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Article: Design, Synthesis, and Antitumor Evaluation of an Opioid Growth Factor Bioconjugate Targeting Pancreatic Ductal Adenocarcinoma.

Budka, Justyna / Debowski, Dawid / Mai, Shaoshan / Narajczyk, Magdalena / Hac, Stanislaw / Rolka, Krzysztof / Vrettos, Eirinaios I / Tzakos, Andreas G / Inkielewicz-Stepniak, Iwona

Pharmaceutics

2024 Volume 16, Issue 2

Abstract: Pancreatic ductal adenocarcinoma (PDAC) presents a formidable challenge with high lethality and limited effective drug treatments. Its heightened metastatic potential further complicates the prognosis. Owing to the significant toxicity of current ... ...

Abstract	Pancreatic ductal adenocarcinoma (PDAC) presents a formidable challenge with high lethality and limited effective drug treatments. Its heightened metastatic potential further complicates the prognosis. Owing to the significant toxicity of current chemotherapeutics, compounds like [Met
Language	English
Publishing date	2024-02-16
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics16020283
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Vasopressin and Its Analogues: From Natural Hormones to Multitasking Peptides.

Glavaš, Mladena / Gitlin-Domagalska, Agata / Dębowski, Dawid / Ptaszyńska, Natalia / Łęgowska, Anna / Rolka, Krzysztof

International journal of molecular sciences

2022 Volume 23, Issue 6

Abstract: Human neurohormone vasopressin (AVP) is synthesized in overlapping regions in the hypothalamus. It is mainly known for its vasoconstricting abilities, and it is responsible for the regulation of plasma osmolality by maintaining fluid homeostasis. Over ... ...

Abstract	Human neurohormone vasopressin (AVP) is synthesized in overlapping regions in the hypothalamus. It is mainly known for its vasoconstricting abilities, and it is responsible for the regulation of plasma osmolality by maintaining fluid homeostasis. Over years, many attempts have been made to modify this hormone and find AVP analogues with different pharmacological profiles that could overcome its limitations. Non-peptide AVP analogues with low molecular weight presented good affinity to AVP receptors. Natural peptide counterparts, found in animals, are successfully applied as therapeutics; for instance, lypressin used in treatment of diabetes insipidus. Synthetic peptide analogues compensate for the shortcomings of AVP. Desmopressin is more resistant to proteolysis and presents mainly antidiuretic effects, while terlipressin is a long-acting AVP analogue and a drug recommended in the treatment of varicose bleeding in patients with liver cirrhosis. Recently published results on diverse applications of AVP analogues in medicinal practice, including potential lypressin, terlipressin and ornipressin in the treatment of SARS-CoV-2, are discussed.
MeSH term(s)	Animals ; Antidiuretic Agents/chemistry ; Antidiuretic Agents/metabolism ; Antidiuretic Agents/therapeutic use ; COVID-19/drug therapy ; COVID-19/epidemiology ; COVID-19/virology ; Deamino Arginine Vasopressin/chemistry ; Deamino Arginine Vasopressin/metabolism ; Deamino Arginine Vasopressin/therapeutic use ; Diabetes Insipidus/metabolism ; Diabetes Insipidus/prevention & control ; Hemostatics/chemistry ; Hemostatics/metabolism ; Hemostatics/therapeutic use ; Humans ; Lypressin/chemistry ; Lypressin/metabolism ; Lypressin/therapeutic use ; Molecular Structure ; Ornipressin/chemistry ; Ornipressin/metabolism ; Ornipressin/therapeutic use ; Pandemics/prevention & control ; SARS-CoV-2/drug effects ; SARS-CoV-2/metabolism ; SARS-CoV-2/physiology ; Terlipressin/chemistry ; Terlipressin/metabolism ; Terlipressin/therapeutic use ; Vasopressins/chemistry ; Vasopressins/metabolism ; Vasopressins/therapeutic use
Chemical Substances	Antidiuretic Agents ; Hemostatics ; Vasopressins (11000-17-2) ; Ornipressin (1KTH6N080W) ; Lypressin (50-57-7) ; Terlipressin (7Z5X49W53P) ; Deamino Arginine Vasopressin (ENR1LLB0FP)
Language	English
Publishing date	2022-03-12
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2019364-6
ISSN	1422-0067 ; 1422-0067 ; 1661-6596
ISSN (online)	1422-0067
ISSN	1422-0067 ; 1661-6596
DOI	10.3390/ijms23063068
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry.

