共 40 条
Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q
被引:98
作者:

Jin, WL
论文数: 0 引用数: 0
h-index: 0
机构:
Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA

Klem, AM
论文数: 0 引用数: 0
h-index: 0
机构:
Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA

Lewis, JH
论文数: 0 引用数: 0
h-index: 0
机构:
Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA

Lu, Z
论文数: 0 引用数: 0
h-index: 0
机构:
Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA
机构:
[1] Univ Penn, Dept Physiol, Philadelphia, PA 19104 USA
关键词:
D O I:
10.1021/bi991206j
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
Tertiapin-Q (TPNQ) is a derivative of honey bee toxin tertiapin (TPN) whose methionine residue is replaced with a glutamine residue. TPNQ inhibits the ROMK1 and GIRK1/4 inward-rectifier K+ channels with affinities very similar to TPN. However, unlike native TPN, TPNQ is nonoxidizable by air. The stability of TPNQ allows us to investigate how it interacts with the targeted channels. We found that the interaction between TPNQ and the ROMK1 channel is a bimolecular reaction, i.e., one TPNQ molecule binds to one channel. The interaction surface in TPNQ is primarily formed by its alpha helix rather than the beta sheets with which scorpion toxins form their interaction surface. The mutagenesis studies on both the channel and TPNQ together strongly suggest that to block the K+ pore TPNQ plugs its alpha helix into the vestibule of the K+ pore, while leaving the extended structural portion sticking out of the Vestibule into the extracellular media.
引用
收藏
页码:14294 / 14301
页数:8
相关论文
共 40 条
[1]
TOPOLOGY OF THE PORE-REGION OF A K+ CHANNEL REVEALED BY THE NMR-DERIVED STRUCTURES OF SCORPION TOXINS
[J].
AIYAR, J
;
WITHKA, JM
;
RIZZI, JP
;
SINGLETON, DH
;
ANDREWS, GC
;
LIN, W
;
BOYD, J
;
HANSON, DC
;
SIMON, M
;
DETHLEFS, B
;
LEE, CL
;
HALL, JE
;
GUTMAN, GA
;
CHANDY, KG
.
NEURON,
1995, 15 (05)
:1169-1181

AIYAR, J
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

WITHKA, JM
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

RIZZI, JP
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

SINGLETON, DH
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

ANDREWS, GC
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

LIN, W
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

BOYD, J
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

HANSON, DC
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

SIMON, M
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

DETHLEFS, B
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

LEE, CL
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

HALL, JE
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

GUTMAN, GA
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA

CHANDY, KG
论文数: 0 引用数: 0
h-index: 0
机构: UNIV CALIF IRVINE, DEPT MICROBIOL & MOLEC GENET, IRVINE, CA 92717 USA
[2]
SINGLE APAMIN-BLOCKED CA-ACTIVATED K+ CHANNELS OF SMALL CONDUCTANCE IN CULTURED RAT SKELETAL-MUSCLE
[J].
BLATZ, AL
;
MAGLEBY, KL
.
NATURE,
1986, 323 (6090)
:718-720

BLATZ, AL
论文数: 0 引用数: 0
h-index: 0

MAGLEBY, KL
论文数: 0 引用数: 0
h-index: 0
[3]
ANALYSIS OF SIDE-CHAIN ORGANIZATION ON A REFINED MODEL OF CHARYBDOTOXIN - STRUCTURAL AND FUNCTIONAL IMPLICATIONS
[J].
BONTEMS, F
;
GILQUIN, B
;
ROUMESTAND, C
;
MENEZ, A
;
TOMA, F
.
BIOCHEMISTRY,
1992, 31 (34)
:7756-7764

BONTEMS, F
论文数: 0 引用数: 0
h-index: 0
机构:
CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE

GILQUIN, B
论文数: 0 引用数: 0
h-index: 0
机构:
CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE

ROUMESTAND, C
论文数: 0 引用数: 0
h-index: 0
机构:
CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE

MENEZ, A
论文数: 0 引用数: 0
h-index: 0
机构:
CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE

TOMA, F
论文数: 0 引用数: 0
h-index: 0
机构:
CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE CE SACLAY, DEPT INGN & ETUD PROT, STRUCT PROT SOLUT LAB, F-91191 GIF SUR YVETTE, FRANCE
[4]
A HOT-SPOT OF BINDING-ENERGY IN A HORMONE-RECEPTOR INTERFACE
[J].
CLACKSON, T
;
WELLS, JA
.
SCIENCE,
1995, 267 (5196)
:383-386

CLACKSON, T
论文数: 0 引用数: 0
h-index: 0
机构:
GENENTECH INC, DEPT PROT ENGN, S SAN FRANCISCO, CA 94080 USA GENENTECH INC, DEPT PROT ENGN, S SAN FRANCISCO, CA 94080 USA

WELLS, JA
论文数: 0 引用数: 0
h-index: 0
机构:
GENENTECH INC, DEPT PROT ENGN, S SAN FRANCISCO, CA 94080 USA GENENTECH INC, DEPT PROT ENGN, S SAN FRANCISCO, CA 94080 USA
[5]
The structure of the potassium channel:: Molecular basis of K+ conduction and selectivity
[J].
Doyle, DA
;
Cabral, JM
;
Pfuetzner, RA
;
Kuo, AL
;
Gulbis, JM
;
Cohen, SL
;
Chait, BT
;
MacKinnon, R
.
SCIENCE,
1998, 280 (5360)
:69-77

