PHAGE INFECTION STRUCT OF G3P IN COMPLEX W/ CORECEPTOR, C TERMINAL DOMAIN
PHAGE INFECTION STRUCT OF G3P IN COMPLEX W/ CORECEPTOR, C TERMINAL DOMAIN
批准号:
6205776
负责人:
ALEX WLODAWER
金额:
$0.0万
依托单位国家:
美国
项目类别:
财政年份:
1999
资助国家:
美国
项目状态:
已结题
起止时间:
1999-09-01 至 2000-08-31
中文摘要
史蒂文·阿尔莫博士,一位X射线结晶学家
同步加速器体验,引领了一项合作努力
与酶学家张忠银博士和大卫博士合作
劳伦斯,一位合成化学家。这个项目的目标是
基于结构的潜在治疗剂的设计
蛋白酪氨酸磷酸酶(PTPase)的研究进展
新型PTPase的结构。由于在旋转阳极上收集的数据
AECOM的震源分辨率不够高,为单晶
在光束线X9B收集的衍射数据绝对是
对当前的进步至关重要。H使用同步加速器方法,Dr。
Almo的团队已经解决了人类蛋白质酪氨酸的结构问题
几种不同底物的复合体中的磷酸酶1B(PTP1B),
使用在X9B收集的1.9A数据。PTP1B与a的络合物
合成法合成高亲和力非肽H底物
劳伦斯小组证明了一种新的芳基的存在
磷酸结合位点,为设计提供了一个新的H范式
紧密结合的抑制剂。这是报道的最高分辨率
这项工作最近发表在了
美国国家航空航天局。基于这些发现,劳伦斯实验室合成了一种
系列第二代双芳基PTP1B配体
磷酸盐官能团和数据已于
几个不同的复合体。
英文摘要
Dr. Steven Almo, an x-ray crystallographer with significant
synchrotron experience, has spearheaded a collaborative effort in
conjunction with Dr. Zhong-Yin Zhang, an enzymologist, and Dr. David
Lawrence, a synthetic chemist. The goal of this project is the
structure-based design of potential therapeutic agents which bind to
protein tyrosine phosphatases (PTPases), and the elucidation of the
structures of novel PTPases. Since data collected on rotating anode
sources at AECOM were of insufficient resolution, single-crystal
diffraction data collected at beamline X9B has been absolutely
essential for current progress. H Using synchrotron methods, Dr.
Almo's group has solved the Hstructure of human protein tyrosine
phosphatase 1B (PTP1B) in complex Hwith several different substrates,
using 1.9A data collected at X9B. HThe complex of PTP1B and a
synthetic high-affinity non-peptide Hsubstrate synthesized by the
Lawrence group has demonstrated the Hexistence of a novel aryl
phosphate binding site, which provides a new Hparadigm for the design
of tight-binding inhibitors. This is the Hhighest resolution reported
for this enzyme and this work has recently Hled to a publication in
PNAS. Based on these findings, the Lawrence Hlab has synthesized a
series second generation of PTP1B ligands that Hencompass both aryl
phosphate functionalities and data has been Hcollected at X-9B on
several different complexes.
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会议论文
DECAMERS OBSERVED IN CRYSTAL OF BOVINE PANCREATIC TRYPSIN INHIBITOR
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批准号:6205777
-
项目类别:
-
资助金额:$0.0万
-
财政年份:1999
-
负责人:ALEX WLODAWER
-
依托单位:
CHEM SYNTH & HIGH RES CRYSTAL STRUCT OF POTENT ANTI HIV PROTEIN AOP RANTES
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批准号:6205778
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项目类别:
-
资助金额:$0.0万
-
财政年份:1999
-
负责人:ALEX WLODAWER
-
依托单位:
RNASE-INHIBITOR X-RAY CRYSTAL STRUCTURE
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批准号:6307523
-
项目类别:
-
资助金额:$0.82万
-
财政年份:1999
-
负责人:ALEX WLODAWER
-
依托单位:
SYNCHROTRON CRYSTALLOGRAPHY OF RANTES
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批准号:6120418
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项目类别:
-
资助金额:$0.0万
-
财政年份:1998
-
负责人:ALEX WLODAWER
-
依托单位:
STRUCTURE FUNCTION OF CATALYTIC DOMAIN OF AVIAN SARCOMA VIRUS INTEGRASE: HIV
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批准号:6120416
-
项目类别:
-
资助金额:$0.34万
-
财政年份:1998
-
负责人:ALEX WLODAWER
-
依托单位:
SYNCHROTRON CRYSTALLOGRAPHY OF RNA 3 TERMINAL PHOSPHATE CYCLASE
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批准号:6120417
-
项目类别:
-
资助金额:$0.0万
-
财政年份:1998
-
负责人:ALEX WLODAWER
-
依托单位:
RNASE-INHIBITOR X-RAY CRYSTAL STRUCTURE
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批准号:6279550
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项目类别:
-
资助金额:$0.59万
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财政年份:1997
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负责人:ALEX WLODAWER
-
依托单位:
PROTEIN STRUCTURE
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批准号:6422155
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项目类别:
-
资助金额:$0.0万
-
财政年份:--
-
负责人:ALEX WLODAWER
-
依托单位:
Protein Structure
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批准号:6763645
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项目类别:
-
资助金额:$0.0万
-
财政年份:--
-
负责人:ALEX WLODAWER
-
依托单位:
Protein Structure
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批准号:6559232
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项目类别:
-
资助金额:$0.0万
-
财政年份:--
-
负责人:ALEX WLODAWER
-
依托单位:
海外基金