Gitlin-Domagalska, Agata / Dębowski, Dawid / Maciejewska, Aleksandra / Samsonov, Sergey / Maszota-Zieleniak, Martyna / Ptaszyńska, Natalia / Łęgowska, Anna / Rolka, Krzysztof

ACS medicinal chemistry letters

2023 Volume 14, Issue 4, Page(s) 458–465

Abstract: Furin is a human serine protease responsible for activating numerous physiologically relevant cell substrates and is also involved in the development of various pathological conditions, including inflammatory diseases, cancers, and viral and bacterial ... ...

Abstract	Furin is a human serine protease responsible for activating numerous physiologically relevant cell substrates and is also involved in the development of various pathological conditions, including inflammatory diseases, cancers, and viral and bacterial infections. Therefore, compounds with the ability to inhibit furin's proteolytic action are regarded as potential therapeutics. Here we took the combinatorial chemistry approach (library consisting of 2000 peptides) to obtain new, strong, and stable peptide furin inhibitors. The extensively studied trypsin inhibitor SFTI-1 was used as a leading structure. A selected monocylic inhibitor was further modified to finally yield five mono- or bicyclic furin inhibitors with values of
Language	English
Publishing date	2023-03-15
Publishing country	United States
Document type	Journal Article
ISSN	1948-5875
ISSN	1948-5875
DOI	10.1021/acsmedchemlett.3c00008
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Lactoferricin B Combined with Antibiotics Exhibits Leukemic Selectivity and Antimicrobial Activity.

Lica, Jan Jakub / Gucwa, Katarzyna / Heldt, Mateusz / Stupak, Anna / Maciejewska, Natalia / Ptaszyńska, Natalia / Łęgowska, Anna / Pradhan, Bhaskar / Gitlin-Domagalska, Agata / Dębowski, Dawid / Jakóbkiewicz-Banecka, Joanna / Rolka, Krzysztof

Molecules (Basel, Switzerland)

2024 Volume 29, Issue 3

Abstract: The fusion of penetrating peptides (PPs), e.g., cell penetration peptides (CPPs) or antimicrobial peptides (AMPs), together with antimicrobial agents is an expanding research field. Specific AMPs, such as lactoferricin B (LfcinB), have demonstrated ... ...

Abstract	The fusion of penetrating peptides (PPs), e.g., cell penetration peptides (CPPs) or antimicrobial peptides (AMPs), together with antimicrobial agents is an expanding research field. Specific AMPs, such as lactoferricin B (LfcinB), have demonstrated strong antibacterial, antifungal, and antiparasitic activity, as well as valuable anticancer activity, proving beneficial in the development of anticancer conjugates. The resulting conjugates offer potential dual functionality, acting as both an anticancer and an antimicrobial agent. This is especially necessary in cancer treatment, where microbial infections pose a critical risk. Leukemic cells frequently exhibit altered outer lipid membranes compared to healthy cells, making them more sensitive to compounds that interfere with their membrane. In this study, we revisited and reanalyzed our earlier research on LfcinB and its conjugates. Furthermore, we carried out new experiments with a specific focus on cell proliferation, changes in membrane asymmetric phosphatidylserine location, intracellular reactive oxygen species (ROS) generation, mitochondrial functions, and in vitro bacterial topoisomerase inhibition.
MeSH term(s)	Anti-Bacterial Agents/pharmacology ; Lactoferrin/pharmacology ; Lactoferrin/chemistry ; Anti-Infective Agents/pharmacology ; Peptides/chemistry ; Microbial Sensitivity Tests
Chemical Substances	lactoferricin B (146897-68-9) ; Anti-Bacterial Agents ; Lactoferrin (EC 3.4.21.-) ; Anti-Infective Agents ; Peptides
Language	English
Publishing date	2024-02-01
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules29030678
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Book ; Conference proceedings: Peptides 2006

Rolka, Krzysztof

proceedings of the Twenty-Ninth European Peptide Symposium, September 3 - 8, 2006, Gdansk, Poland

2007

Institution	European Peptide Society
Event/congress	EPS (29, 2006.09.03-08, Gdansk) ; European Peptide Symposium (29, 2006.09.03-08, Gdansk)
Author's details	[European Peptide Society]. Ed. by Krzysztof Rolka
Language	English
Size	LII, 843 S., Ill., graph. Darst.
Publisher	Kenes Internat
Publishing place	Geneva
Document type	Book ; Conference proceedings
ISBN	9789655552973 ; 9655552977
Database	Library catalogue of the German National Library of Science and Technology (TIB), Hannover

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Article: New Peptide Based Fluconazole Conjugates with Expanded Molecular Targets.

