Abstract:
:In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a parallel format. These tests require either the lead or the target immobilization followed by incubation with the set of potential interaction partners and detection of a signal related to the target-ligand binding. In the first part of the review the different detection strategies amenable for drug screening are discussed. In the second part, a review of immobilization approaches for leads or targets, allowing the parallel screening of arrays of molecules, is presented.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Bergese P,Cretich M,Oldani C,Oliviero G,Di Carlo G,Depero LE,Chiari Mdoi
10.2174/092986708784872366subject
Has Abstractpub_date
2008-01-01 00:00:00pages
1706-19issue
17eissn
0929-8673issn
1875-533Xjournal_volume
15pub_type
杂志文章,评审abstract::RNA aptamers are non-coding small RNAs that bind to their cognate targets with high specificity and affinity. They are generally identified by iterative rounds of in vitro selection termed SELEX (Systemic Evolution of Ligands by Exponential Enrichment). Similar to antibodies, they can inhibit, modulate and disrupt the...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867311320290011
更新日期:2013-01-01 00:00:00
abstract::Vitamins are dietary components which are necessary for life. They play a major role in health and their deficiency may be linked to symptoms of psychiatric disorders. B vitamins are required for proper functioning of the methylation cycle, monoamine oxidase production, DNA synthesis and the repair and maintenance of ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160920110810
更新日期:2016-01-01 00:00:00
abstract::This review focuses on the development of nanoparticle systems for antimicrobial drug delivery. Numerous antimicrobial drugs have been prescribed to kill or inhibit the growth of microbes such as bacteria, fungi and viruses. Even though the therapeutic efficacy of these drugs has been well established, inefficient del...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710790416290
更新日期:2010-01-01 00:00:00
abstract:BACKGROUND:Visible light is absorbed by photoacceptors in pigmented and non-pigmented mammalian cells, activating signaling cascades and downstream mechanisms that lead to the modulation of cellular processes. Most studies have investigated the molecular mechanisms and therapeutic applications of UV and the red to near...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170727112206
更新日期:2018-01-01 00:00:00
abstract::The story of antimalarials as antinflammatory drugs dates back several centuries. Chinin, the extract of the Cinchona bark, has been exploited since the 18th century for its antimalarial and antifebrile properties. Later, during the Second World War, the broad use of antimalarials allowed arguing their antirheumatic e...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170911162331
更新日期:2018-01-01 00:00:00
abstract::Type 2 diabetes mellitus is a metabolic disease widely spread across industrialized countries. Sedentary lifestyle and unhealthy alimentary habits lead to obesity, boosting both glucose and fatty acid in the bloodstream and eventually, insulin resistance, pancreas inflammation and faulty insulin production or secretio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666171205163944
更新日期:2019-01-01 00:00:00
abstract::Kinetoplastid and apicomplexan parasites comprise a group of protozoans responsible for human diseases, with a serious impact on human health and the socioeconomic growth of developing countries. Chemotherapy is the main option to control these pathogenic organisms and nucleotide metabolism is considered a promising a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180926154329
更新日期:2019-01-01 00:00:00
abstract::Andrographolide, the main bioactive component separated from Andrographis paniculata in 1951, have been scrutinized with modern drug discovery approach for anti-inflammatory properties since 1984. Identifying new uses for existing drugs can be facilitated by evidence linking them to known or yet undiscovered drug targ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327666200810135604
更新日期:2020-08-10 00:00:00
abstract:BACKGROUND:Vaccines are very effective medical tools for disease prevention and life span increase. Controversies have raised concern about their safety, from autism to polio vaccine contamination with simian virus 40 (SV-40). Hysteria surrounding vaccine-associated risks has resulted in a declining number of vaccinati...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180518072730
更新日期:2018-01-01 00:00:00
abstract::Nitric Oxide (NO) is a signaling radical, highly diffusible pleiotropic regulator of a large set of different molecular and biological pathways, including, neurotransmission, vasodilatation and macrophagemediated responses against infections. It is produced from the amino acid L-Arginine and oxygen by the enzymatic ac...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160727105101
更新日期:2016-01-01 00:00:00
abstract::Inflammation is an initial response of the body to a harmful stimuli and it is achieved by the increased movement of leukocytes (especially granulocytes) from blood into injured tissues. It is required for healing wounds and infections. Despite their indispensable role in microbial killing, the inflammation reactions ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160607111806
更新日期:2016-01-01 00:00:00
abstract::Polyphenolic molecules produced by higher plants in response to biotic and abiotic stresses exert numerous effects on tumorigenic cell transformation, and on tumor cells in vitro and in vivo, and may interact with conventional anti-tumor therapies. In the present review, we collected and critically discussed data on: ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986709789352312
更新日期:2009-01-01 00:00:00
abstract::There is a need for novel drugs for the treatment of infectious diseases, autoimmunity and cancer. Cyclic peptides constitute a class of compounds that have made crucial contributions to the treatment of certain diseases. Penicillin, Vancomycin, Cyclosporin, the Echinocandins and Bleomycin are well-known cyclic peptid...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706777935113
更新日期:2006-01-01 00:00:00
abstract::Bile formation is an osmotic process driven by the vectorial transport of actively transferred biliary components across the basolateral (sinusoidal) and apical (canalicular) hepatocyte membranes, the latter being the rate-limiting step of the overall blood-to-bile transfer. The ATP-binding cassette (ABC) superfamily ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043455918
更新日期:2004-02-01 00:00:00
