339:
263:, which play a role in cell signaling, pigmentation and in defense against predation. Secondary metabolites are a rich source of biologically active compounds and hence are often used as research tools and leads for drug discovery. Examples of secondary metabolites include:
561:
The majority of drugs from the general reference set have molecular weights below 550. In contrast the molecular-weight distribution of oral antibacterial agents is bimodal: 340–450 Da but with another group in the 700–900 molecular weight
474:
agents. SMATs are new, broad-spectrum drugs that unify antibacterial, antiviral and anti-malarial activities into a single therapeutic that offers substantial cost benefits and logistic advantages for physicians and the military.
242:
administration. Small molecule drugs are also typically simpler to manufacture and cheaper for the purchaser. A downside is that not all targets are amenable to modification with small-molecule drugs; bacteria and
192:") has been recommended for oral small molecule drug candidates based on the observation that clinical attrition rates are significantly reduced if the molecular weight is kept below this limit.
542:
617:
Veber DF, Johnson SR, Cheng HY, Smith BR, Ward KW, Kopple KD (June 2002). "Molecular properties that influence the oral bioavailability of drug candidates".
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limit for a small molecule is approximately 900 daltons, which allows for the possibility to rapidly diffuse across cell membranes so that it can reach
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Table 5.13: Route of
Administration: Small Molecules: oral administration usually possible; Biomolecules: Usually administered parenterally
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78:, and monosaccharides, respectively) are often considered small molecules. Small molecules may be used as research tools to probe
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417:
226:. Small molecules are more likely to be absorbed, although some of them are only absorbed after oral administration if given as
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409:
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Arkin MR, Wells JA (April 2004). "Small-molecule inhibitors of protein-protein interactions: progressing towards the dream".
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Leeson PD, Springthorpe B (November 2007). "The influence of drug-like concepts on decision-making in medicinal chemistry".
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416:, which promotes cancer, making it a useful investigative tool. There is also interest in creating small molecule
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is that many small molecules can be taken orally whereas biologics generally require injection or another
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sites of action. This molecular weight cutoff is also a necessary but insufficient condition for oral
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Introduction to
Biological and Small Molecule Drug Research and Development: theory and case studies
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cells. In addition to intestinal permeability, the molecule must also possess a reasonably rapid
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are not small molecules, although their constituent monomers (ribo- or deoxyribonucleotides,
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Lipinski CA (December 2004). "Lead-and drug-like compounds: the rule-of-five revolution".
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usually restricts the term "small molecule" to molecules that bind specific biological
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A variety of organisms including bacteria, fungi, and plants, produce small molecule
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Most pharmaceuticals are small molecules, although some drugs can be proteins (e.g.,
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that may regulate a biological process, with a size on the order of 1 nm. Many
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to quantify the reaction affinities and kinetic properties and also any induced
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in farming, and in many other roles. These compounds can be natural (such as
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Cell culture example of a small molecule as a tool instead of a protein. In
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can be characterised using a variety of analytical techniques such as
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are small molecules; the terms are equivalent in the literature.
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Mfopou JK, De Groote V, Xu X, Heimberg H, Bouwens L (May 2007).
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136:); they may have a beneficial effect against a disease (such as
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748:(Kindle ed.). New York: Academic Press. pp. 161–203.
90:. Some can inhibit a specific function of a protein or disrupt
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543:"Chemical properties of antibacterials and their uniqueness"
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Wienken CJ, Baaske P, Rothbauer U, Braun D, Duhr S (2010).
424:, examples include wrenchnolol (a wrench shaped molecule).
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Enzymes and receptors are often activated or inhibited by
742:"Chapter 5.2 How do SMDs differ from biomolecular drugs?"
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Ngo, Huy X.; Garneau-Tsodikova, Sylvie (23 April 2018).
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pathway inhibited, which can be done by adding to the
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744:. In Ganellin CR, Jefferis R, Roberts SM (eds.).
27:Organic molecule with a weight of ≤1000 daltons
361:signaling pathway must be activated while the
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408:An example is the teratogen and carcinogen
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247:are often resistant to their effects.
841:. Vol. 36. Amsterdam: Elsevier.
839:Studies in Natural Products Chemistry
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547:Antibiotic Discovery and Development
545:. In Dougherty TJ, Pucci MJ (eds.).
782:"What are the drugs of the future?"
940:Koh JT, Zheng J (September 2007).
754:10.1016/B978-0-12-397176-0.00005-4
664:Drug Discovery Today: Technologies
234:(SMDs) have over "large molecule"
46:is a low molecular weight (≤ 1000
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919:. New York: J. Wiley & Sons.
140:) or may be detrimental (such as
441:dual polarisation interferometry
418:artificial transcription factors
410:phorbol 12-myristate 13-acetate
1034:. San Francisco Business Times
180:into water and adequate water
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699:Nature Reviews Drug Discovery
576:Nature Reviews Drug Discovery
1032:"Bio-defense company re-ups"
837:Atta-ur-Rahman, ed. (2012).
549:. Springer. pp. 801–2.
375:Hedgehog interacting protein
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86:in the development of new
470:signatures found in many
451:Anti-genomic therapeutics
437:microscale thermophoresis
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391:small molecule inhibitors
218:). With the exception of
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1056:Small+Molecule+Libraries
911:Voet JG, Voet D (1995).
466:technology that targets
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230:. One advantage that
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184:and moderate to low
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80:biological function
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868:Stem Cells
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401:or on the
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308:Polyketide
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