Joanna Bakala - Academia.edu (original) (raw)

Papers by Joanna Bakala

La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, ... more La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, A1 est le radical correspondant a D- ou L- Ser, A2 est le radical correspondant a D- ou L- Asp ou Glu, A3 est le radical correspondant a D- ou L- Lys, Arg ou Orn, A4 est le radical correspondant a D- ou L- Pro, R1 et R2 sont choisis independamment parmi H, C1-C12-alkyle substitue ou non, C7-C20-arylalkyle substitue ou non, R4CO ou R4COO, R4 etant C1-C12-alkyle sustitue ou non, C7-C20-arylalkyle substitue ou non, parmi les substitutions il faut citer OH, NH2 ou COOH, X1 et X2 sont des liaisons peptidiques ou pseudopeptidiques, X3 est CO ou CH2 et R3 est OH, NH2, C1-C12-alcoxy ou NH-X4-CH2-Z, X4 est un C1-C12-hydrocarbone normal ou ramifie, Z est H, OH, CO2H ou CONH2, ou bien les tripeptides correspondants comprenant les radicaux A1, A2, A3, ainsi que les sels pharmaceuticement acceptables, pour la realisation d'un medicament destine au traitement des pathologies pouvant beneficier d&#...

STEM CELLS, 1999

The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP), an inhibitor of hematopoietic stem cell proli... more The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP), an inhibitor of hematopoietic stem cell proliferation, is known to reduce in vivo the damage resulting from treatment with chemotherapeutic agents or ionizing radiation on the stem cell compartment. Recently, AcSDKP has been shown to be a physiological substrate of the N-active site of angiotensin I-converting enzyme (ACE). Four analogs of the tetrapeptide expressing a high stability towards ACE degradation in vitro have been synthesized in order to provide new molecules likely to improve the myeloprotection displayed by AcSDKP. These analogs are three pseudopeptides with a modified peptidic bond, Ac-Serpsi(CH2-NH)Asp-Lys-Pro, Ac-Ser-Asppsi(CH2-NH)Lys-Pro, Ac-Ser-Asp-Lyspsi(CH2-N)Pro, and one C-terminus modified peptide (AcSDKP-NH2). We report here that these analogs reduce in vitro the proportion of murine colony-forming units-granulocyte/macrophage in S-phase and inhibit the entry into cycle of high proliferative potential colony-forming cells. The efficacy of AcSDKP analogs in preventing in vitro primitive hematopoietic stem cells from entering into cycle suggests that these molecules could be new candidates for the powerful inhibition of hematopoietic stem and progenitor cell proliferation in vivo.

Leukemia Research, 1989

A semi-purified fraction extracted from fetal calf bone marrow was previously shown to contain a ... more A semi-purified fraction extracted from fetal calf bone marrow was previously shown to contain a tetrapeptide N-Ac-Ser-Asp-Lys-Pro which inhibits in mice, hematopoietic stem cell entry into the cell cycle. This peptide however, did not exhibit any effect on either IL-3 nor GM-CSF dependent cell growth. We report herein that a semi-purified fraction also contains another activity which is antagonistic to IL-3. Addition of the fraction in vitro decreased IL-3 dependent mast cell colony formation. Growth of IL-3 dependent cell lines (DA-1 and FDC-P2) was also suppressed. No effect was observed in the same dose range on granulocyte-macrophage colony formation nor on IL-3 independent cell growth.

Blood, 1998

The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP or Goralatide), a physiological regulator of he... more The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP or Goralatide), a physiological regulator of hematopoiesis, inhibits the entry into the S-phase of murine and human hematopoietic stem cells. It has been shown to reduce the damage to specific compartments in the bone marrow resulting from treatment with chemotherapeutic agents, ionizing radiations, hyperthermy, or phototherapy. The present study was performed to assess the therapeutic potential of AcSDKP in vivo in reducing both the toxicity and the hematopoietic damage induced by fractionated administration of doxorubicin (DOX), a widely used anticancer drug. Here we showed that AcSDKP could reduce DOX-induced mortality in mice and could protect particularly the long-term reconstituting cells (LTRCs) in addition to colony forming units-spleen, high proliferative potential colony-forming cells, and colony-forming units–granulocyte-macrophage (CFU-GM) from DOX toxicity. The protection against DOX-induced mortality in mice was improve...

