Results 171 to 180 of about 93,555 (212)
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FKBPs in chromatin modification and cancer
Current Opinion in Pharmacology, 2011FK506-binding proteins (FKBPs) are intracellular receptors for FK506 and rapamycin, immunosuppressants that have recently been utilized as anticancer drugs. In the cytoplasm, FKBPs and these drugs modulate signal transduction pathways. However, recent reports reveal novel functions of FKBPs in the nucleus, which include regulation of transcription ...
Ya-Li, Yao +3 more
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Design and synthesis of novel FKBP inhibitors
Journal of Medicinal Chemistry, 1992Small molecule FKBP inhibitors were prepared with inhibitory activity ranging from micromolar to nanomolar. The design of these inhibitors derives from a structural analysis of the substrates for FKBP and cyclophilin. As a consequence of this analysis two key observations were made, namely: (1) amino ketone moieties are suitable as FKBP recognition ...
J R, Hauske +5 more
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Recent Progress in FKBP Ligand Development
Current Molecular Pharmacology, 2015FK506-binding proteins have been implicated in numerous human diseases suggesting novel therapeutic opportunities. In particular, the large FKBP51 has emerged as an important regulator of the stress-coping system and as an established risk factor for stress-related disorders.
Xixi, Feng +2 more
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FKBP Ligands as Novel Therapeutics for Neurological Disorders
Mini-Reviews in Medicinal Chemistry, 2001Given their clinical importance for the treatment of acute and chronic neurodegenerative diseases in humans including nerve injuries (e.g. Alzheimer's disease, Parkinson's disease, diabetic neuropathy) a number of different approaches were pursued to obtain selectively acting FK506-binding protein (FKBP) ligands: computational methods and target ...
C, Christner, T, Herdegen, G, Fischer
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Targeting FKBP isoforms with small-molecule ligands
Current Opinion in Pharmacology, 2011The FK506 binding protein (FKBP) family of proteins provide an interesting series of drug targets since different isoforms modulate diverse cellular pathways. There are therapeutic opportunities in the fields of cancer therapy, neurodegenerative conditions and psychiatric disorders. X-ray crystallographic or NMR data are available for eight of fourteen
Elizabeth A, Blackburn +1 more
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FKBPs and their role in neuronal signaling
Biochimica et Biophysica Acta (BBA) - General Subjects, 2015Ligands for FK506-binding proteins, also referred to as neuroimmunophilin ligands, have repeatedly been described as neuritotrophic, neuroprotective or neuroregenerative agents. However, the precise molecular mechanism of action underlying the observed effects has remained elusive, which eventually led to a reduced interest in FKBP ligand development.A
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FKBP-12 is not an Inhibitor of Protein Kinase C
Immunological Investigations, 1992It was recently noted that the amino acid sequence of FK506 binding protein (FKBP-12) is nearly identical to that of an endogenous inhibitor of protein kinase C, PKCI-2. To follow up on this observation, we have tested the hypothesis that FKBP-12 is an inhibitor of PKC.
V A, Ruff +4 more
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Three-dimensional structure of FKBPs
1997Abstract The mammalian cytosolic FKBP12 protein was discovered through its ability to bind the immunosuppressive agents FK506 (tacrolimus) and rapamycin (sirolimus) (Harding et al., 1989; Siekierka et al., 1989). The FKBP family, for FK506 binding proteins, is growing rapidly, and the best characterized members are the mammalian proteins
J Liang, J Clardy
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Direct calculation of the binding free energies of FKBP ligands
The Journal of Chemical Physics, 2005Direct calculations of the absolute free energies of binding for eight ligands to FKBP protein were performed using the Fujitsu BioServer massively parallel computer. Using the latest version of the general assisted model building with energy refinement (AMBER) force field for ligand model parameters and the Bennett acceptance ratio for computing free ...
Hideaki, Fujitani +7 more
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Tête-à-tête: the function of FKBPs in plant development
Trends in Plant Science, 2007Compared with that of other eukaryotes, the nuclear genome of the model plant Arabidopsis thaliana encodes an expanded family of FK506-binding proteins (FKBPs). Whereas approximately half of the FKBPs are implicated in the regulation of photosynthetic processes, a subcluster appears to be stress responsive. Recent reports indicate that a discrete group
Geisler M, Bailly A
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