Drug Discovery (Lead Identification and High Throughput Screening)

Ravi Kumar

doi:10.52711/2321-5836.2021.00010

Research Journal of Pharmacology and Pharmacodynamics

ISSN

2321-5836 (Online)
0975-4407 (Print)

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Drug Discovery (Lead Identification and High Throughput Screening)

Author(s): Ravi Kumar

Email(s): ravikashyap7417@gmail.com

DOI: 10.52711/2321-5836.2021.00010

Address: Ravi Kumar*
Bharat Institute of Technology, Meerut (U.P.)
*Corresponding Author

Published In: Volume - 13, Issue - 2, Year - 2021

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ABSTRACT:
In this review we will discuss about the Lead identification, the lead identification is mostly used for the discovery of successful clinical development compound, and it is an essential site for drug discovery. Various important factors that required for discovery a quality leads, such as- Physicochemical, ADME, Biological and PK parameters. These all parameters are required for the identification of high-quality leads. The Combinational chemistry is mostly used for the generation of many compounds in only one process from a mixture. The high throughput screening is suitable for new drug in pharmaceutical industries and it’s mostly used from last two decades.

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Cite this article:
Ravi Kumar. Drug Discovery (Lead Identification and High Throughput Screening). Research Journal of Pharmacology and Pharmacodynamics. 2021; 13(2):46-0. doi: 10.52711/2321-5836.2021.00010

Cite(Electronic):
Ravi Kumar. Drug Discovery (Lead Identification and High Throughput Screening). Research Journal of Pharmacology and Pharmacodynamics. 2021; 13(2):46-0. doi: 10.52711/2321-5836.2021.00010 Available on: https://rjppd.org/AbstractView.aspx?PID=2021-13-2-4

