Search Results - "Haviv, Fortuna"
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1
Preclinical Evaluation of Antiangiogenic Thrombospondin-1 Peptide Mimetics, ABT-526 and ABT-510, in Companion Dogs with Naturally Occurring Cancers
Published in Clinical cancer research (15-12-2006)“…Purpose: The angiogenic phenotype of malignant cancers has been established as a target for cancer therapy. ABT-526 and ABT-510, two peptide mimetics of…”
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2
Thrombospondin-1 Mimetic Peptide Inhibitors of Angiogenesis and Tumor Growth: Design, Synthesis, and Optimization of Pharmacokinetics and Biological Activities
Published in Journal of medicinal chemistry (21-04-2005)“…The heptapeptide 1, NAc-Gly-Val-DIle-Thr-Arg-Ile-ArgNHEt, a structurally modified fragment derived from the second type-1 repeat of thrombospondin-1 (TSP-1),…”
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3
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists
Published in Journal of medicinal chemistry (01-02-1993)“…Each peptide bond in leuprolide (1), deslorelin (13), and nafarelin (24) was separately substituted with N-methyl. The synthesized compounds were tested for in…”
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4
Inhibition of tumor growth by systemic treatment with thrombospondin‐1 peptide mimetics
Published in International journal of cancer (10-04-2002)“…Many normal human cells produce thrombospondin‐1 (TSP‐1), a potent antiangiogenic protein that promotes vascular quiescence. In various organ systems,…”
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5
Refolding of misfolded mutant GPCR: Post-translational pharmacoperone action in vitro
Published in Molecular and cellular endocrinology (30-06-2007)“…All reported GnRH receptor mutants (causing human hypogonadotropic hypogonadism) are misfolded proteins that cannot traffic to the plasma membrane…”
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6
In vitro and in vivo Activities of Reduced-Size Antagonists of Luteinizing Hormone-Releasing Hormone
Published in Journal of medicinal chemistry (01-03-1994)“…A novel series of octapeptide LHRH antagonists was designed on the basis of the structure of the (2-9) fragment of a LHRH agonist. By adopting a systematic SAR…”
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7
Structural requirements for the inhibition of 5-lipoxygenase by 15-hydroxyeicosa-5,8,11,13-tetraenoic acid analogs
Published in Journal of medicinal chemistry (01-02-1987)“…The structural requirements for inhibition of RBL-1 (rat basophilic leukemia) 5-lipoxygenase by 15-hydroxyeicosa-5,8,11,13-tetraenoic acid (15-HETE, 1) were…”
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8
Nonpeptide Luteinizing Hormone-Releasing Hormone Antagonists Derived from Erythromycin A: Design, Synthesis, and Biological Activity of Cladinose Replacement Analogues
Published in Journal of medicinal chemistry (26-02-2004)“…The design and synthesis of a series of 11,12-cyclic carbamate derivatives of 6-O-methylerythromycin A that are novel, nonpeptide LHRH antagonists, is…”
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9
Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A
Published in Bioorganic & medicinal chemistry letters (22-03-2004)“…Antibacterial SAR for a series of macrolides derived from erythromycin A that are potent LHRH antagonists was developed in an attempt to eliminate the…”
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10
Condensations of 4-methyl-4-dichloromethyl-2,5-cyclohexadienone
Published in Journal of the American Chemical Society (01-04-1969)Get full text
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11
3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation
Published in Journal of medicinal chemistry (01-09-1988)“…3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural…”
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12
Pharmacological and endocrine characterization of A-198401, an orally active GnRH antagonist, in intact and castrate male rat models
Published in Drug development research (01-03-2001)“…Gonadotropin‐releasing hormone (GnRH) stimulates the synthesis and secretion of the gonadotropins that maintain the reproductive axis in mammals. Efforts have…”
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13
Differential orientation of a GnRH agonist and antagonist in the pituitary GnRH receptor
Published in Endocrinology (Philadelphia) (01-08-1993)“…In the present study we have used a high affinity photoaffinity label (PAL) agonist (pGlu-His-Trp-Ser-125I-iodoTyr-D-Lys(para-N3-Benzoyl)-Leu-Arg-P roNHEt) and…”
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14
Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics
Published in Journal of medicinal chemistry (01-10-1992)“…To stabilize leuprolide (1) against chymotrypsin and intestinal degradation several agonists of LHRH (2-12), modified at position 1, 2, or 3 and/or containing…”
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15
Active reduced-size hexapeptide analogs of luteinizing hormone-releasing hormone
Published in Journal of medicinal chemistry (01-10-1989)“…A series of reduced-size hexapeptide analogues of LH-RH were synthesized that contain the residues corresponding to amino acid positions 4-9 and are linked to…”
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16
The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists
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17
Inhibitors of immune complex-induced inflammation: 3-[1-(2-benzoxazolyl)hydrazino]propanenitrile derivatives
Published in Journal of pharmaceutical sciences (01-06-1989)“…The octanol-water partition coefficients (log P) and the dissociation constants (pKa) of 3-[1-(2-benzoxazolyl)hydrazino]propanenitrile analogues have been…”
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18
Inhibitors of immune complex-induced inflammation: 5-substituted 3-[1-(2-benzoxazolyl)hydrazino]propanenitrile derivatives
Published in Journal of pharmaceutical sciences (01-08-1990)“…A number of 5-substituted 3-[1-(2-benzoxazolyl)hydrazino]propanenitrile analogues have been studied as inhibitors of the rat pleural reverse passive Arthus…”
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19
Transformations of 1-methyl-1-(dichloromethyl)cyclohexane derivatives
Published in Journal of organic chemistry (01-06-1970)Get full text
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20
2-[(Phenylthio)methyl]pyridine derivatives: new antiinflammatory agents
Published in Journal of medicinal chemistry (01-02-1983)“…2-[(Phenylthio)methyl]pyridine derivatives inhibited the dermal reverse passive Arthus reaction (RPAR) in the rat. In the same model, indomethacin was…”
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