Abstract: Biotinylation peptides can be fused to other peptides or proteins of interest using recombinant DNA techniques to provide efficient methods for biotinylating the resulting fusion proteins in vivo or in vitro.
Abstract: Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
Type:
Grant
Filed:
May 19, 1998
Date of Patent:
July 27, 1999
Assignee:
Affymax Technologies N.V.
Inventors:
David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
Abstract: Improved methods and novel compositions for identifying peptides and single-chain antibodies that bind to predetermined receptors or epitopes. Such peptides and antibodies are identified by improved and novel methods for affinity screening of polysomes displaying nascent peptides.
Abstract: Novel compounds are provided which are useful as photocleavable linking groups in solid phase synthesis. Compositions incorporating these linking groups and methods for their use are also described.
Abstract: Peptides that bind to the interleukin-1 type I receptor (IL-1RtI) can be used to assay the amount of IL-1R, or an IL-1R agonist or antagonist, in a sample and comprise a sequence of amino acids selected from the group consisting of (1) WXXXGZ.sub.1 W where Z.sub.1 is L, I, A, or Q (SEQ ID NO:2); (2) XXQZ.sub.5 YZ.sub.6 XX where Z.sub.5 is P or Aze where Aze is azetidine; and Z.sub.6 is S, A, V, or L (SEQ ID NO:1); and (3) Z.sub.23 NZ.sub.24 SZ.sub.25 Z.sub.26 Z.sub.27 Z.sub.28 Z.sub.29 Z.sub.30 L where Z.sub.23 is D or Y; Z.sub.24 is D or S; Z.sub.25 is S or W; Z.sub.26 is S or Y; Z.sub.27 is D or V; Z.sub.28 is S or W; Z.sub.29 is F or L; and Z.sub.30 is D or L (SEQ ID NO:27); and where each amino acid is indicated by standard one letter abbreviation; and each X can be selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids.
Abstract: Disclosed are methods for synthesizing very large collections of diverse diverse tetramic acids, tetronic acids, pentamic acids, pentonic acids, and derivatives thereof and synthetic compound libraries comprising compounds prepared by such methods.
Abstract: Biotinylation peptides can be fused to other peptides or proteins of interest using recombinant DNA techniques to provide efficient methods for biotinylating the resulting fusion proteins in vivo or in vitro.
Abstract: Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.
Type:
Grant
Filed:
December 11, 1996
Date of Patent:
February 9, 1999
Assignee:
Glaxo Group Limited
Inventors:
William J. Dower, Ronald W. Barrett, Steven E. Cwirla, Christian M. Gates, Peter J. Schatz, Palaniappan Balasubramanian, Christopher R. Wagstrom, Richard Wayne Hendren, Randoph B. DePrince, Surekha Podduturi, Qun Yin
Abstract: The invention provides systems and methods for synthesizing various compounds on solid support. According to one exemplary method, a synthesizer is provided having at least one reaction vessel block with a plurality of reaction vessels therein. At least one solid support is introduced into a least some of the reaction vessels, and a reagent is introduced into the reaction vessels having the solid supports. The reaction vessel block is then vibrated while heat is supplied to the reaction vessel block to heat the reaction vessels. Optionally, the synthesized compounds may be cleaved from the solid supports following synthesis while they remain within the reaction vessels.
Abstract: Peptides that bind to the interleukin-1 type I receptor (IL-1RtI) can be used to assay the amount of IL-1R, or an IL-1R agonist or antagonist, in a sample and comprise a sequence of amino acids selected from the group consisting of (1) WXXXGZ.sub.1 W where Z.sub.1 is L, I, A, or Q; (2) XXQZ.sub.5 YZ.sub.6 XX where Z.sub.5 is P or Aze where Aze is azetidine; and Z.sub.6 is S, A, V, or L; and (3) Z.sub.23 NZ.sub.24 SZ.sub.25 Z.sub.26 Z.sub.27 Z.sub.28 Z.sub.29 Z.sub.30 L where Z.sub.23 is D or Y; Z.sub.24 is D or S; Z.sub.25 is S or W; Z.sub.26 is S or Y; Z.sub.27 is D or V; Z.sub.28 is S or W; Z.sub.29 is F or L; and Z.sub.30 is D or L; and where each amino acid is indicated by standard one letter abbreviation; and each X can be selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids. Also provided are peptides which bind to the IL-1RtI, which are 11 to 40 amino acids in length, which comprise the core sequence of amino acids:Z.sub.31 XWZ.sub.32 Z.sub.33 Z.sub.34 Z.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
January 19, 1999
Assignees:
Affymax Technologies N.V., Hoechst Marion Roussel, Inc.
Inventors:
Ronald W. Barrett, Stephen D. Yanofsky, David Baldwin, Jeff W. Jacobs, Phillipe R. Bovy, Ellen M. Leahy, Richard S. Pottorf
Abstract: Disclosed are chemical encryption methods for determining the structure of compounds formed in situ on solid supports by the use of specific amines tags which, after compound synthesis, can be deencrypted to provide the structure of the compound found on the support.
