ubenimex

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ubenimex

Alternative oncology
A competitive protease-inhibiting peptide isolated from the supernatant broth of cultured Streptomyces olivoreticuli that inhibits aminopeptidases B and N and leukotriene A4 hydrolase. Ubenimex stimulates the immune system, activates macrophages, increases production and secretion of IL-1 and IL-2, and stimulates T cells and haematopoiesis. It is in clinical trials for acute myeloid leukaemia and may be effective in treating various cancers, including Hodgkin lymphoma, leukaemia, melanoma, and cancers of the bladder, oesophagus, head and neck, lung and stomach.
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5% deoxycholate, 1 mM PMSF and protease inhibitor cocktail (2 mM [4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride], 14 [micro]M (N-(trans-epoxysuccinyl)-L-leucine 4-guanidinobutylamide], 130 [micro]M bestatin, 0.
1% sodium dodecyl sulfate) containing 100 mM sodium orthovanadate and a protease inhibitor cocktail containing 4-(2-aminoethyl benzenesulfonyl fluoride), pepstatin A, E-64, bestatin, leupeptin, and aprotinin (Sigma).
Genco found that, in test tube experiments, bestatin does not affect chemotaxis in neutrophils from healthy subjects, but it almost doubles the chemotactic activity in neutrophils from LJP patients.
Bestatin is a well-characterized, oral, small molecule inhibitor of leukotriene A[sub.
Bestatin is thus a potential therapeutic candidate for treatment of PAH where pathological inflammation is believed to be important in the etiology of the disease.
Our partnership with Nippon Kayaku and access to Bestatin, a well-characterized, commercially available drug in Japan, allows us to prepare for a clinical study in patients with PAH.
We are pleased to enter into this agreement with Eiger BioPharmaceuticals and establish a path for Bestatin to be studied in PAH," said Yoshihiro Nambu, MD, PhD, Head of Pharmaceuticals Group, Nippon Kayaku.
8 [micro]M aprotinin, 20 [micro]M leupeptin, 50 [micro]M bestatin, 10 [micro]M pepstatin A, 15 [micro]M L-trans-epoxy succinyl-leucyl-amido (4-guanidino) butane, 1 mM phenylmethyl sulfonyl fluoride, 1 mM sodium fluoride, and 1 mM vanadyl sulfate.