Protein and Small-Molecule Leucopoiesis and Thrombopoiesis
Stimulators

J 2021

Protein and Small-Molecule Leucopoiesis and Thrombopoiesis Stimulators

FARSA, Oldřich and Peter ZUBÁČ

Basic information

Original name

Protein and Small-Molecule Leucopoiesis and Thrombopoiesis Stimulators

Authors

FARSA, Oldřich (203 Czech Republic, guarantor, belonging to the institution) and Peter ZUBÁČ (703 Slovakia, belonging to the institution)

Edition

Mini-reviews in medicinal chemistry, Sharjah, Betham Science Publ Ltd. 2021, 1389-5575

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30107 Medicinal chemistry

Country of publisher

United Arab Emirates

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

URL

Impact factor

Impact factor: 3.737

RIV identification code

RIV/00216224:14160/21:00121966

Organization unit

Faculty of Pharmacy

DOI

http://dx.doi.org/10.2174/1389557521999201230195926

UT WoS

000671552600004

Keywords in English

Colony-stimulating factors; stem-cell factors; pegylation; plerixafor; thrombopoietin; romiplostim; eltrombopag

Abstract

V originále

Compounds stimulating the production of various types of blood cells are very important medicaments used in serious pathologies. This review article is devoted to compounds stimulating the production of different white blood cells and blood platelets. For the structure, most of them, mainly natural blood cells production stimulators and their derivatives, belong among so-called biotherapeutics or, following the definition of the World Health Organization (WHO), biologic and biotechnological substances [1]. They are in most pro Pluripotent stem cells of the bone marrow are stimulated by different cytokines to proliferation and differentiation into various types of blood cells. These cytokines are mostly glycoproteins. Erythropoietin stimulates stem cells to the formation of erythrocytes while colony-stimulating factors cause the formation of different types of white blood cells. Stem cell factors play an important role in the maintenance and survival of blood cells of all types. Thrombopoietin stimulates stem cells to proliferation and formation of blood platelets. Granulocyte colony-stimulating factor is probably the most important drug in use. It stimulates stem cells to the formation of neutrophile granulocytes. It is often used in recombinant forms such as filgrastim in the treatment of neutropenia in cancer chemotherapy or AIDS. Its pegylated conjugates such as pegfilgrastim are also available. Its activity can be supported by plerixafor, a small molecule - bicyclam derivative acting as an indirect agonist of stem cells factor. It acts as an antagonist of CXCR4 receptor activation of which brakes hematopoiesis. The treatment of conditions accompanied by thrombocytopenia such as idiopathic thrombocytopenic purpura is currently not performed by thrombopoietin but synthetic agonists of its receptor are preferred. Romiplostim is a peptibody. It consists of a protein part interacting with the thrombopoietin receptor which is, however, different from thrombopoietin, and of Fc fragment of immunoglobulin G1. In contrast, small molecule thrombopoietin receptor agonists represented by eltrombopag can be given orally unlike all of the above. important drug in use. It stimulates stem cells to the formation of neutrophile granulocytes. It is often used in recombinant forms such as filgrastim in the treatment of neutropenia in cancer chemotherapy or AIDS. Its pegylated conjugates such as pegfilgrastim are also available. Its activity can be supported by plerixafor, a small molecule - bicyclam derivative acting as an indirect agonist of stem cells factor. It acts as an antagonist of CXCR4 receptor activation of which brakes hematopoiesis. The treatment of conditions accompanied by thrombocytopenia such as idiopathic thrombocytopenic purpura is currently not performed by thrombopoietin but synthetic agonists of its receptor are preferred. Romiplostim is a peptibody. It consists of a protein part interacting with the thrombopoietin receptor which is, however, different from thrombopoietin, and of Fc fragment of immunoglobulin G1. In contrast, small molecule thrombopoietin receptor agonists represented by eltrombopag can be given orally unlike all of the above.

Citovat

FARSA, Oldřich and Peter ZUBÁČ. Protein and Small-Molecule Leucopoiesis and Thrombopoiesis Stimulators. Mini-reviews in medicinal chemistry. Sharjah: Betham Science Publ Ltd., 2021, vol. 21, No 13, p. 1638-1645. ISSN 1389-5575. Available from: https://dx.doi.org/10.2174/1389557521999201230195926.

