Polymyxin B nonapeptide, a cationic cyclic peptide derived by enzymatic processing from the naturally occurring peptide polymyxin B, is able to increase the permeability of the outer membrane of Gram-negative bacteria toward hydrophobic antibiotics probab
Diazaborine inhibits maturation of rRNAs for the large ribosomal subunit. Diazaborine blocks ribosome biogenesis by inhibiting the AAA-ATPase Drg1. Diazaborine treatment causes, within minutes, a rapid redistribution of the protein from the nucleolus to t
FTI-2153 is a potent and highly selective farnesyltransferase (FTase) inhibitor (IC50: 1.4 nM). FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing.
Globomycin, a lipopeptide antibiotic, is an inhibitor of signal peptidase II (LspA). It binds irreversibly to the peptidase, thereby inhibiting the processing of the prolipoprotein.
CAY10406 is a trifluoromethyl analog of an isatin sulfonamide compound that selectively inhibits caspases 3 and 7. The non-trifluoromethyl compound exhibits Ki values of 1.2 nM and 6 nM for caspases 3 and 7, respectively. For all of the other caspases tested, it is 100 to 1,000 times less potent. Caspases 3 and 7 are 'effector caspases' that are downstream from the initiating steps of apoptosis, and are implicated in the main proteolytic processing of the apoptotic signal. No data is currently available for caspase inhibition by CAY10406.
α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)
Concanamycin B is a macrolide antibiotic that selectively inhibits vacuolar type H+-ATPases, also known as V-ATPases (IC50 = 5 nM). In this way, it blocks the acidification of vacuolar organelles as well as early to late endosomal transport. Concanamycin B interferes with bone resorption and maturation of CD8 T lymphocytes. It also prevents processing of major histocompatibility complex (MHC) class II precursors in human B cells, inhibiting the expression of MHC class II molecules on the cell surface.
MI-1851 is a potent peptidomimetic inhibitor. MI-1851could prevent proteolytic processing of the S protein from SARSCoV-2 by endogenous furin in HEK293 cells.