Zhenkun Ma
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View article: Effect of hypertension on clinical outcomes in ischemic colitis
Effect of hypertension on clinical outcomes in ischemic colitis Open
Hypertension worsens clinical symptoms and endoscopic findings of IC but does not affect clinical outcomes.
View article: Screening of UAV Landable Areas by Integrating Semantic Information and Depth Information
Screening of UAV Landable Areas by Integrating Semantic Information and Depth Information Open
Unmanned aerial vehicle (UAV) landing area identification is a critical research topic in the UAV domain. Traditionally, UAV autonomous landing depends on recognizing cooperative target images on ground platforms, but identifying landable …
View article: Visible‐Light‐Induced C−H Amidation of (Hetero)arenes with Hypervalent Iodine(III) Reagents
Visible‐Light‐Induced C−H Amidation of (Hetero)arenes with Hypervalent Iodine(III) Reagents Open
A visible‐light‐promoted C−H amidation of (hetero)arenes with hypervalent iodine reagents has been successfully achieved with good yields. The high efficiency, broad substrate range and good functional group compatibility demonstrated the …
View article: P-1064. Safety, Tolerability, and Pharmacokinetics of Rifaquizone for Injection in Healthy Participants in China: A Single-center, Double-blind, Randomized, Placebo-controlled, Phase 1 Bridge Study
P-1064. Safety, Tolerability, and Pharmacokinetics of Rifaquizone for Injection in Healthy Participants in China: A Single-center, Double-blind, Randomized, Placebo-controlled, Phase 1 Bridge Study Open
Background Rifaquizinone (RFQ, TNP-2092) is a novel multitargeting antibacterial agent under clinical development for the treatment of acute bacterial skin and skin structure infections (ABSSSIs) and prosthetic joint infections (PJIs). Thi…
View article: P-1089. Pharmacokinetics of Rifaquizinone in Rats and Dogs Following Intra-Articular Administration
P-1089. Pharmacokinetics of Rifaquizinone in Rats and Dogs Following Intra-Articular Administration Open
Background Rifaquizinone (RFQ, TNP-2092) is a novel multitargeting drug conjugate in development for the treatment of prosthetic joint infections (PJIs). RFQ exerts its antibacterial activity by inhibiting RNA polymerase, DNA gyrase, and t…
View article: P-1097. Efficacy of Rifaquizinone in a Murine Model of Prosthetic Joint Infection (PJI) with Fluoroquinolone-Sensitive and -Resistant <i>Staphylococcus aureus</i>
P-1097. Efficacy of Rifaquizinone in a Murine Model of Prosthetic Joint Infection (PJI) with Fluoroquinolone-Sensitive and -Resistant <i>Staphylococcus aureus</i> Open
Background Rifaquizinone (RFQ, TNP-2092) is a novel multitargeting drug conjugate in development for the treatment of serious or life-threatening bacterial infections including those caused by gram-positive pathogens that have developed or…
View article: P-1090. Rifaquizinone for the Treatment of Acute Bacterial Skin and Skin Structure Infections: A Multicenter, Double-Blind, Randomized, Active-Controlled, Phase 2 Trial
P-1090. Rifaquizinone for the Treatment of Acute Bacterial Skin and Skin Structure Infections: A Multicenter, Double-Blind, Randomized, Active-Controlled, Phase 2 Trial Open
Background Rifaquizinone (RFQ, TNP-2092) is under development for the treatment of serious or life-threatening bacterial infections including those caused by gram-positive pathogens that have developed resistance to commonly used antibioti…
View article: P-1088. Safety Study of Rifaquizinone in Dogs Following Intra-articular Administration
P-1088. Safety Study of Rifaquizinone in Dogs Following Intra-articular Administration Open
Background Rifaquizinone (RFQ, TNP-2092) is a novel multitargeting drug conjugate in development for the treatment of prosthetic joint infections (PJIs). RFQ exerts its antibacterial activity by inhibiting RNA polymerase, DNA gyrase, and t…
View article: P-1117. An Open-label Phase 1 Study in Healthy Adult Male Participants to Investigate the Absorption, Metabolism, and Excretion of [14C]-Rifaquizinone Following a Single Intravenous Administration
P-1117. An Open-label Phase 1 Study in Healthy Adult Male Participants to Investigate the Absorption, Metabolism, and Excretion of [14C]-Rifaquizinone Following a Single Intravenous Administration Open
Background Rifaquizinone (RFQ, TNP-2092) is a novel multitargeting drug conjugate in development for the treatment of serious or life-threatening bacterial infections including those caused by gram-positive pathogens that have developed or…
View article: P-1111. Efficacy of Intra-Articular Administration of Rifaquizinone in Rodent Models of Implant Infection Associated with <i>Staphylococcus aureus</i>
P-1111. Efficacy of Intra-Articular Administration of Rifaquizinone in Rodent Models of Implant Infection Associated with <i>Staphylococcus aureus</i> Open
Background Rifaquizinone (RFQ, TNP-2092) is a novel multitargeting drug conjugate in development for the treatment of serious or life-threatening bacterial infections including those caused by gram-positive pathogens that have developed or…
View article: The Efficacy and Safety of an Intra-articular Dual-Acting Antibacterial Agent (TNP-2092) for Implant Infection–Associated Methicillin-Resistant <i>Staphylococcus aureus</i>
The Efficacy and Safety of an Intra-articular Dual-Acting Antibacterial Agent (TNP-2092) for Implant Infection–Associated Methicillin-Resistant <i>Staphylococcus aureus</i> Open
Owing to the presence of microbial biofilm on the implant, the eradication of biofilm-associated infections poses a challenge for antibiotic therapies. The study aimed to investigate the efficacy and safety of the novel antibiotic agent TN…
View article: Knocking down AR promotes osteoblasts to recruit prostate cancer cells by altering exosomal circ-DHPS/miR-214-3p/CCL5 pathway
Knocking down AR promotes osteoblasts to recruit prostate cancer cells by altering exosomal circ-DHPS/miR-214-3p/CCL5 pathway Open
Tumor-derived exosomes have been shown to play a key role in organ-specific metastasis, and the androgen receptor regulates prostate cancer (PCa) progression. It is unclear whether the androgen receptor regulates the recruitment of prostat…
View article: Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens Open
TNP-2198, a stable conjugate of a rifamycin pharmacophore and a nitroimidazole pharmacophore, has been designed, synthesized, and evaluated as a novel dual-targeted antibacterial agent for the treatment of microaerophilic and anaerobic bac…
View article: Correction: Tumor-suppressive microRNA-218 inhibits tumor angiogenesis via targeting the mTOR component RICTOR in prostate cancer
Correction: Tumor-suppressive microRNA-218 inhibits tumor angiogenesis via targeting the mTOR component RICTOR in prostate cancer Open
[This corrects the article DOI: 10.18632/oncotarget.14131.].