@article{1783497,
   author = {Farsa, Oldřich and Zubáč, Peter},
   article_location = {Sharjah},
   article_number = {13},
   doi = {http://dx.doi.org/10.2174/1389557521999201230195926},
   keywords = {Colony-stimulating factors; stem-cell factors; pegylation; plerixafor; thrombopoietin; romiplostim; eltrombopag},
   language = {eng},
   issn = {1389-5575},
   journal = {Mini-reviews in medicinal chemistry},
   title = {Protein and Small-Molecule Leucopoiesis and Thrombopoiesis Stimulators},
   url = {https://www.eurekaselect.com/189654/article},
   volume = {21},
   year = {2021}
}

TY  - JOUR
ID  - 1783497
AU  - Farsa, Oldřich - Zubáč, Peter
PY  - 2021
TI  - Protein and Small-Molecule Leucopoiesis and Thrombopoiesis Stimulators
JF  - Mini-reviews in medicinal chemistry
VL  - 21
IS  - 13
SP  - 1638-1645
EP  - 1638-1645
PB  - Betham Science Publ Ltd.
SN  - 13895575
KW  - Colony-stimulating factors
KW  - stem-cell factors
KW  - pegylation
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KW  - eltrombopag
UR  - https://www.eurekaselect.com/189654/article
N2  - Compounds stimulating the production of various types of blood cells are very important medicaments used in serious pathologies. This review article is devoted to compounds stimulating the production of different white blood cells and blood platelets. For the structure, most of them, mainly natural blood cells production stimulators and their derivatives, belong among so-called biotherapeutics or, following the definition of the World Health Organization (WHO), biologic and biotechnological substances [1]. They are in most pro Pluripotent stem cells of the bone marrow are stimulated by different cytokines to proliferation and differentiation into various types of blood cells. These cytokines are mostly glycoproteins. Erythropoietin stimulates stem cells to the formation of erythrocytes while colony-stimulating factors cause the formation of different types of white blood cells. Stem cell factors play an important role in the maintenance and survival of blood cells of all types. Thrombopoietin stimulates stem cells to proliferation and formation of blood platelets. Granulocyte colony-stimulating factor is probably the most important drug in use. It stimulates stem cells to the formation of neutrophile granulocytes. It is often used in recombinant forms such as filgrastim in the treatment of neutropenia in cancer chemotherapy or AIDS. Its pegylated conjugates such as pegfilgrastim are also available. Its activity can be supported by plerixafor, a small molecule - bicyclam derivative acting as an indirect agonist of stem cells factor. It acts as an antagonist of CXCR4 receptor activation of which brakes hematopoiesis. The treatment of conditions accompanied by thrombocytopenia such as idiopathic thrombocytopenic purpura is currently not performed by thrombopoietin but synthetic agonists of its receptor are preferred. Romiplostim is a peptibody. It consists of a protein part interacting with the thrombopoietin receptor which is, however, different from thrombopoietin, and of Fc fragment of immunoglobulin G1. In contrast, small molecule thrombopoietin receptor agonists represented by eltrombopag can be given orally unlike all of the above. important drug in use. It stimulates stem cells to the formation of neutrophile granulocytes. It is often used in recombinant forms such as filgrastim in the treatment of neutropenia in cancer chemotherapy or AIDS. Its pegylated conjugates such as pegfilgrastim are also available. Its activity can be supported by plerixafor, a small molecule - bicyclam derivative acting as an indirect agonist of stem cells factor. It acts as an antagonist of CXCR4 receptor activation of which brakes hematopoiesis. The treatment of conditions accompanied by thrombocytopenia such as idiopathic thrombocytopenic purpura is currently not performed by thrombopoietin but synthetic agonists of its receptor are preferred. Romiplostim is a peptibody. It consists of a protein part interacting with the thrombopoietin receptor which is, however, different from thrombopoietin, and of Fc fragment of immunoglobulin G1. In contrast, small molecule thrombopoietin receptor agonists represented by eltrombopag can be given orally unlike all of the above.
ER  -

FARSA, Oldřich and Peter ZUBÁČ. Protein and Small-Molecule Leucopoiesis and Thrombopoiesis Stimulators. \textit{Mini-reviews in medicinal chemistry}. Sharjah: Betham Science Publ Ltd., 2021, vol.~21, No~13, p.~1638-1645. ISSN~1389-5575. Available from: https://dx.doi.org/10.2174/1389557521999201230195926.

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