Ciclesonide Inhibits SARS-CoV-2 Papain-Like Protease in Vitro
Biol Pharm Bull. 2024;47(5):965-966. doi: 10.1248/bpb.b24-00038.ABSTRACTThe emergence of coronavirus disease 2019 (COVID-19), a novel identified pneumonia resulting from the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, has significantly impacted and posed significant challenges to human society. The papain-like protease (PLpro) found in the nonstructural protein 3 of SARS-CoV-2 plays a vital role in viral replication. Moreover, PLpro disrupts the host immune response by cleaving ubiquitin and interferon-stimulated gene 15 from host proteins. Consequently, PLpro has emerged as a promising drug target ...
Source: Biological and Pharmaceutical Bulletin - May 19, 2024 Category: Drugs & Pharmacology Authors: Yuka Kiba Takashi Tanikawa Masashi Kitamura Source Type: research

Computational Estimation of Residues Involving Resistance to the SARS-CoV-2 Main Protease Inhibitor Ensitrelvir Based on Virtual Alanine Scan of the Active Site
In this study, we computationally constructed 24 mutants, in which one residue around the active site was replaced with alanine and performed molecular dynamics simulations to the complex of Mpro and ensitrelvir to predict the residues involved in drug resistance. We evaluated the changes in the entire protein structure and ligand configuration in each of these mutants and estimated which residues were involved in ensitrelvir recognition. This method is called a virtual alanine scan. In nine mutants (S1A, T26A, H41A, M49A, L141A, H163A, E166A, V186A, and R188A), although the entire protein structure and catalytic dyad (cys...
Source: Biological and Pharmaceutical Bulletin - May 19, 2024 Category: Drugs & Pharmacology Authors: Ayato Mizuno Tomoki Nakayoshi Koichi Kato Eiji Kurimoto Akifumi Oda Source Type: research

Risk Factors for Teicoplanin-Associated Acute Kidney Injury in Patients with Hematological Malignancies: Focusing on Concomitant Use of Tazobactam/Piperacillin
Biol Pharm Bull. 2024;47(5):988-996. doi: 10.1248/bpb.b23-00848.ABSTRACTPatients with hematological malignancies (HM) often receive tazobactam/piperacillin (TAZ/PIPC) and glycopeptide antibiotics for febrile neutropenia. The effect of concomitant use of TAZ/PIPC on risk of teicoplanin (TEIC)-associated acute kidney injury (AKI) remains unclear. We investigated the impact of concomitant TAZ/PIPC use on TEIC-associated AKI in HM patients and identified the risk factors. In this retrospective, single-center, observational cohort study, 203 patients received TEIC, 176 of whom satisfied the selection criteria and were divided i...
Source: Biological and Pharmaceutical Bulletin - May 19, 2024 Category: Drugs & Pharmacology Authors: Yuko Morinaga Ryota Tanaka Ryosuke Tatsuta Kuniko Takano Takehiro Hashimoto Masao Ogata Kazufumi Hiramatsu Hiroki Itoh Source Type: research

Structure-Activity Relationship Analysis of Fluoxetine for Suppression of Inflammatory Cytokine Production
Biol Pharm Bull. 2024;47(5):946-954. doi: 10.1248/bpb.b24-00083.ABSTRACTThere is accumulating evidence that selective serotonin reuptake inhibitors (SSRIs), clinically used as antidepressants, have a beneficial effect on inflammatory diseases such as coronavirus disease 2019 (COVID-19). We previously compared the inhibitory effects of five U.S. Food and Drug Administration (FDA)-approved SSRIs on the production of an inflammatory cytokine, interleukin-6 (IL-6), and concluded that fluoxetine (FLX) showed the most potent anti-inflammatory activity. Here, we investigated the structure-activity relationship of FLX for anti-inf...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Yohei Takenaka Ryu Tanaka Kazuki Kitabatake Fumiaki Uchiumi Shin Aoki Kouji Kuramochi Mitsutoshi Tsukimoto Source Type: research

Impact of Hepatitis B Surface and Core Antibody Levels on Hepatitis B Virus Reactivation
We examined the levels of HBV surface antibody (HBsAb) and HBV core antibody (HBcAb) to assess the incidence of HBV-R in cancer patients including hematopoietic stem cell transplantation (HSCT) and rituximab administration. This retrospective cohort study included 590 patients with resolved HBV infection. The incidence of HBV-R was evaluated 761.5 (range, 90-3898) days after the inititiation of chemotherapy. Of the patients, 13 (2.2%) developed HBV-R after the start of chemotherapy. All 13 patients exhibited lower HBsAb (<100 mIU/mL) levels at baseline. A higher level of HBcAb (≥100 cut off index (C.O.I.)) was a possi...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Maki Ohkubo Emiko Seo Kosuke Doki Yoshiharu Suzuki Ikuo Sekine Masato Homma Source Type: research

