Abdurrahman Olgaç
Gazi University
Desensitization (telecommunications)Modular designVirtual screeningMeta-Software engineeringBiological activityDocking (molecular)Molecular biologyMedicinal chemistryAMPA receptorTranslational medicineProinflammatory cytokineReceptorNanotechnologyWorkflowPolitical scienceMolecular modelLipid signalingChemistryStructure–activity relationshipIn vivoProcess engineeringIn silicoOxidative stressFragment (logic)LeukotrieneResveratrolInflammationHeLaThiobarbituric acidProstaglandin E2AntioxidantArachidonic acidBenzodiazepineBenzimidazolePeroxynitrite5-lipoxygenase-activating proteinPiceatannolDrugProstaglandinMTT assayIsoxazoleTubulin Modulators5-Lipoxygenase-Activating Protein InhibitorsCell cycleChemical societyBioactive moleculesNatural resourceScoring methodsIstanbul turkeyNature inspiredKey factorsStructure basedPharmacoinformaticsComputer scienceProcess (engineering)Pipeline (software)ScalabilityRational designBiosynthesisBiochemistryPotencyGlutamate receptorCell growthCheminformaticsComputational biologyStereochemistryDrug discoveryCloud computingCell cultureTubulinBiologyMicrosomeScaffoldArachidonate 5-lipoxygenaseChemical space
Publications 14
#1Tuğba Gürses (Gazi University)
#2Abdurrahman Olgaç (Gazi University)H-Index: 7
Last. Erden Banoglu (Gazi University)H-Index: 20
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Abstract Microsomal prostaglandin E2 synthase-1 (mPGES-1), 5-lipoxygenase (5-LO) and 5- lipoxygenase-activating protein (FLAP) are key for biosynthesis of proinflammatory lipid mediators and pharmacologically relevant drug targets. In the present study, we made an attempt to explore the role of small heteroaromatic fragments on the 4,5-diarylisoxazol-3-carboxylic acid scaffold, which are selected to interact with focused regions in the active sites of mPGES-1, 5-LO and FLAP. We report that the s...
#1Abdurrahman Olgaç (Gazi University)H-Index: 7
#2Andrea Carotti (University of Perugia)H-Index: 21
Last. Erden Banoglu (Gazi University)H-Index: 20
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Leukotrienes (LTs) are proinflammatory mediators derived from arachidonic acid (AA), which play significant roles in inflammatory diseases. 5-lipoxygenase-activating protein (FLAP) is an integral membrane protein, which is essential for the initial step in LT biosynthesis. The aim of this study was to discover novel and chemically diverse FLAP inhibitors for treatment of inflammatory diseases requiring anti-LT therapy. Both ligand- and structure-based approaches have been applied to explain the ...
3 CitationsSource
#1Mohammad Qneibi (An-Najah National University)H-Index: 7
#2Nidal Jaradat (An-Najah National University)H-Index: 16
Last. Nour Emwas (An-Najah National University)H-Index: 4
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2,3-Benzodiazepine compounds are an important family of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) antagonists that act in a noncompetitive manner. Due to the critical role of AMPARs in the synapse and various neurological diseases, significant scientific interest in elucidating the molecular basis of the function of the receptors has spiked. The analogues were synthesized to assess the functional consequence of removing the amine group of the phenyl ring, the potency ...
1 CitationsSource
#1Abdurrahman Olgaç (Gazi University)H-Index: 7
#2Ismail Yalcin (Ankara University)H-Index: 28
Last. Esin Aki-Yalcin (Ankara University)H-Index: 5
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AFMC-AIMECS meetings are internationally organized biannually by the Asian Federation for Medicinal Chemistry (AFMC) and are focused on recent studies in drug discovery and development both in academia and industry. Member organizations of the AFMC are the Pharmaceutical Society of Japan, the Chinese Pharmaceutical Association, the Royal Australian Chemical Institute, the Pharmaceutical Society of Korea, the Korean Chemical Society, the Chemical Society Located in Taipei, the Indonesian Society ...
1 CitationsSource
#2Maria DonniacuoH-Index: 12
Last. Rosanna Filosa (National Research Council)H-Index: 8
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Abstract Stilbenes with well-known antioxidant and antiradical properties are beneficial in different pathologies including cardiovascular diseases. The present research was performed to investigate the potential protective effect of resveratrol (1) and piceatannol (2) , against hypoxia-induced oxidative stress in the H9c2 cardiomyoblast cell line, and the underlying mechanisms. Compounds 1 and 2 significantly inhibited the release of peroxynitrite and thiobarbituric acid levels at na no- or sub...
9 CitationsSource
#1Abdulkarim NajjarH-Index: 5
#2Abdurrahman OlgaçH-Index: 7
Last. Wolfgang SipplH-Index: 59
view all 4 authors...
1 CitationsSource
#1Abdurrahman Olgaç (Gazi University)H-Index: 7
#2Aslı Türe (Marmara University)H-Index: 4
Last. Steffen Möller (University of Rostock)H-Index: 24
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Drug discovery and development requires the integration of multiple scientific and technological disciplines in chemistry, biology and extensive use of information technology. Computer Aided Drug Discovery (CADD) methods are being used in this work area with several different workflows. Virtual screening (VS) is one of the most often applied CADD methods used in rational drug design, which may be applied in early stages of drug discovery pipeline. The increasing number of modular and scalable cl...
6 CitationsSource
#1Ferdinando BrunoH-Index: 5
#2Suann Errico (FSU: University of Jena)H-Index: 1
Last. Rosanna Filosa (National Research Council)H-Index: 8
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Abstract The release of pro-inflammatory mediators, such as prostaglandines (PGs) and leukotrienes (LTs), arising from the arachidonic acid (AA) cascade, play a crucial role in initiating, maintaining, and regulating inflammatory processes. New dual inhibitors of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), that block, at the same time, the formation of PGE2 and LTs, are currently emerged as a highly interesting drug candidates for better pharmacotherapie of inflam...
7 CitationsSource
#1Zehra Tugce Gur (Gazi University)H-Index: 3
#2Burcu Çalışkan (Gazi University)H-Index: 11
Last. Erden Banoglu (Gazi University)H-Index: 20
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Abstract Leukotrienes (LTs) and prostaglandin (PG)E 2 are enzymatically produced from arachidonic acid and represent highly bioactive lipid mediators with pro-inflammatory functions. Here, we report on novel multi-target inhibitors that potently and dually interfere with 5-lipoxygenase-activating protein (FLAP) and microsomal prostaglandin E 2 synthase (mPGES)-1 in LT and PGE 2 biosynthesis, based on the previously identified selective FLAP inhibitor BRP-7 ( 8 , IC 50 = 0.31 μM). C (5)-substitut...
5 CitationsSource
#1Abdurrahman Olgaç (Gazi University)H-Index: 7
#2Ilkay Erdogan Orhan (Gazi University)H-Index: 58
Last. Erden Banoglu (Gazi University)H-Index: 20
view all 3 authors...
In recent years, integration of in silico approaches to natural product (NP) research reawakened the declined interest in NP-based drug discovery efforts. In particular, advancements in cheminformatics enabled comparison of NP databases with contemporary small-molecule libraries in terms of molecular properties and chemical space localizations. Virtual screening and target fishing approaches were successful in recognizing the untold macromolecular targets for NPs to exploit the unmet therapeutic...
14 CitationsSource