Photoaffinity labeling in drug discovery and developments: chemical gateway for entering proteomic frontier.

Abstract:

:One of the major events occurring at biological interfaces is the specific recognition of bioactive ligands by their receptor proteins. The elucidation of interacting partners is an immediate entrance into the discovery of medicinal leads. The method of photoaffinity labeling enables the direct probing of target protein through a covalent bond introduced between a ligand and its specific receptor. Thus, the photoaffinity labeling is applied in two stages of drug discovery and development processes. First, the method is useful for the screening of early leads. If the binding site analysis of target protein is important for defining a particular pharmacophore, the photoaffinity labeling will give the structural information at the contact point of drugs with receptors. Second, emerging new technologies, combinatorial chemistry, recombinant DNA techniques, and high-throughput analysis, are extending the potential of photoaffinity labeling to become a rapid and more sensitive means for the identification of drug-receptor pairs as well as the elucidation of molecular recognition mechanism at drug-receptor interfaces. This review focuses on several recent impacts of photoaffinity labeling as a useful tool for drug discovery and developments.

journal_name

Curr Top Med Chem

authors

Hatanaka Y,Sadakane Y

doi

10.2174/1568026023394182

keywords:

subject

Has Abstract

pub_date

2002-03-01 00:00:00

pages

271-88

issue

3

eissn

1568-0266

issn

1873-4294

journal_volume

2

pub_type

杂志文章,评审
  • Modulators of protein-protein interactions: novel approaches in targeting protein kinases and other pharmaceutically relevant biomolecules.

    abstract::In recent years the development of small organic molecules modulating protein-protein interactions (P-PIs) has drawn major attention in both academic and industrial research. Despite the appreciable progress being made, targeting such extensive interaction areas with comparatively small, drug-like agents has proven to...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802611795589610

    authors: Rechfeld F,Gruber P,Hofmann J,Kirchmair J

    更新日期:2011-01-01 00:00:00

  • QSAR in the pharmaceutical research setting: QSAR models for broad, large problems.

    abstract::The field of quantitative structure activity relationships (QSAR) has evolved into an integral tool for pharmaceutical discovery. It is presently an accessible technology, as can be shown by the number papers which are easily found through PubMed literature searches. At one level, QSAR is used routinely and invisibly ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802610791111506

    authors: Sprous DG,Palmer RK,Swanson JT,Lawless M

    更新日期:2010-01-01 00:00:00

  • General theory for multiple input-output perturbations in complex molecular systems. 1. Linear QSPR electronegativity models in physical, organic, and medicinal chemistry.

    abstract::In general perturbation methods starts with a known exact solution of a problem and add "small" variation terms in order to approach to a solution for a related problem without known exact solution. Perturbation theory has been widely used in almost all areas of science. Bhor's quantum model, Heisenberg's matrix mecha...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026611313140011

    authors: González-Díaz H,Arrasate S,Gómez-SanJuan A,Sotomayor N,Lete E,Besada-Porto L,Ruso JM

    更新日期:2013-01-01 00:00:00

  • Prediction and Dissection of Protein-RNA Interactions by Molecular Descriptors.

    abstract::Protein-RNA interactions play crucial roles in numerous biological processes. However, detecting the interactions and binding sites between protein and RNA by traditional experiments is still time consuming and labor costing. Thus, it is of importance to develop bioinformatics methods for predicting protein-RNA intera...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026615666150819110703

    authors: Liu ZP,Chen L

    更新日期:2016-01-01 00:00:00

  • The Importance of Bioactivation in Computer-Guided Drug Repositioning. Why the Parent Drug is Not Always Enough.

    abstract::Although bioactivation is a well-documented process and the role of active metabolites in the drug discovery field has long been recognized, drug metabolites are usually ignored in virtual screening campaigns oriented to drug repositioning. The present article discusses different issues related to overlooking of the a...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666160216155043

    authors: Talevi A

    更新日期:2016-01-01 00:00:00

  • Sex steroids effects in normal endocrine pancreatic function and diabetes.

