US6054047A
Expired / Lapsed
US
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Apparatus for screening compound libraries
Assignee: Synsorb Biotech Inc
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Filing: 1998-04-29
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Granted: 2000-04-25
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Expires: 2018-04-29
Abstract
Abstract Disclosed are apparatus for screening compound libraries using frontal chromatography in combination with mass spectrometry to identify and rank those members of the library that bind to a target receptor. The apparatus of this invention also permit a compound library to be rapidly screened to determine if any member of the library has a higher affinity for the target receptor relative to a pre-selected indicator compound.
Inventors
- 👤 Ole Hindsgaul
- 👤 David C. Schriemer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 02:43
CPC Classifications
G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/68; G01N33/6803; G01N33/6845; G01N30/00; G01N30/02; G01N30/26; G01N30/38; G01N30/46; G01N30/466; G01N30/62; G01N30/72; G01N30/7233; G01N30/724; G01N30/7266; G01N33/53; G01N33/536; G01N33/537; G01N33/538; G01N33/543; G01N33/54306; G01N33/54366; G01N33/6842; G01N33/6848; B; B01; B01J; B01J2219/00; B01J2219/00274; B01J2219/00583; B01J2219/00585; B01J2219/0068; B01J2219/00702; B01J2219/00704; B01J2219/00707; B01J2219/00718; B01J2219/0072; B01J2219/00731; B01J2219/00738; B01J2219/00745; B01J2219/00747; C; C40; C40B; C40B30/00; C40B30/08; C40B40/00; C40B40/04; C40B40/12; C40B40/18; G01N2030/628; H; H01; H01J; H01J49/00
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
157 words
An apparatus for screening a plurality of compound libraries to determine the relative or absolute affinity of a plurality of putative ligands in each library to a target receptor, which apparatus comprises: (a) a plurality of columns each comprising a target receptor optionally attached to a solid phase support and each having a inflow end and an outflow end, wherein each of said columns is capable of independently having a compound library comprising a plurality of putative ligands continuously applied thereto under frontal chromatography conditions whereby the target ligand is continuously contacted with the compound library to produce an effluent from the outflow end of the column; (b) a plurality of first reservoirs each connected to the inflow end of one of the columns for continuously applying a compound library to the columns; (c) a mass spectrometer connected to the outflow end of each of said columns for intermittently analyzing the effluent from each of the column.
Claim 2
Independent Claim
157 words
An apparatus for screening a plurality of compound libraries to determine the relative or absolute affinity of a plurality of putative ligands in each library to a target receptor, which apparatus comprises: (a) a plurality of columns each comprising a target receptor optionally attached to a solid phase support and each having a inflow end and an outflow end, wherein each of said columns is capable of independently having a compound library comprising a plurality of putative ligands continuously applied thereto under frontal chromatography conditions whereby the target ligand is continuously contacted with the compound library to produce an effluent from the outflow end of the column; (b) a plurality of first reservoirs each connected to the inflow end of one of the columns for continuously applying a compound library to the columns; (c) a mass spectrometer connected to the outflow end of each of said columns for intermittently analyzing the effluent from each of the column.
Claim 3
Dependent Claim
57 words
The apparatus of claim 1, wherein said apparatus further comprises: (d) a plurality of second reservoirs each connected to the inflow end of one of the columns for applying either (i) a mixture comprising the compound library and one or more indicator compounds, (ii) one or more indicator compounds, or (iii) a buffer solution to the column.
Claim 4
Dependent Claim
41 words
The apparatus of claim 1, wherein said apparatus further comprises: (e) a third reservoir connected to the outflow end of each of the columns for supplying a supplemental diluent to the effluent from each column before analysis by the mass spectrometer.
Claim 5
Dependent Claim
15 words
The apparatus of claim 1, wherein said apparatus comprises from 2 to about 100 columns.
Claim 6
Dependent Claim
15 words
The apparatus of claim 4, wherein said apparatus comprises from 3 to about 50 columns.
Claim 7
Dependent Claim
15 words
The apparatus of claim 5, wherein said apparatus comprises from 5 to about 10 columns.
Claim 8
Dependent Claim
28 words
The apparatus of claim 4, wherein each column is intermittently monitored for a period of about 0.5 seconds to about 10 seconds before switching to the next column.
Claim 9
Dependent Claim
25 words
The apparatus of claim 7, wherein each column is intermittently monitored for about 1 second to about 5 seconds before switching to the next column.
Claim 10
Dependent Claim
21 words
The apparatus of claim 1, wherein the column has an internal diameter ranging from about 10 μm to about 4.6 mm.
Claim 11
Dependent Claim
21 words
The apparatus of claim 9, wherein the column has an internal diameter of from about 100 μm to about 250 μm.
Claim 12
Dependent Claim
20 words
The apparatus of claim 1, wherein the column has a length of from about 1 cm to about 30 cm.
Claim 13
Dependent Claim
20 words
The apparatus of claim 1, wherein the column has a length of from about 2 cm to about 20 cm.
Claim 14
Dependent Claim
68 words
The apparatus of claim 1, wherein the target receptor is selected from the group consisting of proteins, glycoproteins, glycosaminoglycans, proteoglycans, integrins, enzymes, lectins, selecting, cell-adhesion molecules, toxins, bacterial pili, transport proteins, receptors involved in signal transduction or hormone-binding, hormones, antibodies, major histocompatability complexes, immunoglobulin superfamilies, cadherins, DNA or DNA fragments, RNA and RNA fragments, whole cells, tissues, bacteria, fungi, viruses, parasites, preons, and synthetic analogs or derivatives thereof.
Claim 15
Dependent Claim
16 words
The apparatus of claim 1, wherin the target receptor is bound to a solid phase support.
Claim 16
Dependent Claim
24 words
The apparatus of claim 14, wherein the target receptor is covalently bound to the solid phase support or bound via biotin-avidin or biotin-streptavidin binding.
Claim 17
Dependent Claim
27 words
The apparatus of claim 14, wherein the solid phase support is selected from the group consisting of resin beads, glass beads, silica chips, silica capillaries and agarose.
Claim 18
Dependent Claim
22 words
The apparatus of claim 1, wherein the column contains from about 1 pmol to about 10 nmol of target receptor active sites.
Claim 19
Dependent Claim
14 words
The apparatus of claim 1, wherein the mass spectrometer is an electrospray mass spectrometer.
References Cited (Backward Citations)
US5106756A
Cited
US4842701A
Cited
US4869093A
Cited
US5561046A
Cited
US4970085A
Cited
US5646046A
Cited
US5481476A
Cited
JPH06500396A
Cited
WO1992002815A2
Cited
JPH06201650A
Cited
US5503805A
Cited
WO1995025737A1
Cited
JPH10500951A
Cited
WO1995032425A1
Cited
WO1996032642A1
Cited
JPH09101306A
Cited
EP0742438A2
Cited
WO1997043641A1
Cited
WO1997043301A2
Cited
US5792431A
Cited
US5917185A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 2003-04-25 | 2003-10-25 | 2004-04-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2007-04-25 | 2007-10-25 | 2008-04-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2011-04-25 | 2011-10-25 | 2012-04-25 | $7700.00 | Window Closed / Lapsed |