skin-structure

Omadacycline (Amadacycline), a new tetracycline antibiotic, can inhibit the 30s subunit of bacterial ribosome.

Tuaminoheptane is a sympathomimetic and vasoconstrictor that was once used as a nasal decongestant. It works by inhibiting and accelerating the release of norepinephrine, a mechanism that likely underpins its decongestant and stimulating effects. Unlike other norepinephrine-releasing agents such as phenethylamines, Tuaminoheptane's chemical structure lacks an aromatic ring. Additionally, it acts as a skin irritant and may cause contact dermatitis by inhibiting volume-regulated cation channels, which limits its utility as a decongestant.

Avarofloxacin (JNJ-Q2) is a broad-spectrum fluoroquinolone antibacterial drug under development for treating acute bacterial skin and skin structure infections, as well as community-acquired pneumonia.

Acorafloxacin is a broad-spectrum fluoroquinolone antibacterial drug being developed for the treatment of acute bacterial skin and skin structure infections and community-acquired pneumonia.

Ceftaroline fosamil hydrate acetate is a powerful cephalosporin antibiotic that exhibits broad-spectrum efficacy against both Gram-positive pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative bacteria. It possesses anti-infective properties suitable for studying complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP) [1] [2] [3].

Ceramide 1 A is a waxy lipid compound that is a lipid in the top skin layer. It has a special molecular structure because it contains a linoleic acid linked to a long chain omega-hydroxy acid.

Tuaminoheptane was originally developed as a nasal decongestant and belongs to the class of sympathomimetics and vasoconstrictors. It exhibits decongestant and stimulating effects by inhibiting and releasing norepinephrine. Unlike phenethylamine-based norepinephrine releasers, Tuaminoheptane has a unique chemical structure. Additionally, it may cause contact dermatitis due to its potential to irritate the skin by inhibiting volume-regulated anion channels, which limits its effectiveness as a decongestant.

Zifanocycline (KBP-7072), a third-generation semisynthetic aminomethylcycline antibiotic, inhibits bacterial ribosome function, displaying broad-spectrum antibacterial activity in vitro against both Gram-positive and Gram-negative bacteria, notably multidrug-resistant strains. It is formulated for oral and injectable use, targeting research on acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections [1] [2].

Cefdinir is an advanced broad-spectrum cephalosporin antibacterial compound approved for treating community-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, acute maxillary sinusitis, pharyngitis tonsillitis, acute bacterial otitis media, and uncomplicated skin and skin structure infections in both adult and pediatric patients.

Zifanocycline (KBP-7072) TFA is a semi-synthetic aminomethylcycline antibiotic with oral bioavailability that targets bacterial ribosomes to impede their function. Displaying a broad spectrum of in vitro antimicrobial efficacy, it combats both Gram-positive and Gram-negative bacteria, including numerous multidrug-resistant strains. Clinical investigations focus on treating acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections [1] [2].

Transdermal Peptide is a 11-amino acid peptide, binds to Na+ K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules. Transdermal Peptide (TD1) binds to ATP1B1, and mainly interacts with the C-terminus of ATP1B1 in yeast and mammalian cells. The interaction affects the expression and localization of ATP1B1 and epidermal structure, but can be antagonized by the exogenous competitor ATP1B1 or be inhibited by ouabain. Inhibition of Transdermal Peptide binding to ATP1B1 causes decreased delivery of macromolecular drugs across the skin[1]. [1]. Wang C, et al. Role of the Na(+) K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67.

Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (ORG1) that induces calcium accumulation in cells overexpressing OGR1 (EC50= ~35 nM).4Levels of D-erythrolysosphingomyelin are increased in skin isolated from patients with atopic dermatitis, as well as postmortem brain from patients with Niemann-Pick disease type A, but not type B.2,5L-threolysosphingomyelin is also an S1P1-3agonist (EC50s = 19.3, 131.8, and 313.3 nM, respectively).3This product is a mixture of D-erythroand L-threolysosphingomyelin. [Matreya, LLC. Catalog No. 1321] 1.Ito, M., Kurita, T., and Kita, K.A novel enzyme that cleaves the N-acyl linkage of ceramides in various glycosphingolipids as well as sphingomyelin to produce their lyso formsJ. Biol. Chem.270(41)24370-24374(1995) 2.Nixon, G.F., Mathieson, F.A., and Hunter, I.The multi-functional role of sphingosylphosphorylcholineProg. Lipid Res.47(1)62-75(2008) 3.Im, D.-S., Clemens, J., Macdonald, T.L., et al.Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): Structure-activity relationship of sphingosine1-phosphate receptorsBiochemistry40(46)14053-14060(2001) 4.Meyer zu Heringdorf, D., Himmel, H.M., and Jakobs, K.H.Sphingosylphosphorylcholine-biological functions and mechanisms of actionBiochim. Biophys. Acta1582(1-3)178-189(2002) 5.Rodriguez-Lafrasse, C., and Vanier, M.T.Sphingosylphosphorylcholine in Niemann-Pick disease brain: Accumulation in type A but not in type BNeurochem. Res.24(2)199-205(1999)