Type:
Grant
Filed:
December 22, 1995
Date of Patent:
December 8, 1998
Assignee:
Glaxo Group Limited
Inventors:
Mark A. Gallop, Eric Gordon, Zhi-Jie Ni, Derek MacLean, Christopher Holmes, William Fitch, Nikhil Shah
Abstract: Disclosed are novel inhibitors of collagenase-1 and stromelysin-I metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
Type:
Grant
Filed:
October 27, 1995
Date of Patent:
November 24, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
Abstract: Peptides of 10 to 40 or more amino acid residues in length and having the sequence X.sub.3 X.sub.4 X.sub.5 GPX.sub.6 TWX.sub.7 X.sub.8 (SEQ ID NO:252) where each amino acid is indicated by standard one letter abbreviation; X.sub.3 is C; X.sub.4 is R, H, L, or W; X.sub.5 is M, F, or I; X.sub.6 is independently selected from any one of the 20 genetically coded L-amino acids; X.sub.7 is D, E, I, L, or V; and X.sub.8 is C, which bind and activate the erythropoietin receptor (EPO-R) or otherwise act as an EPO agonist, and methods for their use.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
November 3, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
Nicholas C. Wrighton, William J. Dower, Ray S. Chang, Arun K. Kashyap
Abstract: Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
Type:
Grant
Filed:
October 27, 1995
Date of Patent:
November 3, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
David A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
Abstract: The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
Type:
Grant
Filed:
October 11, 1996
Date of Patent:
October 6, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
Anna Katrin Szardenings, David Campbell
Abstract: PTH analogs comprising an amino acid sequence that is: SVSEIQLLHNX.sub.1 X.sub.2 X.sub.3 HX.sub.4 X.sub.3 X.sub.3 X.sub.3 X.sub.5 RVX.sub.5 WLR X.sub.4 X.sub.4 LX.sub.3 X.sub.3 VX.sub.1 X.sub.3 X.sub.3 X (SEQ ID NO:10) wherein X.sub.1 is a neutral or positively charged amino acid, X.sub.2 is a neutral amino acid, X.sub.3 is a neutral, positively charged, or negatively charged amino acid, X.sub.4 is a positively charged amino acid, X.sub.5 is a positively charged or negatively charged amino acid, and X is selected from the group consisting of Hol, Ho, a homoserine amide, or the sequence of amino acids comprising residues 35-84 of PTH, have enhanced activity and increased serum half-life as compared with human PTH. The PTH analogs can be produced as fusion proteins in high yields in E. coli host cells; the fusion proteins can be subsequently cleaved to produce the PTH analog.
Abstract: A general stochastic method for synthesizing random oligomers on particles is disclosed. A further aspect of the invention relates to the use of identification tags on the particles to facilitate identification of the sequence of the monomers in the oligomer.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 4, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
William J. Dower, Ronald W. Barrett, Mark A. Gallop
Abstract: Peptides that bind to the interleukin-1 type I receptor (IL-1RtI) can be used to assay the amount of IL-1R, or an IL-1R agonist or antagonist, in a sample and comprise a sequence of amino acids selected from the group consisting of (1) WXXXGZ.sub.1 W where Z.sub.1 is L, I, A, or Q; (2) XXQZ.sub.5 YZ.sub.6 XX where Z.sub.5 is P or Aze where Aze is azetidine; and Z.sub.6 is S, A, V, or L; and (3) Z.sub.23 NZ.sub.24 SZ.sub.25 Z.sub.26 Z.sub.27 Z.sub.28 Z.sub.29 Z.sub.30 L where Z.sub.23 is D or Y; Z.sub.24 is D or S; Z.sub.25 is S or W; Z.sub.26 is S or Y; Z.sub.27 is D or V; Z.sub.28 is S or W; Z.sub.29 is F or L; and Z.sub.30 is D or L; and where each amino acid is indicated by standard one letter abbreviation; and each X can be selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids. Also provided are peptides which bind to the IL-1RtI, which are 11 to 40 amino acids in length, which comprise the core sequence of amino acids:Z.sub.31 XWZ.sub.32 Z.sub.33 Z.sub.34 Z.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
July 28, 1998
Assignees:
Affymax Technologies N.V., Hoechst Marion Roussel, Inc.
Inventors:
Ronald W. Barrett, Stephen D. Yanofsky, David Baldwin, Jeff W. Jacobs, Phillipe R. Bovy, Ellen M. Leahy, Richard S. Pottorf
Abstract: Disclosed are peptides and peptide mimetics that bind selectins, including endothelial leukocyte adhesion molecule 1 (ELAM-1). Such peptides and peptide mimetics are useful in methods for blocking adhesion of leukocytes to the selectins for the purpose of inhibiting inflammation as well as in diagnostic methods employing labeled peptides and peptide mimetics that bind selectins for the purpose of determining the site of inflammation in mammals which inflammation is mediated by the presence of one or more selectins.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
July 28, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
Ronald W. Barrett, Steven E. Cwirla, William J. Dower, Kerry J. Koller, Jung Lee, Christine L. Martens, Beatrice Ruhland-Fritsch
Abstract: Peptides of 10 to 40 or more amino acid residues in length and having the sequence X.sub.3 X.sub.4 X.sub.5 GPX.sub.6 TWX.sub.7 X.sub.8 (SEQ ID NO:252) where each amino acid is indicated by standard one letter abbreviation; X.sub.3 is C; X.sub.4 is R, H, L, or W; X.sub.5 is M, F, or I; X.sub.6 is independently selected from any one of the 20 genetically coded L-amino acids; X.sub.7 is D, E, I, L, or V; and X.sub.8 is C, which bind and activate the erythropoietin receptor (EPO-R) or otherwise act as an EPO agonist, and methods for their use.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
June 30, 1998
Assignee:
Affymax Technologies N.V.
Inventors:
Nicholas C. Wrighton, William J. Dower, Ray S. Chang, Arun K. Kashyap, Linda K. Jolliffe, Dana Johnson, Linda Mulcahy