Robotnikinin
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This article, Robotnikinin, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission. |
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Robotnikinin, IUPAC name (E)-N-(4-chlorobenzyl)-2-(5,12-dioxo-2-phenyl-1-oxa-4-azacyclododec-8-en-6-yl)acetamide, is a small-molecule chemical inhibitor of sonic hedgehog (Shh) morphogen, inhibiting hedgehog signaling through specific binding and blockade of Shh signaling factor. It is the first-characterized hedgehog inhibitor whose molecular mechanism of action is through blockade of Shh protein and not a subsequent factor of the hedgehog signaling cascade.[1]
It is a 12-membered macrocycle originally synthesized and characterized by Stanton et. al in 2009 by a collaboration based at Harvard University, Stanford University School of Medicine, Massachusetts General Hospital, the Broad Institute of Harvard and Massachusetts Institute of Technology, and Howard Hughes Medical Institute.
[edit] References
- ↑ Stanton et. al (2009). A small molecule that binds Hedgehog and blocks its signaling in human cells. Nature Chemical Biology (5), 154-156
| Anticancer Drugs (Acumen Science Laboratories): Chemical Biology and Oncology | ||
|---|---|---|
| A-83-01 (Colon Cancer) · Bicuculline (Brain Cancer) · BMS-354825 (Chronic Myeloid Leukemia) · Dorsomorphin/LDN-193189 (Lung Cancer) · Cyclopamine/Robotnikinin/SANT1 (Skin, Brain, Prostate, and Colon Cancers) · LY165163 (Brain Cancer) · PK115-584 (Colon and Brain Cancer) | ||
| Source · Edit | ||
| Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant) | ||
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| Receptor Tyrosine Kinases | A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR) | |
| Signaling Kinases | A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK) | |
| G Protein-Coupled Receptor | (+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3) | |
| Ion Channels | BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR) | |
| Transporters | O-1783 (DAT) · WF-23 (DAT, SERT) | |
| Nuclear Receptor | All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3) | |
| Protein Phosphatases | Endothall (PP2A) | |
| Polypharmacological | Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine | |
| Other | 2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB) | |
| Uncharacterized | Neuropathiazol | |
| Libraries | Kinase Inhibitor Library | |
| Publications | ||
| Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine) | ||
| Source · Edit | ||