The present invention relates to a compound of formula (I): wherein: - m is an integer from 0 to ... more The present invention relates to a compound of formula (I): wherein: - m is an integer from 0 to 3, preferably 0 to 2; - n is an integer from 0 to 3, preferably from 0 to 2; - m + n ≥ 1 - EAG represents an electron withdrawing group independently selected from halogen, NO2, CF3, CC13, CN, CO2H, (C = O) NR2, CH = NR, (C = S) OR , (C = O) SR, CS2R, SO2R, SO2NR2, SO3R, P (O) (OR) 2, P (O) (R) 2, B (OR) 2, wherein R is (C1 - C6) alkyl, phenyl or hydrogen; - A represents a hydrocarbon chain, saturated or unsaturated, linear or branched comprising from 1 to 10 carbon atoms; and - R1 and R2 are each independently of one another, a hydrogen, CO- (C1 - C6) -alkyl, (C1 - C6) alkyl, phenyl or phenyl (C1 - C6) -alkyl, wherein R1 and R2 together with the nitrogen atom which carries them, a heterocycle with 5 to 15 ring members, optionally substituted with a (C1 - C6) alkyl; including its stereoisomers and mixtures thereof, or a pharmaceutically acceptable acid salt thereof.

The present invention relates to the cosmetic use of at least one compound of formula (I) wherein... more The present invention relates to the cosmetic use of at least one compound of formula (I) wherein, A1 is the radical corresponding to D- or L- Ser, A2 is the radical corresponding to D- or L- Asp or Glu, A3 is the radical corresponding to D- or L- Lys, Arg or Orn, A4 is the radical corresponding to D- or L- Pro, R1, R2, R3 are as defined in the claims as an agent anti-aging and restructuring skin.

Use of a biguanide derivative of general formula I below: wherein: R1 and R2 groups represent, in... more Use of a biguanide derivative of general formula I below: wherein: R1 and R2 groups represent, independently of one another, a hydrogen atom; alkyl group of C1- C7; a cycloalkyl group of C3-C7; a heterocycle comprising from 3 to 7 atoms, one or more of them an oxygen atom, nitrogen or sulfur and the others being carbon atoms; an alkenyl group of C2-C7; a phenyl group optionally substituted with a group C1-C7 alkenyl group, C2-C7 or a halogen; a phenylalkyl group whose alkyl group is C1-C7, and the phenyl group is optionally substituted with a C1-C7 alkenyl group, C2-C7 or a halogen; a phenyloxy group whose alkyl group is C1-C7, and the phenyl group is optionally substituted with a C1-C7 alkenyl group, C2-C7 or a halogen; a furyl, isoxazyl, pyridyl or pyrimidyl; or R1 and R2 taken together represent a C2-C7 alkylene WHAT CAN contain one or more heteroatoms; and the group R3 represents a primary or tertiary amine, or an amine of formula: or pharmaceutically acceptable salt thereof as ...

The present invention relates to the use of a compound of formula I: in which, A 1 is the radical... more The present invention relates to the use of a compound of formula I: in which, A 1 is the radical corresponding to D- or L-Ser, A 2 is the radical corresponding to D- or L-Asp or Glu, A 3 is the radical corresponding to D- or L-Lys, Arg or Gm, A 4 is the radical corresponding to D- or L-Pro, R 1 and R 2 are chosen, independently, from H, C 1 -C 12 -alkyl which may or may not be substituted, C 7 -C 20 -arylalkyl which may or may not be substituted, R 4 CO or R 4 COO, R 4 being C 1 -C 12 -alkyl which may or may not be substituted, or C 7 -C 20 -arylalkyl which may or may not be substituted; among the substitutions, mention should be made of OH, NH 2 or COOH, X 1 and X 2 are peptide or pseudopeptide bonds, X 3 is CO or CH 2 and R 3 is OH, NH 2 , C 1 -C 1 -alkoxy or NH-X 4 -CH 2 -Z, X 4 is a normal or branched C 1 -C 12 hydrocarbon, and Z is H, OH, CO 2 H or CONH 2 , or the corresponding tripeptides comprising the radicals A 1 , A 2 , A 3 , and also the pharmacautically acceptable salts...

wherein, A1 is the radical corresponding to D- or L- Ser, A2 is the radical corresponding to D- o... more wherein, A1 is the radical corresponding to D- or L- Ser, A2 is the radical corresponding to D- or L- Asp or Glu, A3 is the radical corresponding to D- or L- Lys, Arg or Orn, A4 is the radical corresponding to D- or L- Pro, R1, R2, R3 are as defined in the claims as an agent for fighting against hair loss.

