WO2003014308A3 - Cysteine mutants and methods for detecting ligand binding to biological molecules - Google Patents

Cysteine mutants and methods for detecting ligand binding to biological molecules Download PDF

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Publication number
WO2003014308A3
WO2003014308A3 PCT/US2002/024921 US0224921W WO03014308A3 WO 2003014308 A3 WO2003014308 A3 WO 2003014308A3 US 0224921 W US0224921 W US 0224921W WO 03014308 A3 WO03014308 A3 WO 03014308A3
Authority
WO
WIPO (PCT)
Prior art keywords
tbms
methods
biological molecules
ligand binding
cysteine mutants
Prior art date
Application number
PCT/US2002/024921
Other languages
French (fr)
Other versions
WO2003014308A9 (en
WO2003014308A2 (en
Inventor
Robert S Mcdowell
W Michael Flanagan
Original Assignee
Sunesis Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US09/981,547 external-priority patent/US20020022233A1/en
Priority claimed from US09/990,421 external-priority patent/US6919178B2/en
Priority claimed from US10/121,216 external-priority patent/US6998233B2/en
Priority to IL15990002A priority Critical patent/IL159900A0/en
Priority to CA002454246A priority patent/CA2454246A1/en
Priority to NZ530721A priority patent/NZ530721A/en
Application filed by Sunesis Pharmaceuticals Inc filed Critical Sunesis Pharmaceuticals Inc
Priority to EP02761258A priority patent/EP1421379A2/en
Priority to MXPA04001000A priority patent/MXPA04001000A/en
Priority to JP2003519438A priority patent/JP2005503380A/en
Publication of WO2003014308A2 publication Critical patent/WO2003014308A2/en
Priority to ZA2004/00342A priority patent/ZA200400342B/en
Publication of WO2003014308A3 publication Critical patent/WO2003014308A3/en
Publication of WO2003014308A9 publication Critical patent/WO2003014308A9/en

Links

Classifications

    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803—General methods of protein analysis not limited to specific proteins or families of proteins
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value

Landscapes

  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Chemical & Material Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Physics & Mathematics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Microbiology (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Food Science & Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Peptides Or Proteins (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

The present invention relates generally to variants of target biological molecules ('TBMs') and to methods of making and using the same to identify ligands of TBMs. More specifically, the invention relates to individual variant TBMs and sets of variant TBMs, each of which represents a modified version of a protein of interest where a thiol has been introduced at or near a site of interest. Ligands of TBMs are identified in part through the formation of a covalent bond between a potential ligand and a reactive thiol on the TBM.
PCT/US2002/024921 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules WO2003014308A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
JP2003519438A JP2005503380A (en) 2001-08-07 2002-08-05 Methods for detecting cysteine variants and ligands that bind to biological molecules
MXPA04001000A MXPA04001000A (en) 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules.
EP02761258A EP1421379A2 (en) 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules
CA002454246A CA2454246A1 (en) 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules
NZ530721A NZ530721A (en) 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules
IL15990002A IL159900A0 (en) 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules
ZA2004/00342A ZA200400342B (en) 2001-08-07 2004-01-16 Cysteine mutants and methods for detecting ligand binding to biological molecules

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US31072501P 2001-08-07 2001-08-07
US60/310,725 2001-08-07
US09/981,547 2001-10-17
US09/981,547 US20020022233A1 (en) 1998-06-26 2001-10-17 Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
US09/990,421 US6919178B2 (en) 2000-11-21 2001-11-21 Extended tethering approach for rapid identification of ligands
US09/990,421 2001-11-21
US10/121,216 US6998233B2 (en) 1998-06-26 2002-04-10 Methods for ligand discovery
US10/121,216 2002-04-10

Publications (3)

Publication Number Publication Date
WO2003014308A2 WO2003014308A2 (en) 2003-02-20
WO2003014308A3 true WO2003014308A3 (en) 2004-03-18
WO2003014308A9 WO2003014308A9 (en) 2004-04-22

Family

ID=27494353

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/024921 WO2003014308A2 (en) 2001-08-07 2002-08-05 Cysteine mutants and methods for detecting ligand binding to biological molecules

Country Status (7)

Country Link
EP (1) EP1421379A2 (en)
JP (1) JP2005503380A (en)
CA (1) CA2454246A1 (en)
IL (1) IL159900A0 (en)
MX (1) MXPA04001000A (en)
NZ (1) NZ530721A (en)
WO (1) WO2003014308A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7214487B2 (en) 1998-06-26 2007-05-08 Sunesis Pharmaceuticals, Inc. Methods for identifying compounds that modulate enzymatic activities by employing covalently bonded target-extender complexes with ligand candidates
AU2003228345B2 (en) 2002-03-21 2009-02-05 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
WO2005034840A2 (en) * 2003-09-17 2005-04-21 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6010861A (en) * 1994-08-03 2000-01-04 Dgi Biotechnologies, Llc Target specific screens and their use for discovering small organic molecular pharmacophores
US6308145B1 (en) * 1992-03-27 2001-10-23 Akiko Itai Methods for searching stable docking models of biopolymer-ligand molecule complex

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6308145B1 (en) * 1992-03-27 2001-10-23 Akiko Itai Methods for searching stable docking models of biopolymer-ligand molecule complex
US6010861A (en) * 1994-08-03 2000-01-04 Dgi Biotechnologies, Llc Target specific screens and their use for discovering small organic molecular pharmacophores

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
HART ET AL.: "A missing link in cupredoxins: crystal structure of cucumber stellacyanin at 1.6 angstroms resolution", PROTEIN SCIENCE, vol. 5, 1996, pages 2175 - 2183, XP002964154 *
IPPOLITO ET AL.: "Structural consequences of redesigning a protein-Zinc binding site", BIOCHEMISTRY, vol. 33, 1994, pages 15241 - 15249, XP002964151 *
ISOGAI ET AL.: "Design and synthesis of a globin fold", BIOCHEMISTRY, vol. 38, 1999, pages 7431 - 7443, XP002964153 *
JI ET AL.: "A three-dimensional model of lanosterol 14 alpha-demethylase of candida albicans and its interaction with azole antifungals", JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, no. 13, 2000, pages 2493 - 2505, XP002964156 *
ROSEN ET AL.: "Molecular shape comparisons in searches for active sites and functional similarity", PROTEIN ENGINEERING, vol. 11, no. 4, 1998, pages 263 - 277, XP002964155 *
SUGIO ET AL.: "Crystal structure of human serum albumin at 2.5 angstroms resolution", PROTEIN ENGINEERING, vol. 12, no. 6, 1999, pages 439 - 446, XP002964157 *
WHERLAND ET AL.: "Three-dimensional model of stellacyanin and its implications for electron transfer reactivity", JOURNAL OF MOLECULAR BIOLOGY, vol. 204, 1988, pages 407 - 415, XP002964152 *

Also Published As

Publication number Publication date
CA2454246A1 (en) 2003-02-20
NZ530721A (en) 2006-09-29
WO2003014308A9 (en) 2004-04-22
IL159900A0 (en) 2004-06-20
EP1421379A2 (en) 2004-05-26
MXPA04001000A (en) 2004-06-25
WO2003014308A2 (en) 2003-02-20
JP2005503380A (en) 2005-02-03

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