Fragment-based drug discovery in academia: Experiences from a tuberculosis programme

T.J. Heikkila; S. Surade; H.L. Silvestre; M.V.B. Dias; A. Ciulli; K. Bromfield; D. Scott; N. Howard; S. Wen; A.H. Wei; D. Osborne; C. Abell; T.L. Blundell

doi:10.1007/978-90-481-2339-1_3

Fragment-based drug discovery in academia: Experiences from a tuberculosis programme

T.J. Heikkila, S. Surade, H.L. Silvestre, M.V.B. Dias, A. Ciulli, K. Bromfield, D. Scott, N. Howard, S. Wen, A.H. Wei, D. Osborne, C. Abell, T.L. Blundell

Research output: Chapter in Book/Report/Conference proceeding › Chapter

2 Citations (Scopus)

Abstract

The problems associated with neglected diseases are often compounded by increasing incidence of antibiotic resistance. Patient negligence and abuse of antibiotics has lead to explosive growth in cases of tuberculosis, with some M. tuberculosis strains becoming virtually untreatable. Structure-based drug development is viewed as cost-effective and time-consuming method for discovery and development of hits to lead compounds. In this review we will discuss the suitability of fragment-based methods for developing new chemotherapeutics against neglected diseases, providing examples from our tuberculosis programme.

Original language	English
Title of host publication	From Molecules to Medicines
Subtitle of host publication	Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism
Editors	Joel L. Sussman, Paola Spadon
Publisher	Springer Netherlands
Pages	21-36
Number of pages	16
ISBN (Electronic)	9789048123391
ISBN (Print)	9789048123384
DOIs	https://doi.org/10.1007/978-90-481-2339-1_3
Publication status	Published - 2009

Publication series

Name	NATO Science for Peace and Security Series A: Chemistry and Biology
ISSN (Print)	1874-6489

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1007/978-90-481-2339-1_3

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Heikkila, T. J., Surade, S., Silvestre, H. L., Dias, M. V. B., Ciulli, A., Bromfield, K., Scott, D., Howard, N., Wen, S., Wei, A. H., Osborne, D., Abell, C., & Blundell, T. L. (2009). Fragment-based drug discovery in academia: Experiences from a tuberculosis programme. In J. L. Sussman, & P. Spadon (Eds.), From Molecules to Medicines: Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism (pp. 21-36). (NATO Science for Peace and Security Series A: Chemistry and Biology). Springer Netherlands. https://doi.org/10.1007/978-90-481-2339-1_3

Heikkila, T.J. ; Surade, S. ; Silvestre, H.L. et al. / Fragment-based drug discovery in academia : Experiences from a tuberculosis programme. From Molecules to Medicines: Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism. editor / Joel L. Sussman ; Paola Spadon. Springer Netherlands, 2009. pp. 21-36 (NATO Science for Peace and Security Series A: Chemistry and Biology).

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title = "Fragment-based drug discovery in academia: Experiences from a tuberculosis programme",

abstract = "The problems associated with neglected diseases are often compounded by increasing incidence of antibiotic resistance. Patient negligence and abuse of antibiotics has lead to explosive growth in cases of tuberculosis, with some M. tuberculosis strains becoming virtually untreatable. Structure-based drug development is viewed as cost-effective and time-consuming method for discovery and development of hits to lead compounds. In this review we will discuss the suitability of fragment-based methods for developing new chemotherapeutics against neglected diseases, providing examples from our tuberculosis programme.",

author = "T.J. Heikkila and S. Surade and H.L. Silvestre and M.V.B. Dias and A. Ciulli and K. Bromfield and D. Scott and N. Howard and S. Wen and A.H. Wei and D. Osborne and C. Abell and T.L. Blundell",

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language = "English",

isbn = "9789048123384",

series = "NATO Science for Peace and Security Series A: Chemistry and Biology",

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Heikkila, TJ, Surade, S, Silvestre, HL, Dias, MVB, Ciulli, A, Bromfield, K, Scott, D, Howard, N, Wen, S, Wei, AH, Osborne, D, Abell, C & Blundell, TL 2009, Fragment-based drug discovery in academia: Experiences from a tuberculosis programme. in JL Sussman & P Spadon (eds), From Molecules to Medicines: Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism. NATO Science for Peace and Security Series A: Chemistry and Biology, Springer Netherlands, pp. 21-36. https://doi.org/10.1007/978-90-481-2339-1_3

Fragment-based drug discovery in academia: Experiences from a tuberculosis programme. / Heikkila, T.J.; Surade, S.; Silvestre, H.L. et al.
From Molecules to Medicines: Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism. ed. / Joel L. Sussman; Paola Spadon. Springer Netherlands, 2009. p. 21-36 (NATO Science for Peace and Security Series A: Chemistry and Biology).

Research output: Chapter in Book/Report/Conference proceeding › Chapter

TY - CHAP

T1 - Fragment-based drug discovery in academia

T2 - Experiences from a tuberculosis programme

AU - Heikkila, T.J.

AU - Surade, S.

AU - Silvestre, H.L.

AU - Dias, M.V.B.

AU - Ciulli, A.

AU - Bromfield, K.

AU - Scott, D.

AU - Howard, N.

AU - Wen, S.

AU - Wei, A.H.

AU - Osborne, D.

AU - Abell, C.

AU - Blundell, T.L.

PY - 2009

Y1 - 2009

N2 - The problems associated with neglected diseases are often compounded by increasing incidence of antibiotic resistance. Patient negligence and abuse of antibiotics has lead to explosive growth in cases of tuberculosis, with some M. tuberculosis strains becoming virtually untreatable. Structure-based drug development is viewed as cost-effective and time-consuming method for discovery and development of hits to lead compounds. In this review we will discuss the suitability of fragment-based methods for developing new chemotherapeutics against neglected diseases, providing examples from our tuberculosis programme.

AB - The problems associated with neglected diseases are often compounded by increasing incidence of antibiotic resistance. Patient negligence and abuse of antibiotics has lead to explosive growth in cases of tuberculosis, with some M. tuberculosis strains becoming virtually untreatable. Structure-based drug development is viewed as cost-effective and time-consuming method for discovery and development of hits to lead compounds. In this review we will discuss the suitability of fragment-based methods for developing new chemotherapeutics against neglected diseases, providing examples from our tuberculosis programme.

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U2 - 10.1007/978-90-481-2339-1_3

DO - 10.1007/978-90-481-2339-1_3

M3 - Chapter

AN - SCOPUS:65349170092

SN - 9789048123384

T3 - NATO Science for Peace and Security Series A: Chemistry and Biology

SP - 21

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BT - From Molecules to Medicines

A2 - Sussman, Joel L.

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PB - Springer Netherlands

ER -

Heikkila TJ, Surade S, Silvestre HL, Dias MVB, Ciulli A, Bromfield K et al. Fragment-based drug discovery in academia: Experiences from a tuberculosis programme. In Sussman JL, Spadon P, editors, From Molecules to Medicines: Structure of Biological Macromolecules and Its Relevance in Combating New Diseases and Bioterrorism. Springer Netherlands. 2009. p. 21-36. (NATO Science for Peace and Security Series A: Chemistry and Biology). doi: 10.1007/978-90-481-2339-1_3

Fragment-based drug discovery in academia: Experiences from a tuberculosis programme

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