This invention relates to the cosmetic use of a biguanide derivative as an asset anti-aging and r... more This invention relates to the cosmetic use of a biguanide derivative as an asset anti-aging and restructuring of the skin. In particular, metformin is suitable for use in the present invention.

The present invention thus relates to the use of biguanide derivatives of the following general f... more The present invention thus relates to the use of biguanide derivatives of the following general formula I: (CF DRAWING IN BOPI) in which: the groups R1 and R2 represent, independently of one another, a hydrogen atom, a C 1 -C 7 alkyl group, a cycloalkyl group, a heterocycle, a C 2 -C 7 alkenyl group, an aryl group, an aralkyl group, an aryloxylalkyl group or a heteroaryl group or R 1 and R 2 taken together represent a C 2 -C 7 alkylene which may contain one or more heteroatoms and the group R3 represents a primary, secondary or tertiary amine or pharmaceutically acceptable salts thereof to produce a medicament having a healing effect.

La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, ... more La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, A1 est le radical correspondant a D- ou L- Ser, A2 est le radical correspondant a D- ou L- Asp ou Glu, A3 est le radical correspondant a D- ou L- Lys, Arg ou Orn, A4 est le radical correspondant a D- ou L- Pro, R1 et R2 sont choisis independamment parmi H, C1-C12-alkyle substitue ou non, C7-C20-arylalkyle substitue ou non, R4CO ou R4COO, R4 etant C1-C12-alkyle sustitue ou non, C7-C20-arylalkyle substitue ou non, parmi les substitutions il faut citer OH, NH2 ou COOH, X1 et X2 sont des liaisons peptidiques ou pseudopeptidiques, X3 est CO ou CH2 et R3 est OH, NH2, C1-C12-alcoxy ou NH-X4-CH2-Z, X4 est un C1-C12-hydrocarbone normal ou ramifie, Z est H, OH, CO2H ou CONH2, ou bien les tripeptides correspondants comprenant les radicaux A1, A2, A3, ainsi que les sels pharmaceuticement acceptables, pour la realisation d'un medicament destine au traitement des pathologies pouvant beneficier d&#...

La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, ... more La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, A1 est le radical correspondant a D- ou L- Ser, A2 est le radical correspondant a D- ou L- Asp ou Glu, A3 est le radical correspondant a D- ou L- Lys, Arg ou Orn, A4 est le radical correspondant a D- ou L- Pro, R1 et R2 sont choisis independamment parmi H, C1-C12-alkyle substitue ou non, C7-C20-arylalkyle substitue ou non, R4CO ou R4COO, R4 etant C1-C12-alkyle sustitue ou non, C7-C20-arylalkyle substitue ou non, parmi les substitutions il faut citer OH, NH2 ou COOH, X1 et X2 sont des liaisons peptidiques ou pseudopeptidiques, X3 est CO ou CH2 et R3 est OH, NH2, C1-C12-alcoxy ou NH-X4-CH2-Z, X4 est un C1-C12-hydrocarbone normal ou ramifie, Z est H, OH, CO2H ou CONH2, ou bien les tripeptides correspondants comprenant les radicaux A1, A2, A3, ainsi que les sels pharmaceuticement acceptables, pour la realisation d'un medicament destine au traitement des pathologies pouvant beneficier d&#...

STEM CELLS, 1999

The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP), an inhibitor of hematopoietic stem cell proli... more The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP), an inhibitor of hematopoietic stem cell proliferation, is known to reduce in vivo the damage resulting from treatment with chemotherapeutic agents or ionizing radiation on the stem cell compartment. Recently, AcSDKP has been shown to be a physiological substrate of the N-active site of angiotensin I-converting enzyme (ACE). Four analogs of the tetrapeptide expressing a high stability towards ACE degradation in vitro have been synthesized in order to provide new molecules likely to improve the myeloprotection displayed by AcSDKP. These analogs are three pseudopeptides with a modified peptidic bond, Ac-Serpsi(CH2-NH)Asp-Lys-Pro, Ac-Ser-Asppsi(CH2-NH)Lys-Pro, Ac-Ser-Asp-Lyspsi(CH2-N)Pro, and one C-terminus modified peptide (AcSDKP-NH2). We report here that these analogs reduce in vitro the proportion of murine colony-forming units-granulocyte/macrophage in S-phase and inhibit the entry into cycle of high proliferative potential colony-forming cells. The efficacy of AcSDKP analogs in preventing in vitro primitive hematopoietic stem cells from entering into cycle suggests that these molecules could be new candidates for the powerful inhibition of hematopoietic stem and progenitor cell proliferation in vivo.