REFERENCES:
1.   Gordon, E. M., Barrett, R. W., Dower, W. J., Fodor, S. P. A., Gallop, M. A. Applications of Combinatorial Technologies to Drug Discovery: 2. Combinatorial Organic Synthesis, Library Screening Strategies, and Future Directions. J. Med. Chem. 1994, 37, 1385–1401.
2.   Schafffrath, M., von Roedern, E., Hamley, P., Stilz, H. U. High-Throughput Purification of Single Compounds and Libraries. J. Comb. Chem. 2005, 7, 546–553.
3.   Ohlmeyer, M. H., Swanson, R. N., Dillard, L. W., Reader, J. C., Asouline, G., Kobayashi, R. Complex Synthetic Chemical Libraries Indexed with Molecular Tags. Proc. Natl. Acad. Sci. 1993, 90, 10922–10926.
4.   Erlandson, D. A., McDowell, R. S., O’Brien, T. Fragment Based Drug Discovery. J. Med. Chem. 2004, 47, 3463–3482.
5.   Carr, R. A. E., Congreve, M., Murray, C. W., Rees, D. C. Fragment-Based Lead Discovery: Leads by Design. Drug Disc. Today. 2005, 10, 987–992.
6.   Krishnamurthy, V. M., Semetey, V., Bracher, P. J., Shen, N., Whitesides, G. M. Dependence of Effective Molarity on Linker Length for an Intramolecular Protein-Ligand System. J. Am. Chem. Soc. 2007, 129, 1312–1320.
7.   Shuker, S. B., Hajduk, P. J., Meadows, R. P., Fesik, S. W. Discovering High-Affinity Ligands for Proteins: SAR by NMR. Science. 1996, 274, 1531–1534.
8.   Hajduk, P. J., Sheppard, G., Nettesheim, D. G., Olejniczak, E. T., Shuker, S. B., Meadows, R. P, Discovery of Potent Nonpeptide Inhibitors of Stromelysin Using SAR by NMR. J. Am. Chem. Soc. 1997, 119, 5818–5827.
9.   Congreve, M. S., Davis, D. J., Devine, L., Granata, C., O’Reilly, M., Wyatt, P. G., Jhoti, H. Detection of Ligands from a Dynamic Combinatorial Library by X-ray Crystallography. Angew. Chem. Int. Ed. 2003, 42, 4479–4482.
10.   Lyne, P. D. Structure-Based Virtual Screening: An Overview. Drug Disc. Today. 2002, 7, 1047–1055.
11.   Irwin, J. J., Shoichet, B. K. ZINC: A Free Database of Commercially Available Compounds for Virtual Screening. J. Chem. Inf. Model. 2005, 45, 177–182.
12.   Forino, M., Jung, D., Easton, J. B., Houghton, P. J., Pellecchia, M. Virtual Docking Approaches to Protein Kinase B Inhibition. J. Med. Chem. 2005, 48, 2278–2281.
13.   Tervo, A. J., Kyrylenko, S., Niskanen, P., Salminen, A., Leppänen, J., Nyrönen, T. H., An in Silico Approach to Discovering Novel Inhibitors of Human Sirtuin Type 2. J. Med. Chem. 2004, 47, 6292–6298.
14.   Kellenberger, E., Springael, J.-Y., Permentier, M., HachetHaas, M., Galzi, J.-L., Rognan, D. Identification of Nonpeptide CCR5 Receptor Agonists by Structure-Based Virtual Screening. J. Med. Chem. 2007, 50, 1294–1303.
15.   Cole, C. J., Pfund, W. P. Permeability Assays. Mod. Drug Disc. 2000, 3, 73–76.
16.   Li, A. P. Preclinical in Vitro Screening Assays for DrugLike Properties. Drug Disc. Today. 2005, 2, 179–185.
17.   Wunberg, T., Hendrix, M., Hillisch, A., Lobell, M., Meier, H., Schmeck, C. Improving the Hit-to-Lead Process: Data-Driven Assessment of Drug-Like and Lead-Like Screening Hits. Drug Disc. Today. 2006, 11, 175–180.
18.   Lipinski, C. A., Lombardo, F., Dominy, B. W., Feeney, P. J. Experimental and Computational Approaches to Estimate Solubility and Permeability in Drug Discovery and Development Settings. Adv. Drug Del. Rev. 1997, 23, 3–25.
19.   Teague, S. J., Davis, A. M., Leeson, P. D., Oprea, T. The Design of Leadlike Combinatorial Libraries. Angew. Chem. Int. Ed. 1999, 38, 3743–3748.
20.   Veber, D. F., Johnson, S. R., Cheng, H.-Y., Smith, B. R., Ward, K. W., and Kopple, K. D. Molecular Properties That Influence the Oral Bioavailability of Drug Candidates. J. Med. Chem. 2002, 45, 2615–2623.
21.   Edwards, M. P., Price, D. A. Role of Physiochemical Properties and Ligand Lipophilicity Efficiency in Addressing Drug Safety Risks. Annu. Rep. Med. Chem. 2010, 45, 381–391.
22.   Nassar, A.-E. F., Kamel, A. M., Clarimont, C. Improving the Decision-Making Process in Structural Modification of Drug Candidates: Reducing Toxicity. Drug Disc. Today. 2004, 9, 1055–1064.
23.   The American Heritage Dictionary of the English Language (4th ed.). New York: Houghton Mifflin, 2000.
24.   Sneader, W. Drug Prototypes and their Exploitation. New York: Wiley, 1996, pp. 469–478.
25.   Sternbach, L. H. The Benzodiazepine Story. J. Med. Chem. 1979, 22, 1–7.
26.   Wermuth, C. Selective Optimization of Side Activities: Another Way for Drug Discovery. J. Med. Chem. 2004, 47, 1303–1314.
27.   Greenwood, D. T., Mallion, K. B., Todd, A. H., Turner, R. W. 2-Aryloxymethyl-2,3,5,6-tetrahydro-1,4-oxazines: A New Class of Antidepressants. J. Med. Chem. 1975, 18, 573–577.
28.   Kling, J. From Hypertension to Angina to Viagra. Mod. Drug Disc. 1998, 1(2), 31–38.
29.   Newman, D. J., Cragg, G. M. Natural Products as Sources of New Drugs over the Last 25 Years. J. Nat. Prod. 2007, 70, 461–477.
30.   Quinn, R. J., Carroll, A. R., Pham, N. B., Baron, P., Palframan, M. E., Suraweera, L. Developing a Drug-Like Natural Product Library. J. Nat. Prod. 2008, 71, 464–468.

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