The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
26954324 |
77 |
Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51. |
Max Planck Institute of Psychiatry |
26200936 |
39 |
Applications of Fluorine in Medicinal Chemistry. |
Bristol-Myers Squibb Research and Development |
26419422 |
33 |
Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands. |
Max Planck Institute of Psychiatry |
26321603 |
8 |
Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity. |
Xi'An Jiaotong University |
26102506 |
40 |
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
Celgene |
26083478 |
66 |
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
Celgene |
23647266 |
35 |
Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control. |
Max Institute of Psychiatry |
8627611 |
17 |
Structure-based design of novel, urea-containing FKBP12 inhibitors. |
Agouron Pharmaceuticals |
| 6 |
High-affinity FKBP-12 ligands derived from (R)-()-carvone. Synthesis and evaluation of FK506 pyranose ring replacements |
TBA |
| 12 |
Design, synthesis and evaluation of dual domain FKBP ligands |
TBA |
21413808 |
170 |
Synopsis of some recent tactical application of bioisosteres in drug design. |
Bristol-Myers Squibb Pharmaceutical Research and Development |
22455444 |
93 |
Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52. |
Max Planck Institute of Psychiatry |
22455398 |
122 |
Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52. |
Max Planck Institute of Psychiatry |
21142106 |
28 |
Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein. |
University of Wu£Rzburg |
16134928 |
34 |
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. |
The Scripps Research Institute |
7241506 |
40 |
New analgesic drugs derived from phencyclidine. |
TBA |
9857082 |
67 |
Immunophilins: beyond immunosuppression. |
Guilford Pharmaceuticals |
10091702 |
2 |
Cleavage of the cyclohexyl-subunit of rapamycin results in loss of immunosuppressive activity. |
Novartis Pharma |
| 13 |
Synthesis of FK506-Cyclosporin hybrid macrocycles |
TBA |
| 8 |
Design, synthesis and X-ray crystallographic studies of [7.3.1] and [8.3.1] macrocyclic FKBP-12 ligands |
TBA |
| 8 |
Preparation and in vitro activities of naphthyl and indolyl ether derivatives of the FK-506 related immunosuppressive macrolide ascomycin |
TBA |
| 1 |
Synthesis and FKBP binding of small molecule mimics of the tricarbonyl region of FK506 |
TBA |
| 15 |
Alkyl ether derivatives of the FK-506 related, immunosuppressive macrolide L-683,742 (C31-O-desmethyl ascomycin) |
TBA |
| 4 |
Alkyl ether analogs of the FK-506 related, immunosuppressive macrolide L-683,590 (ascomycin) |
TBA |
| 7 |
Synthesis and evaluation of dual domain macrocyclic FKBP12 ligands. |
TBA |
| 2 |
Synthesis and study of a non macrocyclic FK506 derivative. |
TBA |
| 4 |
The contribution to binding of the pyranoside substituents in the excised binding domain of FK-506 |
TBA |
| 2 |
The affinity of the excised binding domain of FK-506 for the immunophilin FKBP12. |
TBA |
18038971 |
88 |
Nuclear magnetic resonance fragment-based identification of novel FKBP12 inhibitors. |
University of California San Diego |
12951089 |
13 |
Regulation of gene expression by synthetic dimerizers with novel specificity. |
Ariad Gene Therapeutics |
12139466 |
11 |
Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. |
Guilford Pharmaceuticals |
11992791 |
53 |
Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides. |
Guilford Pharmaceuticals |
11992790 |
40 |
Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors. |
Guilford Pharmaceuticals |
10888319 |
5 |
Antifungal rapamycin analogues with reduced immunosuppressive activity. |
Abbott Laboratories |
10741553 |
8 |
Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
10737745 |
20 |
Investigating protein-ligand interactions with a mutant FKBP possessing a designed specificity pocket. |
Ariad Gene Therapeutics |
10543889 |
4 |
Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12. |
Abbott Laboratories |
10479292 |
16 |
Synthesis and cytotoxic evaluation of cycloheximide derivatives as potential inhibitors of FKBP12 with neuroregenerative properties. |
Max-Planck Research Unit |
10450987 |
22 |
Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity. |
Merck Research Laboratories |
10450986 |
7 |
C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study. |
Merck Research Laboratories |
31693351 |
473 |
Discovery of 4 |
TBA |
29400967 |
136 |
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
Bristol-Myers Squibb |
9873523 |
5 |
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential. |
Merck Research Laboratories |
30565923 |
34 |
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology. |
Eberhard Karls University T£Bingen |
9767630 |
9 |
Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations. |
Yale University |
9599228 |
27 |
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency. |
Abbott Laboratories |
16854055 |
13 |
Simplified cyclic analogues of bastadin-5. Structure-activity relationships for modulation of the RyR1/FKBP12 Ca2+ channel complex. |
University of California |
29578710 |
26 |
Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins. |
Max Planck Institute of Psychiatry |
29308895 |
24 |
Highly Selective, Potent, and Oral mTOR Inhibitor for Treatment of Cancer as Autophagy Inducer. |
Nankai University |
28412204 |
27 |
A calcineurin antifungal strategy with analogs of FK506. |
Amplyx Pharmaceuticals |
14993260 |
2 |
FE200041 (D-Phe-D-Phe-D-Nle-D-Arg-NH2): A peripheral efficacious kappa opioid agonist with unprecedented selectivity. |
University of Arizona |