Brankiewicz, Wioletta / Okońska, Joanna / Serbakowska, Katarzyna / Lica, Jan / Drab, Marek / Ptaszyńska, Natalia / Łęgowska, Anna / Rolka, Krzysztof / Szweda, Piotr

Pharmaceutics

2022 Volume 14, Issue 4

Abstract: Infections ... ...

Abstract	Infections of
Language	English
Publishing date	2022-03-23
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics14040693
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Synthesis of Novel Arginine Building Blocks with Increased Lipophilicity Compatible with Solid-Phase Peptide Synthesis.

Glavaš, Mladena / Gitlin-Domagalska, Agata / Ptaszyńska, Natalia / Starego, Dominika / Freza, Sylwia / Dębowski, Dawid / Helbik-Maciejewska, Aleksandra / Łęgowska, Anna / Gilon, Chaim / Rolka, Krzysztof

Molecules (Basel, Switzerland)

2023 Volume 28, Issue 23

Abstract: Arginine, due to the guanidine moiety, increases peptides' hydrophilicity and enables interactions with charged molecules, but at the same time, its presence in a peptide chain might reduce its permeability through biological membranes. This might be ... ...

Abstract	Arginine, due to the guanidine moiety, increases peptides' hydrophilicity and enables interactions with charged molecules, but at the same time, its presence in a peptide chain might reduce its permeability through biological membranes. This might be resolved by temporary coverage of the peptide charge by lipophilic, enzyme-sensitive alkoxycarbonyl groups. Unfortunately, such a modification of a guanidine moiety has not been reported to date and turned out to be challenging. Here, we present a new, optimized strategy to obtain arginine building blocks with increased lipophilicity that were successfully utilized in the solid-phase peptide synthesis of novel arginine vasopressin prodrugs.
MeSH term(s)	Arginine/chemistry ; Solid-Phase Synthesis Techniques ; Peptides/chemistry ; Guanidines
Chemical Substances	Arginine (94ZLA3W45F) ; Peptides ; Guanidines
Language	English
Publishing date	2023-11-25
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules28237780
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Article: Can Immobilized Artificial Membrane Chromatography Support the Characterization of Antimicrobial Peptide Origin Derivatives?

Ciura, Krzesimir / Ptaszyńska, Natalia / Kapica, Hanna / Pastewska, Monika / Łęgowska, Anna / Rolka, Krzysztof / Kamysz, Wojciech / Sawicki, Wiesław / Greber, Katarzyna E

Antibiotics (Basel, Switzerland)

2021 Volume 10, Issue 10

Abstract: The emergence and spread of multiple drug-resistant bacteria strains caused the development of new antibiotics to be one of the most important challenges of medicinal chemistry. Despite many efforts, the commercial availability of peptide-based ... ...

Abstract	The emergence and spread of multiple drug-resistant bacteria strains caused the development of new antibiotics to be one of the most important challenges of medicinal chemistry. Despite many efforts, the commercial availability of peptide-based antimicrobials is still limited. The presented study aims to explain that immobilized artificial membrane chromatography can support the characterization of antimicrobial peptides. Consequently, the chromatographic experiments of three groups of related peptide substances: (i) short cationic lipopeptides, (ii) citropin analogs, and (iii) conjugates of ciprofloxacin and levofloxacin, with a cell-penetrating peptide were discussed. In light of the discussion of the mechanisms of action of these compounds, the obtained results were interpreted.
Language	English
Publishing date	2021-10-12
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2681345-2
ISSN	2079-6382
ISSN	2079-6382
DOI	10.3390/antibiotics10101237
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Dual-Activity Fluoroquinolone-Transportan 10 Conjugates Offer Alternative Leukemia Therapy during Hematopoietic Cell Transplantation.

Lica, Jan Jakub / Heldt, Mateusz / Wieczór, Milosz / Chodnicki, Pawel / Ptaszyńska, Natalia / Maciejewska, Natalia / Łęgowska, Anna / Brankiewicz, Wioletta / Gucwa, Katarzyna / Stupak, Anna / Pradhan, Bhaskar / Gitlin-Domagalska, Agata / Dębowski, Dawid / Milewski, Sławomir / Bieniaszewska, Maria / Grabe, Grzegorz Jan / Hellmann, Andrzej / Rolka, Krzysztof

Molecular pharmacology

2023 Volume 105, Issue 1, Page(s) 39–53

Abstract: Hematopoietic cell transplantation (HCT) is often considered a last resort leukemia treatment, fraught with limited success due to microbial infections, a leading cause of mortality in leukemia patients. To address this critical issue, we explored a ... ...

