Results 131 to 140 of about 16,181 (141)

Design and Evaluation of Bivalent K‐Ras Inhibitors That Target the CAAX Binding Site and the Acidic Surface of Farnesyltransferase and Geranylgeranyltransferase I

Chemistry – A European Journal, Volume 31, Issue 27, May 14, 2025.
Chemical inhibition of K‐Ras posttranslational prenylation represents a promising strategy against aggressive cancers. A structure‐based design produces piperidine‐based peptidomimetics conjugated to cationic modules, effectively inhibiting FTase and GGTase I at single‐digit nanomolar concentrations.
Naomi Horiuchi, Rania Omer, Fumitoshi Sugino, Nanami Ogino, Yoshihisa Inoue, Kazi Aslamuzzaman, Takeyuki Suzuki, Said M. Sebti, Junko Ohkanda   +8 more
wiley   +1 more source

Quality by Design Based Chromatography Technique Development and Validation for the Medicine Venetoclax (for Chronic Leukemia), in the Context of Impurities Including Degradation Products

Biomedical Chromatography, Volume 39, Issue 5, May 2025.
ABSTRACT The present research study describes the Venetoclax (VEN)‐related substances test method using RP‐HPLC/DAD techniques. It was developed and validated according to ICH Q14 and Q2(R2) guidelines. The substances were separated using an X‐Bridge Phenyl column (150 mm × 4.6 mm, 3.5 μm) and a gradient program.
Rajeshwari Dandabattina, Karuna Sree Merugu, Lova Gani Raju Bandaru, Haridasyam Sharathbabu, Rambabu Gundla, Naresh Kumar Katari   +5 more
wiley   +1 more source

Chidamide, a Histone Deacetylase Inhibitor, Combined With R‐GemOx in Relapsed/Refractory Diffuse Large B‐Cell Lymphoma (TRUST): A Multicenter, Single‐Arm, Phase 2 Trial

Cancer Medicine, Volume 14, Issue 9, May 2025.
ABSTRACT Background Histone deacetylase (HDAC) inhibitors demonstrated a synergistic anti‐tumor effect with rituximab and chemotherapy in preclinical studies on diffuse large B‐cell lymphoma (DLBCL). This phase 2 trial aimed to evaluate the efficacy and safety of chidamide, an orally active HDAC inhibitor, plus the R‐GemOx regimen for relapsed ...
Qihua Zou, Yuchen Zhang, Hui Zhou, Yulin Lai, Yi Cao, Zhiming Li, Ning Su, Wenyu Li, Huiqiang Huang, Panpan Liu, Xu Ye, Yudan Wu, Huo Tan, Runhui Zheng, Bingyi Wu, Hui Yang, Liye Zhong, Yuhong Lu, Yang Liang, Peng Sun, Lirong Li, Yingxian Liu, Danling Dai, Yi Xia, Qingqing Cai   +24 more
wiley   +1 more source

Skeletal Rearrangements of Amides via Breaking Inert Bonds

Chemistry – A European Journal, Volume 31, Issue 25, May 5, 2025.
This review highlights advances in amide skeletal rearrangement reactions over the past two decades, categorized by the initial bond cleavages: C─N bond cleavage, C─C bond cleavage, and C═O bond activation. It summarizes emerging strategies, mechanistic insights, and synthetic applications, providing a focused perspective on recent developments in this
Rui Zhang, Guangbin Dong
wiley   +1 more source

Augmenting the Anti‐Leukemic Activity of the BCL‐2 Inhibitor Venetoclax Through Its Transformation Into Polypharmacologic Dual BCL‐2/HDAC1 and Dual BCL‐2/HDAC6 Inhibitors

Drug Development Research, Volume 86, Issue 3, May 2025.
ABSTRACT Motivated by the anti‐leukemic synergy between histone deacetylase (HDAC) inhibitors and the FDA‐approved BCL‐2 inhibitor venetoclax, coupled with our interests in polypharmacology, we sought to bolster the anti‐leukemic efficacy of the clinical drug by grafting HDAC1‐selective or HDAC6‐selective inhibitor motifs onto a solvent‐accessible ...
Alexandria M. Chan, Christian Eberly, Brandon Drennen, Christopher C. Goodis, Zoe Wuyts, Curt I. Civin, Steven Fletcher   +6 more
wiley   +1 more source

Development of Efficient Covalent Inactivators of a Fungal Aspartate Semialdehyde Dehydrogenase

Drug Development Research, Volume 86, Issue 3, May 2025.
ABSTRACT Aspartate semialdehyde dehydrogenase (ASADH) catalyzes the second step in the fungal pathway towards the synthesis of threonine, isoleucine, and methionine, and it has been identified as a viable target for antifungal drug development. Our previous work produced a group of vinyl sulfones that function as irreversible covalent inactivators of ...
Samantha N. Friday, Liezel A. Koellner, Spencer W. Brown, Christopher N. Calbat, Catherine F. Curran, Jordan D. Dietz, Andreas Koenig‐Dummer, Paul D. Friday, James A. Parker, Noah A. Simmons, Finnean A. Urmey, Alexis N. West, Sebastian G. Zagler, Ronald E. Viola, Christopher J. Halkides   +14 more
wiley   +1 more source

Marburg Virus Disease: A Narrative Review

Health Science Reports, Volume 8, Issue 5, May 2025.
ABSTRACT Background and Aims Given the recent deadly outbreaks of the Marburg virus (MARV), in early 2023 in Tanzania and Equatorial Guinea, and the most recent one in Rwanda in 2024, there has been renewed attention across Africa on the threat posed by the re‐emergence of MARV as a growing concern for public health.
Arash Letafati, Somayeh Sadat Hosseini Fakhr, Ali Qaraee Najafabadi, Negin Karami, Hassan Karami   +4 more
wiley   +1 more source

Structure, function and inhibition of poly(ADP-ribose)polymerase, member 14 (PARP14) [PDF]

, 2018
Levonis, Stephan M, Schweiker, Stephanie S, Sherry, Madeleine, Tauber, Amanda   +3 more
core   +1 more source

Benz[4,5]Isoquino[1,2-\u3cem\u3eb\u3c/em\u3e]Quinazoline-7,9-Dione and a Rearrangement Product of its Hydrolysis, 2-(1,8-Naphthalenedicarboximido)benzamide [PDF]

, 1995
Lindeman, Sergey V., Ponomarev, Igor I., Rusanov, Alexandr L.   +2 more
core   +1 more source

Hamamelitannin analogues potentiate antibiotics in the fight against biofilm-related Staphylococcus aureus infections [PDF]

, 2016
Brackman, Gilles, Coenye, Tom, Cos, Paul, Meyer, Evelyne, Risseeuw, Martijn, Van Calenbergh, Serge, Van Hecke, Kristof, Vermote, Arno   +7 more
core   +1 more source