    abstract::Traditionally the role of sexual steroid hormones was focused primarily on reproductive organs: the breast, female reproductive tract (uterus, mammary gland, and ovary), and male reproductive tract (testes, epididymis and prostate), however our current understanding of tissue-specific effects of sex steroids has eluci...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802611796117540

    authors: Morimoto S,Jiménez-Trejo F,Cerbón M

    更新日期:2011-01-01 00:00:00

  • Coagulation factor Xa inhibition: biological background and rationale.

    abstract::Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug di...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026013395380

    authors: Leadley RJ Jr

    更新日期:2001-06-01 00:00:00

  • Structure-based Methods for Binding Mode and Binding Affinity Prediction for Peptide-MHC Complexes.

    abstract::Understanding the mechanisms involved in the activation of an immune response is essential to many fields in human health, including vaccine development and personalized cancer immunotherapy. A central step in the activation of the adaptive immune response is the recognition, by T-cell lymphocytes, of peptides display...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026619666181224101744

    authors: Antunes DA,Abella JR,Devaurs D,Rigo MM,Kavraki LE

    更新日期:2018-01-01 00:00:00

  • The role of water molecules in computational drug design.

    abstract::Although water molecules are small and only consist of two different atom types, they play various roles in cellular systems. This review discusses their influence on the binding process between biomacromolecular targets and small molecule ligands and how this influence can be modeled in computational drug design appr...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802610790232288

    authors: de Beer SB,Vermeulen NP,Oostenbrink C

    更新日期:2010-01-01 00:00:00

  • Paralog Specific Hsp90 Inhibitors - A Brief History and a Bright Future.

    abstract:BACKGROUND:The high sequence and structural homology among the hsp90 paralogs - Hsp90α, Hsp90β, Grp94, and Trap-1 - has made the development of paralog-specific inhibitors a challenging proposition. OBJECTIVE:This review surveys the state of developments in structural analysis, compound screening, and structure-based ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666160413141154

    authors: Gewirth DT

    更新日期:2016-01-01 00:00:00

  • Carbonic anhydrase inhibitors as anticonvulsant agents.

    abstract::Seizures are one of the most common neurological disorders in clinical medicine. Triggering mechanisms by which seizures form remain unclear, but are related to a rapid change in ionic composition, including an increase of intracellular potassium concentration and pH shifts within the brain. pH buffering of extra- and...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802607780636726

    authors: Thiry A,Dogné JM,Supuran CT,Masereel B

    更新日期:2007-01-01 00:00:00

  • Update on COX-2 Selective Inhibitors: Chemical Classification, Side Effects and their Use in Cancers and Neuronal Diseases.

    abstract::Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026617666170821124947

    authors: Rayar AM,Lagarde N,Ferroud C,Zagury JF,Montes M,Sylla-Iyarreta Veitia M

    更新日期:2017-01-01 00:00:00

  • Assessment of network states: local hemodynamics.

    abstract::Neural activity utilizes energy resources and requires replenishment of metabolites through vascular dilation. During wake, cortical neurons usually have depolarized membrane potentials and exhibit frequent spontaneous action potentials, requiring an increased metabolic delivery to activated tissue and causing blood v...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802611797470349

    authors: Schei JL,Rector DM

    更新日期:2011-01-01 00:00:00

  • The discovery of novel chemotypes of p38 kinase inhibitors.

    abstract::In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors long before the identity of the p38 kinase was known. During the last 10 years a number of novel p38 chemotypes were dis...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026054985948

    authors: Diller DJ,Lin TH,Metzger A

    更新日期:2005-01-01 00:00:00

  • Strategies for the discovery and advancement of novel cationic antimicrobial peptides.

    abstract::Multi-drug resistant bacteria are appearing at an alarming rate and impose significant burdens on healthcare systems worldwide. Cationic peptides have shown great promise as broad spectrum antimicrobial agents with a demonstrated ability to kill resistant bacteria, however, issues such as protease susceptibility and t...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802610793176648

    authors: Hadley EB,Hancock RE

    更新日期:2010-01-01 00:00:00

  • Development of Crystalline Cellulosic Fibres for Sustained Release of Drug.

