Jacek Ostrowski - Academia.edu (original) (raw)

Papers by Jacek Ostrowski

Research paper thumbnail of Thermoelectric Matrix for Human Warmth Harvesting as Secondary Energy Source in Wearable Electronics

2018 International Conference on Signals and Electronic Systems (ICSES), 2018

The paper deals with an idea of a thermoelectric matrix which is capable of harvesting free avail... more The paper deals with an idea of a thermoelectric matrix which is capable of harvesting free available energy dissipated in a form of human heat. The main objective of the work was to provide a proof of concept that the human warmth converted into electrical energy can be used as a secondary power source supporting primary battery in a sensor bracelet. The scope of the article includes presentation of the thermoelectric matrix structure and its electrothermal model in a few configurations of mini-TEGs outputs connections. Then a set of results is presented showing coupled electrical and thermal experimental simulations of the harvesting matrix connected to an ultra-low voltage converter LTC3108. The obtained characteristics of the equivalent output Seebeck voltages and available electrical power in respect to the mini-TEGs connections configurations indicate the best scenario in terms of energy conversion efficiency.

Research paper thumbnail of Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment

JACC: Basic to Translational Science, 2019

Myocardial infarction leads to recruitment of monocyte/macrophages to the injured myocardium to d... more Myocardial infarction leads to recruitment of monocyte/macrophages to the injured myocardium to drive infarct healing. Activation of formyl peptide receptors (FPR1 and FPR2) present on macrophages contributes to key cellular activities that can potentiate wound healing. Myocardial infarction was induced in rodents to study the effects of long-term treatment with Compound 43, a small molecule agonist of FPR1 and FPR2. Main findings: Compound 43 stimulated proresolution macrophage activities, improved left ventricle and infarct structure, and preserved cardiac function post-myocardial infarction. The results suggest that stimulation of proresolution activities of FPRs can favorably alter post-myocardial infarction pathophysiology that leads to heart failure.

Research paper thumbnail of Breath sensor based on conductive foam: Idea, construction, and characterisation

2016 International Conference on Signals and Electronic Systems (ICSES), 2016

This paper deals with breath sensor constructed based on conductive, polyurethane foam, which is ... more This paper deals with breath sensor constructed based on conductive, polyurethane foam, which is usually used for storage of electronics devices. A piece of the foam with especially prepared terminals is placed under tight T-shirt at the chest of a monitored person. The paper presents the idea of the sensor, investigation on its construction and problems being faced with. Parameters assessment processes and results are described too, so finally well characterized electronics component, ready to use, is presented. Some examples of use of the sensor are presented at the end of the paper.

Research paper thumbnail of Extraction of temperature dependent parameters for an electrothermal model of thermoelectric energy harvester

2016 MIXDES - 23rd International Conference Mixed Design of Integrated Circuits and Systems, 2016

A method and procedures have been developed for extraction of temperature dependent parameters of... more A method and procedures have been developed for extraction of temperature dependent parameters of a thermoelectric energy harvester. Temperature functions of Seebeck coefficient S, electrical resistance R, and thermal conductance K were carried out. They are all indispensable for accurate simulation of complex electro-thermal processes associated with conversion of small pieces of free heat energy. The paper discusses the modelling of a single tiny thermoelectric generator with high-density pellets placement. It is intended to be used as a single building block in a wearable thermoelectric matrix for harvesting and conversion of human warmth to electricity.

Research paper thumbnail of Chimeric Therapeutics, Compositions, and Methods for Using Same

Research paper thumbnail of Cell lines and cell-based assays for identification of androgen receptor modulators

Research paper thumbnail of Methods and Compositions for Controlling Assembly of Viral Proteins

Research paper thumbnail of Hydrogen-bond interactions and their influence on conformation of retinoidal-active and -inactive aromatic anilides

Acta Crystallographica Section A Foundations of Crystallography, 1996

Tolterodine is a drug substance contammg (+)-N,Ndiisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl... more Tolterodine is a drug substance contammg (+)-N,Ndiisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylprolylamine hydrogen L(+)-tartrate CC26H37N07).The drug is used for the treatment of minary frequency, urgency and/or urge incontinence. The synthesis of tolterodin L(+)-tartrate is a well established procedure. The crystal structure of tolterodine L(+)-tartrate was determined from single crystal x-ray data at room temperature and 30 K. The structure is monoclinic with two formula units in.the unit cell and all the atoms in the general position of the space-group P2J. The unit cell dimensions at 30 K are a= 9.1759, b = 16.3965c =l2.9196A. = 93.427". In the final stage of the refinement the 3568 reflections recorded at 30 K were refined to an R-value of 4.0%.

