Abdurrahman Olğaç

Abdurrahman Olğaç
Gazi University · Department of Pharmaceutical Chemistry

PhD

About

25
Publications
4,913
Reads
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188
Citations
Education
September 2012 - August 2017
Gazi University
Field of study
  • Pharmaceutical Chemistry

Publications

Publications (25)
Chapter
Full-text available
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 m...
Article
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...
Article
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 inhi...
Article
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-carb...
Article
Cardiovascular diseases are the primary reason for deaths in the world. However, antiplatelet drugs in the market have limitations in use because of the risk of increased bleeding and other side effects that impair primary homeostasis. Therefore, safe and effective antithrombotic drugs are needed for the treatment of plaque formation in blood vesse...
Article
Soluble epoxide hydrolase (sEH) is implicated as a potential therapeutic target for inflammation‐related pathologies in the context of cardiovascular, central nervous system and metabolic diseases. In our search for novel sEH inhibitors, we designed and synthesized novel analogs of the piperazine urea derivative 4, a previously discovered dual micr...
Article
Microsomal prostaglandin E2 synthase-1 (mPGES-1) is recognized as a promising therapeutic target for next-generation anti-inflammatory drugs to treat inflammatory diseases. In this study, we report the identification of new, potent and selective inhibitors of human mPGES-1 such as compounds 10, 31 and 49 with IC50 of 0.03–0.09 μM in a cell-free ass...
Article
Novel compounds containing polar and nonpolar substitutions on the prop-2-en-1-on linker of the trans-indol-3-ylacrylamide scaffold were designed by modeling within the colchicine site of tubulin and then synthesized to determine the role of such substitutions on tubulin polymerization. We first determined the in vitro antiproliferation activities...
Poster
Interleukin-2 (IL-2) is an immunostimulatory cytokine and interacts with IL-2 receptors (IL-2Rs); IL-2Rα, IL-2Rβ, and ƴc receptor. IL-2 binds to β, γ receptors for fighting cancer or α, β, γ receptors for autoimmune diseases [1]. Aldesleukin was the therapeutic version of IL-2 and developed with minor modifications to the sequence of IL-2. There ar...
Article
Full-text available
ABSTRACT An individual's athletic ability is influenced by genetic and environmental factors. Some mitochondrial haplogroups and polymorphisms have been shown to be associated with human performance. The aim of this study is to asses whether the frequency distribution of mitochondrial haplogroups is an association between elite Turkish wrestlers a...
Article
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...
Article
Natural product-derived drugs can be extracts, biological macromolecules or purified small molecule substances. Small molecule drugs can be originally purified from natural products (NPs), can represent semi-synthetic molecules, natural fragment containing small molecules or are fully synthetic molecules that mimic natural compounds. New semi-synth...
Article
Leukotrienes (LTs) and prostaglandin (PG)E2are 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 E2synthase (mPGES)-...
Article
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. Vir...
Article
Pharmacological intervention with 5-lipoxygenase (5-LO) pathway leading to suppression of leukotriene (LT) biosynthesis is a clinically validated strategy for treatment of respiratory and cardiovascular diseases such as asthma and atherosclerosis. Here we describe the synthesis of a series of C(5)-substituted analogues of the previously described 5...
Article
In this article, we report novel leukotriene (LT) biosynthesis inhibitors that may target 5-lipoxygenase-activating protein (FLAP) based on the previously identified isoxazole derivative (8). The design and synthesis was directed towards a subset of 4,5-diaryl-isoxazole-3-carboxylic acid derivatives as LT biosynthesis inhibitors. Biological evaluat...
Conference Paper
Full-text available
Introduction: Sequence analysis of human mitochondrial DNA has been demonstrated to be a valid and reliable tool for discriminating between unrelated individuals. Noncoding, displacement (D) loop contains two hypervariable regions, HV I and HV II. These regions are highly polymorphic. The HV regions have been used extensively in forensic investigat...

Questions

Questions (2)
Question
I am planning to make a molecular dynamics simulation by embedding my protein into nuclear membrane, to study interactions in active site. But I couldn't find any solution to put lipids different for nuclear membrane rather than cellular membrane. If possible I am interested in building system with Maestro to use Desmond.
Question
I am planning to make a virtual screening to find a second target for a ligand that we developed before. What is the fastest and easiest way the way to do it? I've found some solutions for AutoDock but they look hard to do. If possible I am interested in doing it with Glide or Gold.

Projects

Projects (2)
Project
The textbook presents an overview of natural products chemistry, discussing the chemical space of naturally occurring compounds, followed by an overview of computational methods and currently available tools for structure elucidation, drug property prediction, natural product databases, lead identification, metabolite biosynthesis, etc. Selected case studies are discussed.
Project
Developing 5-Lipoxygenase (5-LO), 5-Lipoxygenase Activating Protein (FLAP) and microsomal Prostaglandine E2 Synthase-1 (mPGES-1) inhibitors by combination of structure-based and ligand-based methods.