Leukemia Research, 1989

A semi-purified fraction extracted from fetal calf bone marrow was previously shown to contain a ... more A semi-purified fraction extracted from fetal calf bone marrow was previously shown to contain a tetrapeptide N-Ac-Ser-Asp-Lys-Pro which inhibits in mice, hematopoietic stem cell entry into the cell cycle. This peptide however, did not exhibit any effect on either IL-3 nor GM-CSF dependent cell growth. We report herein that a semi-purified fraction also contains another activity which is antagonistic to IL-3. Addition of the fraction in vitro decreased IL-3 dependent mast cell colony formation. Growth of IL-3 dependent cell lines (DA-1 and FDC-P2) was also suppressed. No effect was observed in the same dose range on granulocyte-macrophage colony formation nor on IL-3 independent cell growth.

Blood, 1998

The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP or Goralatide), a physiological regulator of he... more The tetrapeptide Acetyl-N-Ser-Asp-Lys-Pro (AcSDKP or Goralatide), a physiological regulator of hematopoiesis, inhibits the entry into the S-phase of murine and human hematopoietic stem cells. It has been shown to reduce the damage to specific compartments in the bone marrow resulting from treatment with chemotherapeutic agents, ionizing radiations, hyperthermy, or phototherapy. The present study was performed to assess the therapeutic potential of AcSDKP in vivo in reducing both the toxicity and the hematopoietic damage induced by fractionated administration of doxorubicin (DOX), a widely used anticancer drug. Here we showed that AcSDKP could reduce DOX-induced mortality in mice and could protect particularly the long-term reconstituting cells (LTRCs) in addition to colony forming units-spleen, high proliferative potential colony-forming cells, and colony-forming units–granulocyte-macrophage (CFU-GM) from DOX toxicity. The protection against DOX-induced mortality in mice was improve...

The present invention relates to a compound of formula (I): wherein: - m is an integer from 0 to ... more The present invention relates to a compound of formula (I): wherein: - m is an integer from 0 to 3, preferably 0 to 2; - n is an integer from 0 to 3, preferably from 0 to 2; - m + n ≥ 1 - EAG represents an electron withdrawing group independently selected from halogen, NO2, CF3, CC13, CN, CO2H, (C = O) NR2, CH = NR, (C = S) OR , (C = O) SR, CS2R, SO2R, SO2NR2, SO3R, P (O) (OR) 2, P (O) (R) 2, B (OR) 2, wherein R is (C1 - C6) alkyl, phenyl or hydrogen; - A represents a hydrocarbon chain, saturated or unsaturated, linear or branched comprising from 1 to 10 carbon atoms; and - R1 and R2 are each independently of one another, a hydrogen, CO- (C1 - C6) -alkyl, (C1 - C6) alkyl, phenyl or phenyl (C1 - C6) -alkyl, wherein R1 and R2 together with the nitrogen atom which carries them, a heterocycle with 5 to 15 ring members, optionally substituted with a (C1 - C6) alkyl; including its stereoisomers and mixtures thereof, or a pharmaceutically acceptable acid salt thereof.

The present invention relates to the cosmetic use of at least one compound of formula (I) wherein... more The present invention relates to the cosmetic use of at least one compound of formula (I) wherein, A1 is the radical corresponding to D- or L- Ser, A2 is the radical corresponding to D- or L- Asp or Glu, A3 is the radical corresponding to D- or L- Lys, Arg or Orn, A4 is the radical corresponding to D- or L- Pro, R1, R2, R3 are as defined in the claims as an agent anti-aging and restructuring skin.

Use of a biguanide derivative of general formula I below: wherein: R1 and R2 groups represent, in... more Use of a biguanide derivative of general formula I below: wherein: R1 and R2 groups represent, independently of one another, a hydrogen atom; alkyl group of C1- C7; a cycloalkyl group of C3-C7; a heterocycle comprising from 3 to 7 atoms, one or more of them an oxygen atom, nitrogen or sulfur and the others being carbon atoms; an alkenyl group of C2-C7; a phenyl group optionally substituted with a group C1-C7 alkenyl group, C2-C7 or a halogen; a phenylalkyl group whose alkyl group is C1-C7, and the phenyl group is optionally substituted with a C1-C7 alkenyl group, C2-C7 or a halogen; a phenyloxy group whose alkyl group is C1-C7, and the phenyl group is optionally substituted with a C1-C7 alkenyl group, C2-C7 or a halogen; a furyl, isoxazyl, pyridyl or pyrimidyl; or R1 and R2 taken together represent a C2-C7 alkylene WHAT CAN contain one or more heteroatoms; and the group R3 represents a primary or tertiary amine, or an amine of formula: or pharmaceutically acceptable salt thereof as ...

