Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey

被引：31

作者：

Bosc, Damien ^{[1
]}

Jakhlal, Jouda ^{[1
]}

Deprez, Benoit ^{[1
]}

Deprez-Poulain, Rebecca ^{[1
]}

机构：

[1] Univ Lille, INSERM, Inst Pasteur Lille, Drugs & Mol Living Syst U1177, F-59000 Lille, France

来源：

FUTURE MEDICINAL CHEMISTRY | 2016年 / 8卷 / 04期

关键词：

SITU CLICK-CHEMISTRY; PROTEIN-CAPTURE AGENTS; CARBONIC-ANHYDRASE-II; IN-SITU; ACETYLCHOLINESTERASE INHIBITORS; SELECTIVE INHIBITOR; TERMINAL ALKYNES; ACHE INHIBITORS; THIO ACIDS; AZIDES;

D O I：

10.4155/fmc-2015-0007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

For the last 15 years, kinetic target-guided syntheses, including in situ click chemistry, have been used as alternative methods to find ligands to therapeutically relevant proteins. In this review, a comprehensive survey of biological targets used in kinetic target-guided synthesis covers historical and recent examples. The chemical reactions employed and practical aspects, including controls, library sizes and product detection, are presented. A particular focus is on the reagents and warhead selection and design with a critical overview of the challenges encountered. As protein supply remains a key success factor, it appears that increased efforts should be taken toward miniaturization in order to expand the scope of this strategy and qualify it as a fully fledged drug discovery tool.

引用

页码：381 / 404

页数：24

共 77 条

[1] Iterative In Situ Click Chemistry Creates Antibody-like Protein-Capture Agents [J].

Agnew, Heather D. ;

Rohde, Rosemary D. ;

Millward, Steven W. ;

Nag, Arundhati ;

Yeo, Woon-Seok ;

Hein, Jason E. ;

Pitram, Suresh M. ;

Tariq, Abdul Ahad ;

Burns, Vanessa M. ;

Krom, Russell J. ;

Fokin, Valery V. ;

Sharpless, K. Barry ;

Heath, James R. .

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2009, 48 (27) :4944-4948

[2] Inhibition of Human Sirtuins by in Situ Generation of an Acetylated Lysine-ADP-Ribose Conjugate [J].

Asaba, Tomomi ;

Suzuki, Takayoshi ;

Ueda, Rie ;

Tsumoto, Hiroki ;

Nakagawa, Hidehiko ;

Miyata, Naoki .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2009, 131 (20) :6989-6996

[3]

Bienstock RJ, 2011, ACS S SERIES

[4] Bcl-2 Inhibitors: Emerging Drugs in Cancer Therapy [J].

Bodur, C. ;

Basaga, H. .

CURRENT MEDICINAL CHEMISTRY, 2012, 19 (12) :1804-1820

[5] Ruthenium-catalyzed azide-alkyne cycloaddition: Scope and mechanism [J].

Boren, Brant C. ;

Narayan, Sridhar ;

Rasmussen, Lars K. ;

Zhang, Li ;

Zhao, Haitao ;

Lin, Zhenyang ;

Jia, Guochen ;

Fokin, Valery V. .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2008, 130 (28) :8923-8930

[6] Freeze-frame inhibitor captures acetylcholinesterase in a unique conformation [J].

Bourne, Y ;

Kolb, HC ;

Radic, Z ;

Sharpless, KB ;

Taylor, P ;

Marchot, P .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2004, 101 (06) :1449-1454

[7] 1,2,5-, 1,3,4- AND 1,2,4-OXADIAZOLES - A THEORETICAL STUDY OF ELECTRIC DIPOLE MOMENTS [J].

BROWN, RD ;

COLLER, BAW ;

KENT, JE .

THEORETICA CHIMICA ACTA, 1968, 10 (05) :435-&

[8] Diuretics with carbonic anhydrase inhibitory action: a patent and literature review (2005-2013) [J].

Carta, Fabrizio ;

Supuran, Claudiu T. .

EXPERT OPINION ON THERAPEUTIC PATENTS, 2013, 23 (06) :681-691

[9] CONDITIONS FOR SELF-CATALYSED INACTIVATION OF CARNITINE ACETYLTRANSFERASE - A NOVEL FORM OF ENZYME INHIBITION [J].

CHASE, JFA ;

TUBBS, PK .

BIOCHEMICAL JOURNAL, 1969, 111 (02) :225-&

[10] Selective inhibition of Biotin Protein Ligase from Staphylococcus aureus [J].

da Costa, Tatiana P. Soares ;

Tieu, William ;

Yap, Min Y. ;

Pendini, Nicole R. ;

Polyak, Steven W. ;

Pedersen, Daniel Sejer ;

Morona, Renato ;

Turnidge, John D. ;

Wallace, John C. ;

Wilce, Matthew C. J. ;

Booker, Grant W. ;

Abell, Andrew D. .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2012, 287 (21) :17823-17832

← 1 2 3 4 5 6 7 8 →