    abstract::Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026616666160215160426

    authors: Mishra D,Yadav V,Khare P,Jyotshna,Das MR,Meena A,Shanker K

    更新日期:2016-01-01 00:00:00

  • Marcfortine and paraherquamide class of anthelmintics: discovery of PNU-141962.

    abstract::Three distinct chemical classes for the control of gastrointestinal nematodes are available: benzimidazoles, imidazothiazoles, and macrocyclic lactones. The relentless development of drug resistance has severely limited the usefulness of such drugs and the search for a new class of compounds preferably with a differ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026023393705

    authors: Lee BH,Clothier MF,Dutton FE,Nelson SJ,Johnson SS,Thompson DP,Geary TG,Whaley HD,Haber CL,Marshall VP,Kornis GI,McNally PL,Ciadella JI,Martin DG,Bowman JW,Baker CA,Coscarelli EM,Alexander-Bowman SJ,Davis JP,Zinser E

    更新日期:2002-07-01 00:00:00

  • Achievements in Cancer Research and its Therapeutics in Hundred Years.

    abstract::Cancer research has progressed leaps and bounds over the years. This review is a brief overview of the cancer research, milestone achievements and therapeutic studies on it over the one hundred ten years which would give us an insight into how far we have come to understand and combat this fatal disease leading to mil...

    journal_title:Current topics in medicinal chemistry

    pub_type: 历史文章,杂志文章,评审

    doi:10.2174/1568026619666190730093034

    authors: Shastri S,Chatterjee B,Thakur SS

    更新日期:2019-01-01 00:00:00

  • Elucidating Treatment of Alzheimer's Disease via Different Receptors.

    abstract::Alzheimer's disease (AD) is an irreversible multifaceted neurodegenerative disorder that gradually degrades neuronal cells. Presently, it is the most common reason for the memory loss and dementia in older individuals. It is patho-physiologically described by extracellular amyloid beta (Aβ) deposition, intracellular n...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026617666170103163715

    authors: Ul Islam B,Khan MS,Jabir NR,Kamal MA,Tabrez S

    更新日期:2017-01-01 00:00:00

  • Selective fluorination in drug design and development: an overview of biochemical rationales.

    abstract::Several strategies used in the rational design and synthesis of fluorinated compounds as potential therapeutic agents are reviewed. Applications of fluorine substitution in empirical SAR studies for lead development also are discussed, along with the implications with respect to fluorine target interactions that can b...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802606777951073

    authors: Kirk KL

    更新日期:2006-01-01 00:00:00

  • Impact of COX-2 inhibitors in common clinical practice a gastroenterologist's perspective.

    abstract::Non-selective NSAIDs enhance the risk of serious ulcer complications (bleeding, perforation, obstruction), hospitalization and death about 3-10-fold. The gastrointestinal side effects of NSAIDs have a considerable economical burden, since they are responsible for 5-10 billion dollars in hospitalization charges and los...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026054201703

    authors: Lehmann FS,Beglinger C

    更新日期:2005-01-01 00:00:00

  • N-[3,5-Bis(trifluoromethyl)phenyl]-5-bromo-2-hydroxybenzamide Analogues: Novel Acetyl- and Butyrylcholinesterase Inhibitors.

    abstract:BACKGROUND:Development of acetyl- (AChE) and butyrylcholinesterase (BuChE) inhibitors belongs to viable strategies for the treatment of dementia and other diseases related to decrease in cholinergic neurotransmission. OBJECTIVE:That is why we designed twenty-two analogues of a dual AChEBuChE salicylanilide inhibitor, ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026620666200819154722

    authors: Krátký M,Jaklová K,Štěpánková Š,Svrčková K,Pflégr V,Vinšová J

    更新日期:2020-01-01 00:00:00

  • On the Possible Relevance of Bottom-up Pathways in the Pathogenesis of Alzheimer's Disease.

