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Pure Appl. Chem., Vol. 70, No. 11,
pp. 2126, 1998
Molecular diversity, biological diversity and
the search for new drugs*
Robert P. Borris and Steven J. Gould
Department of Natural Products Drug Discovery, Merck Research Laboratories,
P.O.Box 2000, P. Roy Vagelos Research and Development Center Rahway,
New Jersey 07065, USA.
E-mail: [email protected]
Abstract: The success of the drug discovery process is often
a function of the diversity of chemotypes examined. Natural products
screening represents a potential source of organic chemicals of
unparalleled diversity. To effectively realize this potential requires
use of a selection strategy tailored to the needs of the individual
screening program. Historically, plants and microorganisms have
been extraordinarily rich sources of medicinally and agriculturally
useful compounds. Interest in these sources of new bioactive molecules
continues to the present time. In recent years, the evaluation of
insects and Marine invertebrates as sources of biologically active
compounds has added to the array of new chemotypes. While the efficiencies
of modern screening methods allow for the cost effective evaluation
of vast numbers of samples, the cost of acquiring and processing
natural products, particularly macro-organisms, is substantial relative
to other sources of molecular diversity. A successful drug discovery
program must then aim to evaluate the broadest diversity of relevant
chemical classes in the minimum number of samples and least time.
To achieve this goal, a careful assessment must be made of each
source of molecular diversity, natural and man-made, and a proper
balance of sources established. An evaluation of the ecological/environmental
ramifications of collecting organisms from natural populations for
screening operations and pre-development studies is an integral
part of this assessment. While the screening of natural products,
requiring a very small sample, is a practical endeavour, the realities
of obtaining sufficient quantities of compound from natural populations
of macroorganisms to support product development and eventual sale
are often problematic. Alternative methods of producing interesting
compounds, including synthesis, cell culture and agriculture, may
be required in order to minimize the ecological impact of these
discoveries. While our environmental concerns often focus on the
direct impact of this research, they extend far beyond the scope
of these studies, fostering the preservation and sustainable utilization
of the natural habitats of our collaboratoring source countries.
This presentation will contrast the attributes of the molecular
diversity obtainable from a variety of natural and manmade sources,
with illustrative examples from recent experience.
Download full text (9 pages)
- PDF file (46KB)
* Invited lecture presented at the International
Conference on Bioversity and Bioresources: Conservation and
Utilization, 23-37 November 1997, Phuket, Thailand.
Page last modified 15 April 1999.
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