Doyle, DA
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

Cabral, JM
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

Pfuetzner, RA
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

Kuo, AL
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

Gulbis, JM
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

Cohen, SL
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

Chait, BT
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA

MacKinnon, R
论文数: 0 引用数: 0
h-index: 0
机构: Rockefeller Univ, Lab Mol Neurobiol & Biophys, New York, NY 10021 USA
[6]
PEPTIDE COMPONENTS OF BEE VENOM
[J].
GAULDIE, J
;
HANSON, JM
;
RUMJANEK, FD
;
SHIPOLINI, RA
;
VERNON, CA
.
EUROPEAN JOURNAL OF BIOCHEMISTRY,
1976, 61 (02)
:369-376

GAULDIE, J
论文数: 0 引用数: 0
h-index: 0
机构:
UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND

HANSON, JM
论文数: 0 引用数: 0
h-index: 0
机构:
UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND

RUMJANEK, FD
论文数: 0 引用数: 0
h-index: 0
机构:
UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND

SHIPOLINI, RA
论文数: 0 引用数: 0
h-index: 0
机构:
UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND

VERNON, CA
论文数: 0 引用数: 0
h-index: 0
机构:
UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND UCL, DEPT CHEM, CHRISTOPHER INGOLD LABS, 20 GORDON ST, LONDON WC1H OAJ, ENGLAND
[7]
MECHANISM OF IBERIOTOXIN BLOCK OF THE LARGE-CONDUCTANCE CALCIUM-ACTIVATED POTASSIUM CHANNEL FROM BOVINE AORTIC SMOOTH-MUSCLE
[J].
GIANGIACOMO, KM
;
GARCIA, ML
;
MCMANUS, OB
.
BIOCHEMISTRY,
1992, 31 (29)
:6719-6727

GIANGIACOMO, KM
论文数: 0 引用数: 0
h-index: 0
机构:
MERCK INST THERAPEUT RES,DEPT MEMBRANE BIOCHEM & BIOPHYS,POB 2000,RAHWAY,NJ 07065 MERCK INST THERAPEUT RES,DEPT MEMBRANE BIOCHEM & BIOPHYS,POB 2000,RAHWAY,NJ 07065

GARCIA, ML
论文数: 0 引用数: 0
h-index: 0
机构:
MERCK INST THERAPEUT RES,DEPT MEMBRANE BIOCHEM & BIOPHYS,POB 2000,RAHWAY,NJ 07065 MERCK INST THERAPEUT RES,DEPT MEMBRANE BIOCHEM & BIOPHYS,POB 2000,RAHWAY,NJ 07065

MCMANUS, OB
论文数: 0 引用数: 0
h-index: 0
机构:
MERCK INST THERAPEUT RES,DEPT MEMBRANE BIOCHEM & BIOPHYS,POB 2000,RAHWAY,NJ 07065 MERCK INST THERAPEUT RES,DEPT MEMBRANE BIOCHEM & BIOPHYS,POB 2000,RAHWAY,NJ 07065
[8]
THE CHARYBDOTOXIN RECEPTOR OF A SHAKER K+ CHANNEL - PEPTIDE AND CHANNEL RESIDUES MEDIATING MOLECULAR RECOGNITION
[J].
GOLDSTEIN, SAN
;
PHEASANT, DJ
;
MILLER, C
.
NEURON,
1994, 12 (06)
:1377-1388

GOLDSTEIN, SAN
论文数: 0 引用数: 0
h-index: 0
机构:
BRANDEIS UNIV,HOWARD HUGHES MED INST,GRAD DEPT BIOCHEM,WALTHAM,MA 02254 BRANDEIS UNIV,HOWARD HUGHES MED INST,GRAD DEPT BIOCHEM,WALTHAM,MA 02254

PHEASANT, DJ
论文数: 0 引用数: 0
h-index: 0
机构:
BRANDEIS UNIV,HOWARD HUGHES MED INST,GRAD DEPT BIOCHEM,WALTHAM,MA 02254 BRANDEIS UNIV,HOWARD HUGHES MED INST,GRAD DEPT BIOCHEM,WALTHAM,MA 02254

MILLER, C
论文数: 0 引用数: 0
h-index: 0
机构:
BRANDEIS UNIV,HOWARD HUGHES MED INST,GRAD DEPT BIOCHEM,WALTHAM,MA 02254 BRANDEIS UNIV,HOWARD HUGHES MED INST,GRAD DEPT BIOCHEM,WALTHAM,MA 02254
[9]
Agitoxin footprinting the Shaker potassium channel pore
[J].
Gross, A
;
MacKinnon, R
.
NEURON,
1996, 16 (02)
:399-406

Gross, A
论文数: 0 引用数: 0
h-index: 0
机构: Department of Neurobiology, Harvard Medical School, Boston

MacKinnon, R
论文数: 0 引用数: 0
h-index: 0
机构: Department of Neurobiology, Harvard Medical School, Boston
[10]
TRANSFER OF THE SCORPION TOXIN RECEPTOR TO AN INSENSITIVE POTASSIUM CHANNEL
[J].
GROSS, A
;
ABRAMSON, T
;
MACKINNON, R
.
NEURON,
1994, 13 (04)
:961-966

GROSS, A
论文数: 0 引用数: 0
h-index: 0
机构: Department of Neurobiology Harvard Medical School Boston

ABRAMSON, T
论文数: 0 引用数: 0
h-index: 0
机构: Department of Neurobiology Harvard Medical School Boston

MACKINNON, R
论文数: 0 引用数: 0
h-index: 0
机构: Department of Neurobiology Harvard Medical School Boston