    abstract::Dementia is an increasing health problem in older aged populations worldwide. Age-related changes in the brain can be observed decades before the first symptoms of cognitive decline appear. Cognitive impairment has chronic inflammatory components, which can be enhanced by systemic immune activation. There exist mutual...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026620666200514090359

    authors: Leblhuber F,Steiner K,Geisler S,Fuchs D,Gostner JM

    更新日期:2020-01-01 00:00:00

  • Rational design of potent and selective VLA-4 inhibitors and their utility in the treatment of asthma.

    abstract::Asthma, a chronic inflammatory disease of the airways, is a significant burden on our healthcare system. There is high unmet need for treatments directed towards the underlying causes of the disease. The cell surface integrin VLA-4 (very late antigen-4; alpha4beta1; CD49d/CD29) plays an important role in the trafficki...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026043387520

    authors: Singh J,Adams S,Carter MB,Cuervo H,Lee WC,Lobb RR,Pepinsky RB,Petter R,Scott D

    更新日期:2004-01-01 00:00:00

  • Synthesis of Coumarin Derivatives as Versatile Scaffolds for GSK-3β Enzyme Inhibition.

    abstract:BACKGROUND:Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026619666191019105349

    authors: Francisco CS,Javarini CL,de S Barcelos I,Morais PAB,de Paula H,de S Borges W,Neto ÁC,Lacerda V

    更新日期:2020-01-01 00:00:00

  • Kisspeptin Mediated Signaling in Cancer.

    abstract::Research over the years has gradually and sequentially highlighted contributory role of hypothalamic- based kisspeptin-signaling axis as a major positive modulator of the neuroendocrinological reproductive axis in mammals. However, a series of landmark studies provided convincing evidence of role of this signaling in ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666160212123309

    authors: Jabeen S,Qureshi MZ,Javed Z,Iqbal MJ,Ismail M,Farooqi AA

    更新日期:2016-01-01 00:00:00

  • Axin PPI Networks: New Interacting Proteins and New Targets?

    abstract::The scaffold protein Axin plays important roles in multiple signaling pathways through mediating the formation of different signaling complexes. Axin is best known for its role as a negative regulator in Wnt/β-catenin pathway. Aberrant activation of the key components in Wnt/β-catenin pathway including Axin has been l...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026616666160622220245

    authors: Song X,Cai W,Li L

    更新日期:2016-01-01 00:00:00

  • Dopamine transporter ligands: recent developments and therapeutic potential.

    abstract::The dopamine transporter (DAT) is a target for the development of pharmacotherapies for a number of central disorders including Parkinson's disease, Alzheimer's disease, schizophrenia, Tourette's syndrome, Lesch-Nyhan disease, attention deficit hyperactivity disorder (ADHD), obesity, depression, and stimulant abuse as...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802606778249775

    authors: Runyon SP,Carroll FI

    更新日期:2006-01-01 00:00:00

  • Pyridines and Imidazopyridines with Medicinal Significance.

    abstract::Pyridine and pyridine-fused ring systems are ubiquitous in medicinal research and demonstrate such diverse pharmacological benefits as anticonvulsant therapies, treatment for fungal and bacterial infections as well as chemotherapy agents. For example, imidazo[1,2-a]pyridines have exhibited a broad range of activity as...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666160506145141

    authors: Kishbaugh TL

    更新日期:2016-01-01 00:00:00

  • Dipeptide inhibitors of thermolysin and angiotensin I-converting enzyme.

    abstract::Thermolysin (TLN) and other thermolysin-like zinc metalloproteinases (TLPs),are important virulence factors for pathogenesis of bacterial infections by suppressing the innate immune system of the host. Therapeutic inhibition ofTLPs is believed to be a novel strategy inthe development of a new generation antibiotics.In...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/156802612803989246

    authors: Khan MT,Dedachi K,Matsui T,Kurita N,Borgatti M,Gambari R,Sylte I

    更新日期:2012-01-01 00:00:00