
Jeanne Stuckey, Zaneta Nikolovska-Coleska, Chao Yie Yang, Su Qiu, Jennifer L. Meagher, Sheng Jiang, Shaomeng Wang, Peter P. Roller
Publikováno v:
Biochemistry. 47:9811-9824
We have designed and synthesized a cyclic, bivalent Smac mimetic (compound 3) and characterized its interaction with the X-linked inhibitor of apoptosis protein (XIAP). Compound 3 binds to XIAP containing both BIR2 and BIR3 domains with a biphasic do
Autor:
Sheng Jiang, Peter P. Roller, Su Qiu, Jeanne Stuckey, Shaomeng Wang, Yumi Ueda, Zaneta Nikolovska-Coleska, Haiying Sun, Chao-Yie Yang, York Tomita, Jianfeng Lu, Krzysztof Krajewski, Jennifer L. Meagher
Publikováno v:
Journal of the American Chemical Society. 129:15279-15294
XIAP is a central apoptosis regulator that inhibits apoptosis by binding to and inhibiting the effectors caspase-3/-7 and an initiator caspase-9 through its BIR2 and BIR3 domains, respectively. Smac protein in its dimeric form effectively antagonizes
Autor:
L. Lowell Haas, Barbara A. Lyons, Peter P. Roller, David N. Krag, K. H. Lee, Stephanie C. Pero, Dean E. Wilcox, Haroula J. Argiros, Anne M. Spuches
Publikováno v:
Journal of Molecular Recognition. 20:245-252
Grb7 is a member of the Grb7 family of proteins, which also includes Grb10 and Grb14. All three proteins have been found to be overexpressed in certain cancers and cancer cell lines. In particular, Grb7 (along with the receptor tyrosine kinase erbB2)
Publikováno v:
The Journal of Organic Chemistry. 71:7307-7314
The design and synthesis of four nonnaturally occurring amino acid analogues of l-gamma-carboxyglutamic acid (Gla), appropriately protected for Fmoc-based solid-phase peptide synthesis (SPPS), is described. These amino acids are Bu-Mal 2, BCAH 3, Pen
Autor:
Krzysztof Krajewski, Su Qiu, Wei Gao, Yipin Lu, Zaneta Nikolovska-Coleska, Dongguang Qin, Sanjeev Shangary, Guoping Wang, Jeanne Stuckey, Ke Ding, Shaomeng Wang, Peter P. Roller
Publikováno v:
Journal of Medicinal Chemistry. 49:3432-3435
Potent, specific, non-peptide small-molecule inhibitors of the MDM2-p53 interaction were successfully designed. The most potent inhibitor (MI-63) has a K(i) value of 3 nM binding to MDM2 and greater than 10,000-fold selectivity over Bcl-2/Bcl-xL prot