The present invention relates to the use of a compound of formula I: in which, A 1 is the radical... more The present invention relates to the use of a compound of formula I: in which, A 1 is the radical corresponding to D- or L-Ser, A 2 is the radical corresponding to D- or L-Asp or Glu, A 3 is the radical corresponding to D- or L-Lys, Arg or Gm, A 4 is the radical corresponding to D- or L-Pro, R 1 and R 2 are chosen, independently, from H, C 1 -C 12 -alkyl which may or may not be substituted, C 7 -C 20 -arylalkyl which may or may not be substituted, R 4 CO or R 4 COO, R 4 being C 1 -C 12 -alkyl which may or may not be substituted, or C 7 -C 20 -arylalkyl which may or may not be substituted; among the substitutions, mention should be made of OH, NH 2 or COOH, X 1 and X 2 are peptide or pseudopeptide bonds, X 3 is CO or CH 2 and R 3 is OH, NH 2 , C 1 -C 1 -alkoxy or NH-X 4 -CH 2 -Z, X 4 is a normal or branched C 1 -C 12 hydrocarbon, and Z is H, OH, CO 2 H or CONH 2 , or the corresponding tripeptides comprising the radicals A 1 , A 2 , A 3 , and also the pharmacautically acceptable salts...

wherein, A1 is the radical corresponding to D- or L- Ser, A2 is the radical corresponding to D- o... more wherein, A1 is the radical corresponding to D- or L- Ser, A2 is the radical corresponding to D- or L- Asp or Glu, A3 is the radical corresponding to D- or L- Lys, Arg or Orn, A4 is the radical corresponding to D- or L- Pro, R1, R2, R3 are as defined in the claims as an agent for fighting against hair loss.

This invention relates to the cosmetic use of a biguanide derivative as an asset anti-aging and r... more This invention relates to the cosmetic use of a biguanide derivative as an asset anti-aging and restructuring of the skin. In particular, metformin is suitable for use in the present invention.

The present invention thus relates to the use of biguanide derivatives of the following general f... more The present invention thus relates to the use of biguanide derivatives of the following general formula I: (CF DRAWING IN BOPI) in which: the groups R1 and R2 represent, independently of one another, a hydrogen atom, a C 1 -C 7 alkyl group, a cycloalkyl group, a heterocycle, a C 2 -C 7 alkenyl group, an aryl group, an aralkyl group, an aryloxylalkyl group or a heteroaryl group or R 1 and R 2 taken together represent a C 2 -C 7 alkylene which may contain one or more heteroatoms and the group R3 represents a primary, secondary or tertiary amine or pharmaceutically acceptable salts thereof to produce a medicament having a healing effect.

La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, ... more La presente invention concerne l'utilisation d'un compose de formule (I), dans laquelle, A1 est le radical correspondant a D- ou L- Ser, A2 est le radical correspondant a D- ou L- Asp ou Glu, A3 est le radical correspondant a D- ou L- Lys, Arg ou Orn, A4 est le radical correspondant a D- ou L- Pro, R1 et R2 sont choisis independamment parmi H, C1-C12-alkyle substitue ou non, C7-C20-arylalkyle substitue ou non, R4CO ou R4COO, R4 etant C1-C12-alkyle sustitue ou non, C7-C20-arylalkyle substitue ou non, parmi les substitutions il faut citer OH, NH2 ou COOH, X1 et X2 sont des liaisons peptidiques ou pseudopeptidiques, X3 est CO ou CH2 et R3 est OH, NH2, C1-C12-alcoxy ou NH-X4-CH2-Z, X4 est un C1-C12-hydrocarbone normal ou ramifie, Z est H, OH, CO2H ou CONH2, ou bien les tripeptides correspondants comprenant les radicaux A1, A2, A3, ainsi que les sels pharmaceuticement acceptables, pour la realisation d'un medicament destine au traitement des pathologies pouvant beneficier d&#...