Research paper thumbnail of Selective retinoic acid receptor ligands for rheumatoid arthritis

Current opinion in investigational drugs (London, England : 2000), 2004

Retinoids, modulators of retinoic acid receptors (RARs), have been studied for over 20 years as p... more Retinoids, modulators of retinoic acid receptors (RARs), have been studied for over 20 years as potential therapeutic agents for rheumatoid arthritis (RA). Early successes at the in vitro and in vivo levels were overshadowed by disappointing clinical trials that yielded poor efficacy and unacceptable side effects. A greater understanding of retinoid biology has led to the development of many synthetic retinoids that selectively modulate the RAR isotypes. RAR selective retinoids have a high potential for improved pharmacology with reduced toxicity, thereby renewing interest for the use of retinoids in RA.

Research paper thumbnail of Therapeutic combinations of RAR antagonists and RXR agonists and use thereof

Research paper thumbnail of Two distinct actions of retinoid-receptor ligands

Research paper thumbnail of Inhibition of disease progression by a novel retinoid antagonist in animal models of arthritis

The Journal of rheumatology, 2003

To investigate the usefulness of a novel retinoic acid receptor (RAR) antagonist (BMS-189453) in ... more To investigate the usefulness of a novel retinoic acid receptor (RAR) antagonist (BMS-189453) in animal models of arthritis. BMS-189453 was tested in HIG-82 rabbit synovial fibroblasts to determine its ability to repress collagenase (matrix metalloproteinase-1, MMP-1) mRNA expression in vitro. Cells were stimulated with phorbol myristate acetate or interleukin 1 beta and mRNA quantified by slot-blot analysis. In vivo, BMS-189453 was evaluated in 2 animal models of arthritis: collagen induced arthritis (CIA) in mice and streptococcal cell wall induced arthritis (SCWA) in rats. Clinical scores for arthritis were recorded weekly. At the end of each study, limbs were evaluated histologically. In CIA, these results were correlated with mRNA levels for collagenase-3 (MMP-13) and stromelysin-1 (MMP-3) as determined by Northern blot. BMS-189453 reduced MMP-1 expression in HIG-82 synovial fibroblasts in culture. BMS-189453 treatment blocked the clinical progression of arthritis beyond soft t...

Research paper thumbnail of Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications

Journal of Medicinal Chemistry, 2007

A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active... more A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs), with most of the compounds exhibiting low nM in vitro potency in androgen receptor (AR) binding and functional assays. Once daily oral treatment with the lead compound 11a (AR Ki = 0.9 nM, EC50 = 1.8 nM) for 14 days induced muscle growth with an ED50 of 0.09 mg/kg, providing approximately 50-fold selectivity over prostate growth in an orchidectomized rat model. Pharmacokinetic studies in rats demonstrated that the lead compound 11a had oral bioavailability of 65% and a plasma half-life of 5.5 h. On the basis of their preclinical profiles, the SARMs in this series are expected to provide beneficial anabolic effects on muscle with minimal androgenic effects on prostate tissue.

Research paper thumbnail of Synthesis of Nitrone Analogues of Rar α Selective Retinoid AM580

Synthetic Communications, 1995

ABSTRACT Synthesis of nitrone analogues of RAR a-selective retinoid Am 580 in which the amide lin... more ABSTRACT Synthesis of nitrone analogues of RAR a-selective retinoid Am 580 in which the amide linker is replaced with a nitrone moiety is discribed. The nitrone segment was constructed by oxidizing the corresponding amine using MCPBA or dimethyldioxirane. The resulting ...

Research paper thumbnail of Antagonism of Catecholamine Receptor Signaling by Expression of Cytoplasmic Domains of the Receptors

Science, 1993

transcription (14). To generate a muscle cell from nonmuscle tissue, fibrosarcoma cells may repre... more transcription (14). To generate a muscle cell from nonmuscle tissue, fibrosarcoma cells may repress (or lose) these loci, resulting in the activation of MyoD transcription. Because MyoD can induce growth arrest (15), its expression in a fibrosarcoma may serve as a "fail-safe" mechanism to prevent cell growth. Additional genetic defects that prevent MyoD function, such as the recessive defects described here, would prevent differentiation and result in the generation of a rhabdomyosarcoma. A similar mechanism may apply to other types of tumors that express full or partial differentiation programs.