Structure-Activity Relationship Analysis of Fluoxetine for Suppression of Inflammatory Cytokine Production
Biol Pharm Bull. 2024;47(5):946-954. doi: 10.1248/bpb.b24-00083.ABSTRACTThere is accumulating evidence that selective serotonin reuptake inhibitors (SSRIs), clinically used as antidepressants, have a beneficial effect on inflammatory diseases such as coronavirus disease 2019 (COVID-19). We previously compared the inhibitory effects of five U.S. Food and Drug Administration (FDA)-approved SSRIs on the production of an inflammatory cytokine, interleukin-6 (IL-6), and concluded that fluoxetine (FLX) showed the most potent anti-inflammatory activity. Here, we investigated the structure-activity relationship of FLX for anti-inf...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Yohei Takenaka Ryu Tanaka Kazuki Kitabatake Fumiaki Uchiumi Shin Aoki Kouji Kuramochi Mitsutoshi Tsukimoto Source Type: research

Impact of Hepatitis B Surface and Core Antibody Levels on Hepatitis B Virus Reactivation
We examined the levels of HBV surface antibody (HBsAb) and HBV core antibody (HBcAb) to assess the incidence of HBV-R in cancer patients including hematopoietic stem cell transplantation (HSCT) and rituximab administration. This retrospective cohort study included 590 patients with resolved HBV infection. The incidence of HBV-R was evaluated 761.5 (range, 90-3898) days after the inititiation of chemotherapy. Of the patients, 13 (2.2%) developed HBV-R after the start of chemotherapy. All 13 patients exhibited lower HBsAb (<100 mIU/mL) levels at baseline. A higher level of HBcAb (≥100 cut off index (C.O.I.)) was a possi...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Maki Ohkubo Emiko Seo Kosuke Doki Yoshiharu Suzuki Ikuo Sekine Masato Homma Source Type: research

Structure-Activity Relationship Analysis of Fluoxetine for Suppression of Inflammatory Cytokine Production
Biol Pharm Bull. 2024;47(5):946-954. doi: 10.1248/bpb.b24-00083.ABSTRACTThere is accumulating evidence that selective serotonin reuptake inhibitors (SSRIs), clinically used as antidepressants, have a beneficial effect on inflammatory diseases such as coronavirus disease 2019 (COVID-19). We previously compared the inhibitory effects of five U.S. Food and Drug Administration (FDA)-approved SSRIs on the production of an inflammatory cytokine, interleukin-6 (IL-6), and concluded that fluoxetine (FLX) showed the most potent anti-inflammatory activity. Here, we investigated the structure-activity relationship of FLX for anti-inf...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Yohei Takenaka Ryu Tanaka Kazuki Kitabatake Fumiaki Uchiumi Shin Aoki Kouji Kuramochi Mitsutoshi Tsukimoto Source Type: research

Impact of Hepatitis B Surface and Core Antibody Levels on Hepatitis B Virus Reactivation
We examined the levels of HBV surface antibody (HBsAb) and HBV core antibody (HBcAb) to assess the incidence of HBV-R in cancer patients including hematopoietic stem cell transplantation (HSCT) and rituximab administration. This retrospective cohort study included 590 patients with resolved HBV infection. The incidence of HBV-R was evaluated 761.5 (range, 90-3898) days after the inititiation of chemotherapy. Of the patients, 13 (2.2%) developed HBV-R after the start of chemotherapy. All 13 patients exhibited lower HBsAb (<100 mIU/mL) levels at baseline. A higher level of HBcAb (≥100 cut off index (C.O.I.)) was a possi...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Maki Ohkubo Emiko Seo Kosuke Doki Yoshiharu Suzuki Ikuo Sekine Masato Homma Source Type: research

Structure-Activity Relationship Analysis of Fluoxetine for Suppression of Inflammatory Cytokine Production
Biol Pharm Bull. 2024;47(5):946-954. doi: 10.1248/bpb.b24-00083.ABSTRACTThere is accumulating evidence that selective serotonin reuptake inhibitors (SSRIs), clinically used as antidepressants, have a beneficial effect on inflammatory diseases such as coronavirus disease 2019 (COVID-19). We previously compared the inhibitory effects of five U.S. Food and Drug Administration (FDA)-approved SSRIs on the production of an inflammatory cytokine, interleukin-6 (IL-6), and concluded that fluoxetine (FLX) showed the most potent anti-inflammatory activity. Here, we investigated the structure-activity relationship of FLX for anti-inf...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Yohei Takenaka Ryu Tanaka Kazuki Kitabatake Fumiaki Uchiumi Shin Aoki Kouji Kuramochi Mitsutoshi Tsukimoto Source Type: research