abstract::Flavonoids are major dietary constituents of plant-based food found ubiquitously in plant kingdom where they are usually present in substantial amounts. Rutin is a flavonol-type polyphenol which consists of the flavonol quercetin and the disaccharide rutinose. Rutin has been reported to exert diverse biological effect...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666171003114154
更新日期:2019-01-01 00:00:00
abstract::Protein Kinase Inhibitors (PKIs) and Histone Deacetylase Inhibitors (HDACIs) are two important classes of anticancer agents and have provided a variety of small molecule drugs for the treatment of various types of human cancers. However, malignant tumors are of a multifactorial nature that can hardly be "cured" by tar...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327666200102115720
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Immunomodulation is one of the significant therapeutic strategies. It includes both stimulation and suppression of the immune system by a variety of substances called immunomodulators, designed to regulate the immune response of the organism against infections of varying etiology. An example of such a substa...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170725140826
更新日期:2017-11-17 00:00:00
abstract::This review summarizes our knowledge of biochemical, biological and medical applications and properties of phosphinic acid compounds. Phosphinic acid compounds (phosphinates) are derivatives of phosphinic acid H2P(O)(OH). The major attention of this article is focused on applications of phosphinates of a pseudopeptide...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867003374831
更新日期:2000-06-01 00:00:00
abstract::Perceiving a pharmacophore is the first essential step towards understanding the interaction between a receptor and a ligand. Once a pharmacophore is established, a beneficial use of it is 3D database searching to retrieve novel compounds that would match the pharmacophore, without necessarily duplicating the topologi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867013372481
更新日期:2001-07-01 00:00:00
abstract:BACKGROUND:Numerous studies have demonstrated that halogenated agents elicit myocardial conditioning effects when adminis-tered perioperatively in cardiac surgery. Recent evidence has been published of the benefits of maintaining exposure to halogenated agents during the early postoperative period. The enzymatic mechan...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327999201001202607
更新日期:2020-10-01 00:00:00
abstract::Reprogramming technologies have been developed to revert somatic differentiated cells into pluripotent stem cells that can be differentiated into different lineages potentially useful in stem cell therapy. Reprogramming methods have been progressively refined to increase their efficiency, to obtain a cell population s...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867321666131129125624
更新日期:2014-01-01 00:00:00
abstract::Characterization of liver-specific autoantigens has given a fresh impetus to research in the pathogenesis of autoimmune liver diseases, viral-triggered and drug-induced autoimmunity affecting the liver. Intriguing is the fact that most of the liver-specific autoantigens are enzymes of key importance for cell's homeost...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708785747508
更新日期:2008-01-01 00:00:00
abstract::The maximum therapeutic potentials of pharmacologically active molecules are generally not attained due to their non specific delivery. Ligands associated with drug or delivery system through which it is delivered provide navigation and direction to the carrier system(s) so as to reach and release bioactive(s) at the ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707781368432
更新日期:2007-01-01 00:00:00
abstract::Chagas disease is an infectious tropical disease included within the group of neglected tropical diseases. Though historically endemic to Latin America, it has lately spread to high-income countries due to human migration. At present, there are only two available drugs, nifurtimox and benznidazole, approved for this t...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867326666191016114839
更新日期:2020-01-01 00:00:00
abstract::Existence of residual cancers and recurrence of cancers are two major limitations of conventional therapies against cancers. A naturally-occurring defense system against tumor may be established in cancer patients by induction of antitumor immunity. Both polyvalent and tumor antigen-defined vaccines have been administ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706778742882
更新日期:2006-01-01 00:00:00
abstract::Snakes are fascinating creatures and have been residents of this planet well before ancient humans dwelled the earth. Venomous snakes have been a figure of fear, and cause notable mortality throughout the world. The venom constitutes families of proteins and peptides with various isoforms that make it a cocktail of di...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170605091546
更新日期:2017-01-01 00:00:00
abstract::Chemoprevention is based on the use of non-toxic, pharmacologically active agents to prevent tumor progression. In this regard, natural dietary agents have been described by the most recent literature as promising tools for controlling onset and progression of malignancies. Extensive research has been so far performed...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867325666180629153141
更新日期:2020-01-01 00:00:00
abstract::The purinergic receptor P2X7 is highly expressed in immune peripheral and central cells suggesting its important role in numerous diseases characterized by inflammatory processes like cancer, or neurodegenerative pathologies in relation with modulation of the immune system. Thereby, antagonization of this receptor may...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867322666141212120926
更新日期:2015-01-01 00:00:00
abstract::Atrial fibrillation (AF) and chronic kidney disease (CKD) are disorders with increasing prevalence. The presence of CKD increases the risk of incident AF and vice versa, and the presence of AF may accelerate CKD progression. Nearly a third of patients with established CKD also have AF, whilst half of AF patients may h...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160210130109
更新日期:2016-01-01 00:00:00
abstract::The introduction of highly active antiretroviral therapy (HAART) in 1996 dramatically changed the course of HIV infection. This therapy involves the use of at least three agents from two distinct classes of antivirals: a protease inhibitor (PI) in combination with two nucleoside/nucleotide reverse transcriptase inhibi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707782360141
更新日期:2007-01-01 00:00:00