Research paper thumbnail of A small region of the beta-adrenergic receptor is selectively involved in its rapid regulation

Proceedings of the National Academy of Sciences, 1991

Plasma membrane receptors that couple to guanine nucleotide-binding regulatory proteins (G protei... more Plasma membrane receptors that couple to guanine nucleotide-binding regulatory proteins (G proteins) undergo a variety of rapid (minutes) and longer term (hours) regulatory processes induced by ligands. For the beta 2-adrenergic receptor (beta 2AR), the rapid processes include functional desensitization, mediated by phosphorylation of the receptor by the cAMP-dependent protein kinase and the beta-adrenergic receptor kinase, as well as a loss of hydrophilic ligand binding proposed to represent sequestration of receptors into a cellular compartment distinct from the plasma membrane. The slower processes include beta 2AR down-regulation (i.e., a decrease in the total cellular complement of receptors). It is not yet known whether beta 2AR phosphorylation and/or sequestration are prerequisites for down-regulation of the receptor. Like other G protein-coupled receptors, the beta 2AR molecule spans the plasma membrane seven times, and the cytoplasmic carboxyl-terminal domain has been propo...

Research paper thumbnail of Discovery of Potent, Orally-Active, and Muscle-Selective Androgen Receptor Modulators Based on an N-Aryl-hydroxybicyclohydantoin Scaffold

Journal of Medicinal Chemistry, 2006

A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered th... more A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited >50-fold selectivity for muscle over prostate.

Research paper thumbnail of N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation

Journal of Medicinal Chemistry, 2009

A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtai... more A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of imidazolidin-2-ones. The resulting oxazolidin-2-imines are among the most potent SARMs known, with many analogues exhibiting sub-nM in vitro potency in binding and functional assays. Despite the potential for hydrolytic instability at gut pH, compounds of the present class showed good oral bioavailability and were highly active in a standard rodent pharmacological model.

Research paper thumbnail of Serine 232 and Methionine 272 Define the Ligand Binding Pocket in Retinoic Acid Receptor Subtypes

Journal of Biological Chemistry, 1998

Research paper thumbnail of Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats

Research paper thumbnail of Thermoelectric Matrix for Human Warmth Harvesting as Secondary Energy Source in Wearable Electronics

2018 International Conference on Signals and Electronic Systems (ICSES), 2018

The paper deals with an idea of a thermoelectric matrix which is capable of harvesting free avail... more The paper deals with an idea of a thermoelectric matrix which is capable of harvesting free available energy dissipated in a form of human heat. The main objective of the work was to provide a proof of concept that the human warmth converted into electrical energy can be used as a secondary power source supporting primary battery in a sensor bracelet. The scope of the article includes presentation of the thermoelectric matrix structure and its electrothermal model in a few configurations of mini-TEGs outputs connections. Then a set of results is presented showing coupled electrical and thermal experimental simulations of the harvesting matrix connected to an ultra-low voltage converter LTC3108. The obtained characteristics of the equivalent output Seebeck voltages and available electrical power in respect to the mini-TEGs connections configurations indicate the best scenario in terms of energy conversion efficiency.

Research paper thumbnail of Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment

JACC: Basic to Translational Science, 2019

Myocardial infarction leads to recruitment of monocyte/macrophages to the injured myocardium to d... more Myocardial infarction leads to recruitment of monocyte/macrophages to the injured myocardium to drive infarct healing. Activation of formyl peptide receptors (FPR1 and FPR2) present on macrophages contributes to key cellular activities that can potentiate wound healing. Myocardial infarction was induced in rodents to study the effects of long-term treatment with Compound 43, a small molecule agonist of FPR1 and FPR2. Main findings: Compound 43 stimulated proresolution macrophage activities, improved left ventricle and infarct structure, and preserved cardiac function post-myocardial infarction. The results suggest that stimulation of proresolution activities of FPRs can favorably alter post-myocardial infarction pathophysiology that leads to heart failure.

Research paper thumbnail of Breath sensor based on conductive foam: Idea, construction, and characterisation

2016 International Conference on Signals and Electronic Systems (ICSES), 2016

This paper deals with breath sensor constructed based on conductive, polyurethane foam, which is ... more This paper deals with breath sensor constructed based on conductive, polyurethane foam, which is usually used for storage of electronics devices. A piece of the foam with especially prepared terminals is placed under tight T-shirt at the chest of a monitored person. The paper presents the idea of the sensor, investigation on its construction and problems being faced with. Parameters assessment processes and results are described too, so finally well characterized electronics component, ready to use, is presented. Some examples of use of the sensor are presented at the end of the paper.

