Factor inhibitors

Ketotifen Hrreceptor antagonist, mast cell stabilizer, eosinophil inhibitor, platelet-activating factor inhibitor May inhibit eosinophil chemotaxis... 

ArCOOH Morpholine EDC Growth factor-/ inhibitor 73 2006JME2210... 

A Ru-Josiphos catalyst was highly selective for the hydrogenation of an intermediate for an anthrax lethal factor inhibitor with a tetra-substituted C=C bond, as depicted in Figure 37.8 (Merck [44]). Rh-Josiphos (Lonza [42]) and Rh-Bo-Phoz (Eastman [45]) catalysts were effective for the hydrogenation of an exocy-clic and a cyclopropyl-substituted C=C bond. 

Recently, a SAMDI-MS assay was described by means of which endogenous caspase protease activities in cell lysates can be determined [26], Similar to the assay used to determine anthrax lethal factor inhibitors, peptide substrate SAMs for either caspase-3 or -8 were treated with cell lysates. In contrast to fluorescence assays, also longer peptide substrates could be used, thus enabling a better resolution of the two caspase activities. 

Lucentis contains ranibizumab and is available for intravitreal injection. It is a vascular endothelial growth factor inhibitor indicated for the treatment of neovascular (wet) age-related macular degeneration. Unlike verteporfin, which is used in photodynamic treatment of age-related macular degeneration, ranibizumab does not require activation by local irradiation using non-thermal red light. 

Uses Neovascular wet macular degenoation Action Vascular endothelial growth factor inhibitor Dose 0.5 mg intravitreal inj qmo Caution [C ] Hx thromboembohsm Contra Periocular Infxn Disp Inj SE Endophthalmitis, retinal detachment/hemorrhage, cataract, intraocular inflammation, conjunctival hemorrhage, eye pain, floaters EMS None OD Unlikely, but immediate effect would be vision loss and pain d/t t ocular pressure... 

Vlasuk GP, Bradbury A, Lopes-Kinninger L, Colon S, Bergum PW, Maki S, Rote WE. Pharmacokinetics and anticoagulant properties of the factor Vila - tissue factor inhibitor recombinant nematode anticoagulant protein c2 following subcutaneous administration in man dependence on the stoichiometric binding to circulating factor X. Thromb Haemost 2003 90 803-12. 

Jones RE, Moreland LW Tumor necrosis factor inhibitors for rheumatoid arthritis. Bull Rheum Dis 1999 48 14. 

Weinberg JM et al Biologic therapy for psoriasis An update on the tumor necrosis factor inhibitors infliximab, etanercept, and adalimumab, and the T-cell-targeted therapies efalizumab and alefacept. J Drugs Dermatol 2005 4 544. [PMID 16167412]... 

Drug Anakinra Trade Name Kineret Usual Dosage Subcutaneous injection 100 mg/d. Special Considerations Can be used alone or with other antiarthritic agents, but should not be used with tumor necrosis factor inhibitors. 

Roberts L, McColl GJ. Tumour necrosis factor inhibitors risks and benefits in patients with rheumatoid arthritis. Intern MedJ. 2004 34 687-693. 

Anderson PJ Timor necrosis factor inhibitors clinical implications of their different immunogenicity profiles. Semin. Arthritis Rheum. (2005) 34 (5 Suppl 11) 19-22. 

Broze GJ, Miletich JR Isolation of tissue factor inhibitor produced by HEPG2 hepatoma cells. Proc Natl Acad Sci USA 1987 84 1886-1890. 

The oxazolidinone-based compounds are the most common (Figure 23.1), and examples include antibacterial,27-28 adhesion receptor antagonists,29-30 tumor necrosis factor inhibitors,31 platelet aggregation inhibitors,32 antimigraine drugs,33 and monoamine oxidase inhibitors.3435 In one case, an oxazolidinone has been used as a transdermal drug delivery agent.36... 

Krueger, G. and K. Callis, Potential of tumor necrosis factor inhibitors in psoriasis and psoriatic arthritis. Arch. Dermatol., 2004, 140 218-25. 

Chiu T, Solberg J, Patil S et al (2009) Identification of novel non-hydroxamate anthrax toxin lethal factor inhibitors by topo-meric searching, docking and scoring, and in vitro screening. J Chem Inf Model 49 2726-2734... 

Yuan H, Johnson SL, Chen LH et al (2010) A novel pharmacophore model for the design of anthrax lethal factor inhibitors. Chem Biol Drug Des 76 263-268... 

Roy J, Kumar UC, Machiraju PK et al (2010) In silico studies on anthrax lethal factor inhibitors pharmacophore modeling and virtual screening approaches towards designing of novel inhibitors for a killer. J Mol Graph Model 29 256-265... 

The cereal dual function a-amylase/trypsin inhibitor proteins are cysteine-rich, disulphide-rich, double-headed, 13-16 kDa, dual function inhibitor proteins that inhibit both of the digestion enzymes a-amylase and trypsin [290-325] (Table 11). Thus the Zea (com) member of this family, com Hageman factor inhibitor (CHFI), is a double-headed 14 kDa protein that inhibits a-amylase and the serine proteases trypsin and blood clotting Factor Xlla [323-324] (Table 11). The structures of the bifunctional a-amylase/trypsin inhibitor proteins from Eleusine (ragi) (RBI) [292-295] and Zea (com) (CHFI) [325] have been determined. These proteins are structurally similar to the lipid transfer proteins, being composed of a bundle of 4 a-helices together with a short [3-sheet element connected by loops, the a-amylase- and protease-inhibitory domains being separately located [325]. 

Zea mays (com) (Poaceae) Com Hageman Factor inhibitor (CHFI) (127 aa 14 kDa 10 Cys) Trypsin, Factor XHa (Hageman Factor) (inhibits a-Amylase) [323- 325]... 

---