View article: Novel Linker Variants of Antileishmanial/Antitubercular 7-Substituted 2-Nitroimidazooxazines Offer Enhanced Solubility
Novel Linker Variants of Antileishmanial/Antitubercular 7-Substituted 2-Nitroimidazooxazines Offer Enhanced Solubility Open
Antitubercular 7-substituted 2-nitroimidazo[2,1-b][1,3]oxazines were previously shown to exhibit potent antileishmanial and antitrypanosomal activities, culminating in a new clinical investigational drug for visceral leishmaniasis (DNDI-06…
View article: CD82 Suppresses ADAM17-Dependent E-Cadherin Cleavage and Cell Migration in Prostate Cancer
CD82 Suppresses ADAM17-Dependent E-Cadherin Cleavage and Cell Migration in Prostate Cancer Open
CD82 acts as a tumor suppressor in a series of steps in malignant progression. Here, we identified a novel function of CD82 on posttranslational regulating E-cadherin in prostate cancer. In our study, the declined expression of CD82 was ve…
View article: Synergistic Activity of Nitroimidazole-Oxazolidinone Conjugates against Anaerobic Bacteria
Synergistic Activity of Nitroimidazole-Oxazolidinone Conjugates against Anaerobic Bacteria Open
The introductions of the bicyclic 4-nitroimidazole and the oxazolidinone classes of antimicrobial agents represented the most significant advancements in the infectious disease area during the past two decades. Pretomanid, a bicyclic 4-nit…
View article: 691. Activity of TNP-2092 Against Biofilms Formed by Prosthetic Joint Infection-Associated Staphylococci
691. Activity of TNP-2092 Against Biofilms Formed by Prosthetic Joint Infection-Associated Staphylococci Open
Background Infection occurs in ~1–2% of prosthetic joint replacement surgeries, with staphylococci being the most common cause. TNP-2092 is an investigational drug composed of rifamycin and quinolizinone pharmacophores conjugated via a sta…
View article: Silibinin attenuates TGF‑β1‑induced migration and invasion via EMT suppression and is associated with COX‑2 downregulation in bladder transitional cell carcinoma
Silibinin attenuates TGF‑β1‑induced migration and invasion via EMT suppression and is associated with COX‑2 downregulation in bladder transitional cell carcinoma Open
Transforming growth factor (TGF)‑β1 is highly expressed in bladder transitional cell carcinoma (TCC) and is positively associated with tumor grade. TGF‑β1 signaling promotes cell metastasis by inducing epithelial‑mesenchymal transition (EM…
View article: 7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-<i>b</i>][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis
7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-<i>b</i>][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis Open
Within a backup program for the clinical investigational agent pretomanid (PA-824), scaffold hopping from delamanid inspired the discovery of a novel class of potent antitubercular agents that unexpectedly possessed notable utility against…
View article: 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases
6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases Open
As part of a quest for backups to the antitubercular drug pretomanid (PA-824), we investigated the unexplored 6-nitro-2,3-dihydroimidazo[2,1-b][1,3]-thiazoles and related -oxazoles. The nitroimidazothiazoles were prepared in high yield fro…
View article: Tumor-suppressive microRNA-218 inhibits tumor angiogenesis via targeting the mTOR component RICTOR in prostate cancer
Tumor-suppressive microRNA-218 inhibits tumor angiogenesis via targeting the mTOR component RICTOR in prostate cancer Open
MicroRNAs, a kind of small non-coding RNAs, can regulate gene expression by targeting mRNAs for translational repression or degradation. Much evidence has suggested that miR-218 was a tumor suppressor in many human cancers including prosta…
View article: Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase
Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase Open
The recent development and spread of extensively drug-resistant and totally drug-resistant resistant (TDR) strains of Mycobacterium tuberculosis highlight the need for new antitubercular drugs. Protein synthesis inhibitors have played an i…
View article: Capsaicin enhances anti-proliferation efficacy of pirarubicin via activating TRPV1 and inhibiting PCNA nuclear translocation in 5637 cells
Capsaicin enhances anti-proliferation efficacy of pirarubicin via activating TRPV1 and inhibiting PCNA nuclear translocation in 5637 cells Open
The recurrence of bladder cancer after surgery with or without chemotherapy remains a major challenge in bladder cancer treatment. Previous studies have shown that transient receptor potential vanilloid 1 (TRPV1) acts as a tumor suppressor…