Research paper thumbnail of Extraction of temperature dependent parameters for an electrothermal model of thermoelectric energy harvester

2016 MIXDES - 23rd International Conference Mixed Design of Integrated Circuits and Systems, 2016

A method and procedures have been developed for extraction of temperature dependent parameters of... more A method and procedures have been developed for extraction of temperature dependent parameters of a thermoelectric energy harvester. Temperature functions of Seebeck coefficient S, electrical resistance R, and thermal conductance K were carried out. They are all indispensable for accurate simulation of complex electro-thermal processes associated with conversion of small pieces of free heat energy. The paper discusses the modelling of a single tiny thermoelectric generator with high-density pellets placement. It is intended to be used as a single building block in a wearable thermoelectric matrix for harvesting and conversion of human warmth to electricity.

Research paper thumbnail of Chimeric Therapeutics, Compositions, and Methods for Using Same

Research paper thumbnail of Cell lines and cell-based assays for identification of androgen receptor modulators

Research paper thumbnail of Methods and Compositions for Controlling Assembly of Viral Proteins

Research paper thumbnail of Hydrogen-bond interactions and their influence on conformation of retinoidal-active and -inactive aromatic anilides

Acta Crystallographica Section A Foundations of Crystallography, 1996

Tolterodine is a drug substance contammg (+)-N,Ndiisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl... more Tolterodine is a drug substance contammg (+)-N,Ndiisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylprolylamine hydrogen L(+)-tartrate CC26H37N07).The drug is used for the treatment of minary frequency, urgency and/or urge incontinence. The synthesis of tolterodin L(+)-tartrate is a well established procedure. The crystal structure of tolterodine L(+)-tartrate was determined from single crystal x-ray data at room temperature and 30 K. The structure is monoclinic with two formula units in.the unit cell and all the atoms in the general position of the space-group P2J. The unit cell dimensions at 30 K are a= 9.1759, b = 16.3965c =l2.9196A. = 93.427". In the final stage of the refinement the 3568 reflections recorded at 30 K were refined to an R-value of 4.0%.

Research paper thumbnail of Selective retinoic acid receptor ligands for rheumatoid arthritis

Current opinion in investigational drugs (London, England : 2000), 2004

Retinoids, modulators of retinoic acid receptors (RARs), have been studied for over 20 years as p... more Retinoids, modulators of retinoic acid receptors (RARs), have been studied for over 20 years as potential therapeutic agents for rheumatoid arthritis (RA). Early successes at the in vitro and in vivo levels were overshadowed by disappointing clinical trials that yielded poor efficacy and unacceptable side effects. A greater understanding of retinoid biology has led to the development of many synthetic retinoids that selectively modulate the RAR isotypes. RAR selective retinoids have a high potential for improved pharmacology with reduced toxicity, thereby renewing interest for the use of retinoids in RA.

Research paper thumbnail of Therapeutic combinations of RAR antagonists and RXR agonists and use thereof

Research paper thumbnail of Two distinct actions of retinoid-receptor ligands

Research paper thumbnail of Inhibition of disease progression by a novel retinoid antagonist in animal models of arthritis

The Journal of rheumatology, 2003

To investigate the usefulness of a novel retinoic acid receptor (RAR) antagonist (BMS-189453) in ... more To investigate the usefulness of a novel retinoic acid receptor (RAR) antagonist (BMS-189453) in animal models of arthritis. BMS-189453 was tested in HIG-82 rabbit synovial fibroblasts to determine its ability to repress collagenase (matrix metalloproteinase-1, MMP-1) mRNA expression in vitro. Cells were stimulated with phorbol myristate acetate or interleukin 1 beta and mRNA quantified by slot-blot analysis. In vivo, BMS-189453 was evaluated in 2 animal models of arthritis: collagen induced arthritis (CIA) in mice and streptococcal cell wall induced arthritis (SCWA) in rats. Clinical scores for arthritis were recorded weekly. At the end of each study, limbs were evaluated histologically. In CIA, these results were correlated with mRNA levels for collagenase-3 (MMP-13) and stromelysin-1 (MMP-3) as determined by Northern blot. BMS-189453 reduced MMP-1 expression in HIG-82 synovial fibroblasts in culture. BMS-189453 treatment blocked the clinical progression of arthritis beyond soft t...