Impact of Hepatitis B Surface and Core Antibody Levels on Hepatitis B Virus Reactivation
We examined the levels of HBV surface antibody (HBsAb) and HBV core antibody (HBcAb) to assess the incidence of HBV-R in cancer patients including hematopoietic stem cell transplantation (HSCT) and rituximab administration. This retrospective cohort study included 590 patients with resolved HBV infection. The incidence of HBV-R was evaluated 761.5 (range, 90-3898) days after the inititiation of chemotherapy. Of the patients, 13 (2.2%) developed HBV-R after the start of chemotherapy. All 13 patients exhibited lower HBsAb (<100 mIU/mL) levels at baseline. A higher level of HBcAb (≥100 cut off index (C.O.I.)) was a possi...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Maki Ohkubo Emiko Seo Kosuke Doki Yoshiharu Suzuki Ikuo Sekine Masato Homma Source Type: research

Structure-Activity Relationship Analysis of Fluoxetine for Suppression of Inflammatory Cytokine Production
Biol Pharm Bull. 2024;47(5):946-954. doi: 10.1248/bpb.b24-00083.ABSTRACTThere is accumulating evidence that selective serotonin reuptake inhibitors (SSRIs), clinically used as antidepressants, have a beneficial effect on inflammatory diseases such as coronavirus disease 2019 (COVID-19). We previously compared the inhibitory effects of five U.S. Food and Drug Administration (FDA)-approved SSRIs on the production of an inflammatory cytokine, interleukin-6 (IL-6), and concluded that fluoxetine (FLX) showed the most potent anti-inflammatory activity. Here, we investigated the structure-activity relationship of FLX for anti-inf...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Yohei Takenaka Ryu Tanaka Kazuki Kitabatake Fumiaki Uchiumi Shin Aoki Kouji Kuramochi Mitsutoshi Tsukimoto Source Type: research

Impact of Hepatitis B Surface and Core Antibody Levels on Hepatitis B Virus Reactivation
We examined the levels of HBV surface antibody (HBsAb) and HBV core antibody (HBcAb) to assess the incidence of HBV-R in cancer patients including hematopoietic stem cell transplantation (HSCT) and rituximab administration. This retrospective cohort study included 590 patients with resolved HBV infection. The incidence of HBV-R was evaluated 761.5 (range, 90-3898) days after the inititiation of chemotherapy. Of the patients, 13 (2.2%) developed HBV-R after the start of chemotherapy. All 13 patients exhibited lower HBsAb (<100 mIU/mL) levels at baseline. A higher level of HBcAb (≥100 cut off index (C.O.I.)) was a possi...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Maki Ohkubo Emiko Seo Kosuke Doki Yoshiharu Suzuki Ikuo Sekine Masato Homma Source Type: research

Structure-Activity Relationship Analysis of Fluoxetine for Suppression of Inflammatory Cytokine Production
Biol Pharm Bull. 2024;47(5):946-954. doi: 10.1248/bpb.b24-00083.ABSTRACTThere is accumulating evidence that selective serotonin reuptake inhibitors (SSRIs), clinically used as antidepressants, have a beneficial effect on inflammatory diseases such as coronavirus disease 2019 (COVID-19). We previously compared the inhibitory effects of five U.S. Food and Drug Administration (FDA)-approved SSRIs on the production of an inflammatory cytokine, interleukin-6 (IL-6), and concluded that fluoxetine (FLX) showed the most potent anti-inflammatory activity. Here, we investigated the structure-activity relationship of FLX for anti-inf...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Yohei Takenaka Ryu Tanaka Kazuki Kitabatake Fumiaki Uchiumi Shin Aoki Kouji Kuramochi Mitsutoshi Tsukimoto Source Type: research

Impact of Hepatitis B Surface and Core Antibody Levels on Hepatitis B Virus Reactivation
We examined the levels of HBV surface antibody (HBsAb) and HBV core antibody (HBcAb) to assess the incidence of HBV-R in cancer patients including hematopoietic stem cell transplantation (HSCT) and rituximab administration. This retrospective cohort study included 590 patients with resolved HBV infection. The incidence of HBV-R was evaluated 761.5 (range, 90-3898) days after the inititiation of chemotherapy. Of the patients, 13 (2.2%) developed HBV-R after the start of chemotherapy. All 13 patients exhibited lower HBsAb (<100 mIU/mL) levels at baseline. A higher level of HBcAb (≥100 cut off index (C.O.I.)) was a possi...
Source: Biological and Pharmaceutical Bulletin - May 12, 2024 Category: Drugs & Pharmacology Authors: Maki Ohkubo Emiko Seo Kosuke Doki Yoshiharu Suzuki Ikuo Sekine Masato Homma Source Type: research