糖类药物的研究现状及应用前景
合集下载
相关主题
- 1、下载文档前请自行甄别文档内容的完整性，平台不提供额外的编辑、内容补充、找答案等附加服务。
- 2、"仅部分预览"的文档,不可在线预览部分如存在完整性等问题,可反馈申请退款(可完整预览的文档不适用该条件!)。
- 3、如文档侵犯您的权益，请联系客服反馈,我们会尽快为您处理(人工客服工作时间：9:00-18:30)。
• Potentially faster track to market than using proteins as targets to develop small molecules
• Pharmaceutical companies initiating higher throughput protein screens
Antibodies
35
25
Proteins
15
12
Small Molecules
8
8
一、糖类药物的概念和特点
糖类药物定义 狭义的讲，糖类药物是指含有糖结构的化合物， 包括：寡糖、
ii) In 1930, Karl Landsteiner was awarded the Nobel Prize for this important discover !!
ABO human blood group antigens & antibodies
O
B
A
AB
Antigens On Cells
Growth Drivers
• Nearly half of all biopharmaceuticals in clinical development are therapeutic proteins or antibodies
• Numerous new lead agents for major therapeutic classes including cancer, inflammatory diseases, cardiovascular diseases, and infectious diseases
Revenue In Billions
Glycoprotein Market Growth
$80 $60 $40 $20 $0
Antibodie s Unglycosylated Proteins Glycopr ote ins
2000
2005
wk.baidu.com
2010
Estimated Growth Rates
2000-2005(%) 2005-2010(%)
Penicillin
iii) The chemical structure of penicillin was proved to β-Lactam structure by X-Ray in 1945;
iv) In 1945, A. Fleming, H. Florey and E. Chain shared the Nobel Prizes “for the discovery of penicillin and its curative effect in various infectious diseases “.
HO OH
HO
OO
O
O OH HO OH
Antibodies In Serum
Anti-A Anti-B
HO OH HO O HO OH
OH O O O O
O OH HOOH
Anti-A
HO OH
HO O HO OH
NHAc O
OO
O
O OH HO OH
Anti-B
A&B Antigens
ABO系统各种血型抗原的特异性是决定于糖蛋白上所含的糖链, 即H、A 和B糖抗原
Example 2: The discover of Penicillin
i) Penicillin was discovered by A. Fleming (UK) in 1928;
ii) In 1939, H. Florey and E. Chain successfully isolated Penicillin and investigated its bioactivity in 1940;
据统计，目前市售糖类药物约有500多种，其中主要以糖蛋白药物 为主；而且，在美国市场糖类药物的市场需求量以约50%逐年增高； 在全球市场率也以较高比例增长；
近年来，有关糖类药物的专著、研究文章、专利等也已数以万计， 基于糖分子的药物研究和开发成为实验室和药物公司企业的热点领域
Opportunity for Protein Therapeutics
E. Chain (UK)
H. Florey (AUS)
A. Fleming (UK)
The structure of peptidoglycan on the bacterial cell wall
Meroueh, S. O. et al.. PNAS 2006;103:4404-4409.
Peptidoglycan is a polymer consisting of sugars and amino acids that forms a mesh-like layer outside the plasma membrane of bacteria, forming the cell wall； The sugar part: β-(1,4) linked N-acetylglucosamine and N-acetylmuramic acid The peptide chain: three to five amino acids chain attached to the N-acetylmuramic acid
糖药物的发展历史
1963，从Canavalliaensiformis分离出的一种蛋白能够与红细胞上的 糖进行结合，糖作为药物概念开始出现；
1982年，第一个能与凝集素蛋白（Lectins）结合的动物糖类化合物 被分离、鉴定；
1980’s- 随着现代分析、分离技术的发展，基于糖类化合物的药物 分子得到飞速的发展；
The Role of Carbohydrates in Cell Surface Interactions
Example 1: ABO Blood Typing
Karl Landsteiner (1868-1943)
i) ABO blood types were discovered in 1900 and 1901 at the University of Vienna by Karl Landsteiner;
• Pharmaceutical companies initiating higher throughput protein screens
Antibodies
35
25
Proteins
15
12
Small Molecules
8
8
一、糖类药物的概念和特点
糖类药物定义 狭义的讲，糖类药物是指含有糖结构的化合物， 包括：寡糖、
ii) In 1930, Karl Landsteiner was awarded the Nobel Prize for this important discover !!
ABO human blood group antigens & antibodies
O
B
A
AB
Antigens On Cells
Growth Drivers
• Nearly half of all biopharmaceuticals in clinical development are therapeutic proteins or antibodies
• Numerous new lead agents for major therapeutic classes including cancer, inflammatory diseases, cardiovascular diseases, and infectious diseases
Revenue In Billions
Glycoprotein Market Growth
$80 $60 $40 $20 $0
Antibodie s Unglycosylated Proteins Glycopr ote ins
2000
2005
wk.baidu.com
2010
Estimated Growth Rates
2000-2005(%) 2005-2010(%)
Penicillin
iii) The chemical structure of penicillin was proved to β-Lactam structure by X-Ray in 1945;
iv) In 1945, A. Fleming, H. Florey and E. Chain shared the Nobel Prizes “for the discovery of penicillin and its curative effect in various infectious diseases “.
HO OH
HO
OO
O
O OH HO OH
Antibodies In Serum
Anti-A Anti-B
HO OH HO O HO OH
OH O O O O
O OH HOOH
Anti-A
HO OH
HO O HO OH
NHAc O
OO
O
O OH HO OH
Anti-B
A&B Antigens
ABO系统各种血型抗原的特异性是决定于糖蛋白上所含的糖链, 即H、A 和B糖抗原
Example 2: The discover of Penicillin
i) Penicillin was discovered by A. Fleming (UK) in 1928;
ii) In 1939, H. Florey and E. Chain successfully isolated Penicillin and investigated its bioactivity in 1940;
据统计，目前市售糖类药物约有500多种，其中主要以糖蛋白药物 为主；而且，在美国市场糖类药物的市场需求量以约50%逐年增高； 在全球市场率也以较高比例增长；
近年来，有关糖类药物的专著、研究文章、专利等也已数以万计， 基于糖分子的药物研究和开发成为实验室和药物公司企业的热点领域
Opportunity for Protein Therapeutics
E. Chain (UK)
H. Florey (AUS)
A. Fleming (UK)
The structure of peptidoglycan on the bacterial cell wall
Meroueh, S. O. et al.. PNAS 2006;103:4404-4409.
Peptidoglycan is a polymer consisting of sugars and amino acids that forms a mesh-like layer outside the plasma membrane of bacteria, forming the cell wall； The sugar part: β-(1,4) linked N-acetylglucosamine and N-acetylmuramic acid The peptide chain: three to five amino acids chain attached to the N-acetylmuramic acid
糖药物的发展历史
1963，从Canavalliaensiformis分离出的一种蛋白能够与红细胞上的 糖进行结合，糖作为药物概念开始出现；
1982年，第一个能与凝集素蛋白（Lectins）结合的动物糖类化合物 被分离、鉴定；
1980’s- 随着现代分析、分离技术的发展，基于糖类化合物的药物 分子得到飞速的发展；
The Role of Carbohydrates in Cell Surface Interactions
Example 1: ABO Blood Typing
Karl Landsteiner (1868-1943)
i) ABO blood types were discovered in 1900 and 1901 at the University of Vienna by Karl Landsteiner;