Abstract	Hematopoietic cell transplantation (HCT) is often considered a last resort leukemia treatment, fraught with limited success due to microbial infections, a leading cause of mortality in leukemia patients. To address this critical issue, we explored a novel approach by synthesizing antileukemic agents containing antibacterial substances. This innovative strategy involves conjugating fluoroquinolone antibiotics, such as ciprofloxacin (CIP) or levofloxacin (LVX), with the cell-penetrating peptide transportan 10 (TP10). Here, we demonstrate that the resultant compounds display promising biologic activities in preclinical studies. These novel conjugates not only exhibit potent antimicrobial effects but are also selective against leukemia cells. The cytotoxic mechanism involves rapid disruption of cell membrane asymmetry leading to membrane damage. Importantly, these conjugates penetrated mammalian cells, accumulating within the nuclear membrane without significant effect on cellular architecture or mitochondrial function. Molecular simulations elucidated the aggregation tendencies of TP10 conjugates within lipid bilayers, resulting in membrane disruption and permeabilization. Moreover, mass spectrometry analysis confirmed efficient reduction of disulfide bonds within TP10 conjugates, facilitating release and activation of the fluoroquinolone derivatives. Intriguingly, these compounds inhibited human topoisomerases, setting them apart from traditional fluoroquinolones. Remarkably, TP10 conjugates generated lower intracellular levels of reactive oxygen species compared with CIP and LVX. The combination of antibacterial and antileukemic properties, coupled with selective cytostatic effects and minimal toxicity toward healthy cells, positions TP10 derivatives as promising candidates for innovative therapeutic approaches in the context of antileukemic HCT. This study highlights their potential in search of more effective leukemia treatments. SIGNIFICANCE STATEMENT: Fluoroquinolones are commonly used antibiotics, while transportan 10 (TP10) is a cell-penetrating peptide (CPP) with anticancer properties. In HCT, microbial infections are the primary cause of illness and death. Combining TP10 with fluoroquinolones enhanced their effects on different cell types. The dual pharmacological action of these conjugates offers a promising proof-of-concept solution for leukemic patients undergoing HCT. Strategically designed therapeutics, incorporating CPPs with antibacterial properties, have the potential to reduce microbial infections in the treatment of malignancies.
MeSH term(s)	Animals ; Humans ; Fluoroquinolones/pharmacology ; Cell-Penetrating Peptides/pharmacology ; Cell-Penetrating Peptides/chemistry ; Cell-Penetrating Peptides/metabolism ; Antineoplastic Agents/pharmacology ; Anti-Bacterial Agents/pharmacology ; Leukemia/drug therapy ; Cell Transplantation ; Mammals/metabolism
Chemical Substances	transportan ; Fluoroquinolones ; Cell-Penetrating Peptides ; Antineoplastic Agents ; Anti-Bacterial Agents
Language	English
Publishing date	2023-12-15
Publishing country	United States
Document type	Journal Article
ZDB-ID	124034-1
ISSN	1521-0111 ; 0026-895X
ISSN (online)	1521-0111
ISSN	0026-895X
DOI	10.1124/molpharm.123.000735
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Zs.A 525: Show issues

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Article ; Online: Correction: Stability of Cu(II) complexes with FomA protein fragments containing two His residues in the peptide chain.

Lesiów, Monika Katarzyna / Pietrzyk, Piotr / Bieńko, Alina / Kowalik-Jankowska, Teresa / Łęgowska, Anna / Ptaszyńska, Natalia / Rolka, Krzysztof

Metallomics : integrated biometal science

2020 Volume 12, Issue 12, Page(s) 2199

Abstract: Correction for 'Stability of Cu(ii) complexes with FomA protein fragments containing two His residues in the peptide chain' by Monika Katarzyna Lesiów et al., Metallomics, 2019, 11, 1518-1531, DOI: 10.1039/C9MT00131J. ...

Abstract	Correction for 'Stability of Cu(ii) complexes with FomA protein fragments containing two His residues in the peptide chain' by Monika Katarzyna Lesiów et al., Metallomics, 2019, 11, 1518-1531, DOI: 10.1039/C9MT00131J.
Language	English
Publishing date	2020-12-15
Publishing country	England
Document type	Published Erratum
ZDB-ID	2474317-3
ISSN	1756-591X ; 1756-5901
ISSN (online)	1756-591X
ISSN	1756-5901
DOI	10.1039/d0mt90038a
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