Research paper thumbnail of Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications

Journal of Medicinal Chemistry, 2007

A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active... more A novel series of imidazolin-2-ones were designed and synthesized as highly potent, orally active and muscle selective androgen receptor modulators (SARMs), with most of the compounds exhibiting low nM in vitro potency in androgen receptor (AR) binding and functional assays. Once daily oral treatment with the lead compound 11a (AR Ki = 0.9 nM, EC50 = 1.8 nM) for 14 days induced muscle growth with an ED50 of 0.09 mg/kg, providing approximately 50-fold selectivity over prostate growth in an orchidectomized rat model. Pharmacokinetic studies in rats demonstrated that the lead compound 11a had oral bioavailability of 65% and a plasma half-life of 5.5 h. On the basis of their preclinical profiles, the SARMs in this series are expected to provide beneficial anabolic effects on muscle with minimal androgenic effects on prostate tissue.

Research paper thumbnail of Synthesis of Nitrone Analogues of Rar α Selective Retinoid AM580

Synthetic Communications, 1995

ABSTRACT Synthesis of nitrone analogues of RAR a-selective retinoid Am 580 in which the amide lin... more ABSTRACT Synthesis of nitrone analogues of RAR a-selective retinoid Am 580 in which the amide linker is replaced with a nitrone moiety is discribed. The nitrone segment was constructed by oxidizing the corresponding amine using MCPBA or dimethyldioxirane. The resulting ...

Research paper thumbnail of Antagonism of Catecholamine Receptor Signaling by Expression of Cytoplasmic Domains of the Receptors

Science, 1993

transcription (14). To generate a muscle cell from nonmuscle tissue, fibrosarcoma cells may repre... more transcription (14). To generate a muscle cell from nonmuscle tissue, fibrosarcoma cells may repress (or lose) these loci, resulting in the activation of MyoD transcription. Because MyoD can induce growth arrest (15), its expression in a fibrosarcoma may serve as a "fail-safe" mechanism to prevent cell growth. Additional genetic defects that prevent MyoD function, such as the recessive defects described here, would prevent differentiation and result in the generation of a rhabdomyosarcoma. A similar mechanism may apply to other types of tumors that express full or partial differentiation programs.

Research paper thumbnail of A small region of the beta-adrenergic receptor is selectively involved in its rapid regulation

Proceedings of the National Academy of Sciences, 1991

Plasma membrane receptors that couple to guanine nucleotide-binding regulatory proteins (G protei... more Plasma membrane receptors that couple to guanine nucleotide-binding regulatory proteins (G proteins) undergo a variety of rapid (minutes) and longer term (hours) regulatory processes induced by ligands. For the beta 2-adrenergic receptor (beta 2AR), the rapid processes include functional desensitization, mediated by phosphorylation of the receptor by the cAMP-dependent protein kinase and the beta-adrenergic receptor kinase, as well as a loss of hydrophilic ligand binding proposed to represent sequestration of receptors into a cellular compartment distinct from the plasma membrane. The slower processes include beta 2AR down-regulation (i.e., a decrease in the total cellular complement of receptors). It is not yet known whether beta 2AR phosphorylation and/or sequestration are prerequisites for down-regulation of the receptor. Like other G protein-coupled receptors, the beta 2AR molecule spans the plasma membrane seven times, and the cytoplasmic carboxyl-terminal domain has been propo...

Research paper thumbnail of Discovery of Potent, Orally-Active, and Muscle-Selective Androgen Receptor Modulators Based on an N-Aryl-hydroxybicyclohydantoin Scaffold

Journal of Medicinal Chemistry, 2006

A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered th... more A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited >50-fold selectivity for muscle over prostate.

Research paper thumbnail of N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation

Journal of Medicinal Chemistry, 2009

A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtai... more A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of imidazolidin-2-ones. The resulting oxazolidin-2-imines are among the most potent SARMs known, with many analogues exhibiting sub-nM in vitro potency in binding and functional assays. Despite the potential for hydrolytic instability at gut pH, compounds of the present class showed good oral bioavailability and were highly active in a standard rodent pharmacological model.

Research paper thumbnail of Serine 232 and Methionine 272 Define the Ligand Binding Pocket in Retinoic Acid Receptor Subtypes

Journal of Biological Chemistry, 1998

Research paper thumbnail of Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats