Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Roger Briesewitz"'
Autor:
Ziqing Qian, Roger Briesewitz, Dehua Pei, Zhengrong Wu, Punit Upadhyaya, Nicholas G. Selner, Sarah R. Clippinger
Publikováno v:
Angewandte Chemie International Edition. 54:7602-7606
Ras genes are frequently activated in human cancers, but the mutant Ras proteins remain largely "undruggable" through the conventional small-molecule approach owing to the absence of any obvious binding pockets on their surfaces. By screening a combi
Publikováno v:
MedChemComm. 4:378-382
A combinatorial library of 6 × 106 cyclic peptides was synthesized in the one bead-two compound format, with each bead displaying a unique cyclic peptide on its surface and a linear peptide encoding tag in its interior. Screening of the library agai
Autor:
Roger Briesewitz, Yu-Yu Liu, Amy M. Barrios, Sissy M. Jhiang, Dehua Pei, Ziqing Qian, Tao Liu
Publikováno v:
ACS Chemical Biology. 8:423-431
Cyclic peptides hold great potential as therapeutic agents and research tools, but their broad application has been limited by poor membrane permeability. Here, we report a potentially general approach for intracellular delivery of cyclic peptides. S
Autor:
Michael A. Caligiuri, Anne Marie Duchemin, Donna Frances Kusewitt, Jie Wang, Bradley W. Blaser, Roger Briesewitz, Tom Liu, Lisheng Wang
Publikováno v:
Blood. 110:2075-2083
Entry into the cell cycle is mediated by cyclin-dependent kinase 4/6 (CDK4/6) activation, followed by CDK2 activation. We found that pharmacologic inhibition of the Flt3 internal tandem duplication (ITD), a mutated receptor tyrosine kinase commonly f
Autor:
Patrick D. Braun, Thomas J. Wandless, Yun-Ming Lin, Kasturi Haldar, Thomas Akompong, Gregory Thomas Ray, Roger Briesewitz, Katherine T. Barglow
Publikováno v:
Journal of the American Chemical Society. 125:7575-7580
The cell-permeable dihydrofolate reductase inhibitor methotrexate was covalently linked to a ligand for the protein FKBP to create a bifunctional molecule called MTXSLF. The covalent tether between the two ligands was designed to be prohibitively sho
Publikováno v:
Proceedings of the National Academy of Sciences. 96:1953-1958
A general strategy is described for improving the binding properties of small-molecule ligands to protein targets. A bifunctional molecule is created by chemically linking a ligand of interest to another small molecule that binds tightly to a second
Autor:
Susan P. Whitman, Kristy J. Arnoczky, Min Wei, Trent B. Marburger, Clara D. Bloomfield, Jianhua Yu, Michael A. Caligiuri, Danilo Perrotti, Roger Briesewitz, Lisheng Wang, Jing Wen
Publikováno v:
Blood. 110:1022-1024
The CBL ubiquitin ligase targets a variety of activated tyrosine kinases (TKs) for degradation. Many TKs are mutationally or autocrine activated and/or often overexpressed at the mRNA and protein levels in acute leukemias. We hypothesized that CBL is
Autor:
John M. Goldman, Roger Briesewitz, Ross L. Levine, Steve R. Roof, Joshua J. Oaks, Kyosuke Nagata, Besim Ogretmen, Guido Marcucci, Alistair Reid, Dragana Milojkovic, James R. Van Brocklyn, Robert Bittman, Mark T. Ziolo, Omar Abdel-Wahab, Christopher J. Walker, Ann-Kathrin Eisfeld, Jane F. Apperley, Ralph B. Arlinghaus, Michael A. Caligiuri, Danilo Perrotti, Jason G. Harb, Greg Ferenchak, Paolo Neviani, Ramasamy Santhanam, Sahar A. Saddoughi, Alfonso Quintás-Cardama
Publikováno v:
Blood. 122(11)
FTY720 (Fingolimod, Gilenya) is a sphingosine analog used as an immunosuppressant in multiple sclerosis patients. FTY720 is also a potent protein phosphatase 2A (PP2A)-activating drug (PAD). PP2A is a tumor suppressor found inactivated in different t
Publikováno v:
Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 30(35)
Publikováno v:
The FASEB Journal. 23