Serhii Holota

Dr. Serhii Holota

Molecular Design Center, Danylo Halytsky Lviv National Medical University, Lviv, L’vivs’ka Oblast’, Ukraine
orcid

Research Focus & Metrics

Academic Career Length

20Years (2007-Present)

(Calculated once Scilit publication data is synced: current year − year of first publication + 1)

Representative Publications

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1 May 2007 in European Journal of Medicinal Chemistry
Verified
Journal Article
Closed access
Roman LesykRoman Lesyk
Roman Lesyk
OVOlena Vladzimirska
Olena Vladzimirska
Serhii HolotaSerhii Holota
Serhii Holota
Lucjusz ZaprutkoLucjusz Zaprutko
Lucjusz Zaprutko
AGAndrzej Gzella
Andrzej Gzella

5 February 2020 in Antioxidants
Verified
Journal Article
Open access
PDF file
Andriy CherkasAndriy Cherkas
Andriy Cherkas
Serhii HolotaSerhii Holota
Serhii Holota
TMTamaz Mdzinarashvili
Tamaz Mdzinarashvili
Rosita GabbianelliRosita Gabbianelli
Rosita Gabbianelli
Neven ZarkovicNeven Zarkovic
Neven Zarkovic
A human organism depends on stable glucose blood levels in order to maintain its metabolic needs. Glucose is considered to be the most important energy source, and glycolysis is postulated as a backbone pathway. However, when the glucose supply is limited, ketone bodies and amino acids can be used to produce enough ATP. In contrast, for the functioning of the pentose phosphate pathway (PPP) glucose is essential and cannot be substituted by other metabolites. The PPP generates and maintains the levels of nicotinamide adenine dinucleotide phosphate (NADPH) needed for the reduction in oxidized glutathione and protein thiols, the synthesis of lipids and DNA as well as for xenobiotic detoxification, regulatory redox signaling and counteracting infections. The flux of glucose into a PPP—particularly under extreme oxidative and toxic challenges—is critical for survival, whereas the glycolytic pathway is primarily activated when glucose is abundant, and there is lack of NADP+ that is required for the activation of glucose-6 phosphate dehydrogenase. An important role of glycogen stores in resistance to oxidative challenges is discussed. Current evidences explain the disruptive metabolic effects and detrimental health consequences of chronic nutritional carbohydrate overload, and provide new insights into the positive metabolic effects of intermittent fasting, caloric restriction, exercise, and ketogenic diet through modulation of redox homeostasis.

Verified
Journal Article
Open access
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Piotr RoszczenkoPiotr Roszczenko
Piotr Roszczenko
Serhii HolotaSerhii Holota
Serhii Holota
OSOlga Klaudia Szewczyk-Roszczenko
Olga Klaudia Szewczyk-Roszczenko
RDRostyslav Dudchak
Rostyslav Dudchak
KBKrzysztof Bielawski
Krzysztof Bielawski
Roman LesykRoman Lesyk
Roman Lesyk
Oncological diseases have currently reached an epidemic scale, especially in industrialized countries. Such a situation has prompted complex studies in medicinal chemistry focused on the research and development of novel effective anticancer drugs. In this review, the data concerning new 4-thiazolidinone-bearing hybrid molecules with potential anticancer activity reported during the period from the years 2017–2022 are summarized. The main emphasis is on the application of molecular hybridization methodologies and strategies in the design of small molecules as anticancer agents. Based on the analyzed data, it was observed that the main directions in this field are the hybridization of scaffolds, the hybrid-pharmacophore approach, and the analogue-based drug design of 4-thiazolidinone cores with early approved drugs, natural compounds, and privileged heterocyclic scaffolds. The mentioned design approaches are effective tools/sources for the generation of hit/lead compounds with anticancer activity and will be relevant to future studies.

19 September 2023 in Cells
Verified
Journal Article
Open access
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OSOlga Klaudia Szewczyk-Roszczenko
Olga Klaudia Szewczyk-Roszczenko
Piotr RoszczenkoPiotr Roszczenko
Piotr Roszczenko
ASAnna Shmakova
Anna Shmakova
Nataliya FiniukNataliya Finiuk
Nataliya Finiuk
Serhii HolotaSerhii Holota
Serhii Holota
KBKrzysztof Bielawski
Krzysztof Bielawski
Endocytosis is one of the major ways cells communicate with their environment. This process is frequently hijacked by pathogens. Endocytosis also participates in the oncogenic transformation. Here, we review the approaches to inhibit endocytosis, discuss chemical inhibitors of this process, and discuss potential clinical applications of the endocytosis inhibitors.

1 May 2019 in Bioorganic Chemistry
Verified
Journal Article
Closed access
Serhii HolotaSerhii Holota
Serhii Holota
AKAnna P. Kryshchyshyn-Dylevych
Anna P. Kryshchyshyn-Dylevych
HDHalyna Derkach
Halyna Derkach
YTYaroslava Trufin
Yaroslava Trufin
IDInna Demchuk
Inna Demchuk
Roman LesykRoman Lesyk
Roman Lesyk

10 January 2024 in Molecules
Verified
Journal Article
Open access
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Sara JanowskaSara Janowska
Sara Janowska
Serhii HolotaSerhii Holota
Serhii Holota
Roman LesykRoman Lesyk
Roman Lesyk
Monika WujecMonika Wujec
Monika Wujec
Aromatase is an enzyme that plays a crucial role in the biosynthesis of estrogens, which are hormones that contribute to the growth of certain types of breast cancer. In particular, aromatase catalyzes the conversion of androgens (male hormones) into estrogens (female hormones) in various tissues, including the adrenal glands, ovaries, and adipose tissue. Given the role of estrogen in promoting the growth of hormone-receptor-positive breast cancers, aromatase has become an important molecular target for the development of anticancer agents. Aromatase inhibitors can be classified into two main groups based on their chemical structure: steroidal and non-steroidal inhibitors. This work presents a review of the literature from the last ten years regarding the search for new aromatase inhibitors. We present the directions of search, taking into account the impact of structure modifications on anticancer activity.