Search Results - "Buolamwini, John K."

Integration of fingerprint-based similarity searching and kernel-based partial least squares analysis to predict inhibitory activity against CSK, HER2, JAK1, JAK2, and JAK3 by Deokar, Hemantkumar, Deokar, Mrunalini, Buolamwini, John K.

“…Fingerprint-based similarity searching is an important strategy for virtual screening in drug discovery. In the present study, we carried out a systematic…”
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A small-molecule inhibitor of MDMX activates p53 and induces apoptosis by Wang, Hongbo, Ma, Xujun, Ren, Shumei, Buolamwini, John K, Yan, Chunhong

“…The p53 inactivation caused by aberrant expression of its major regulators (e.g., MDM2 and MDMX) contributes to the genesis of a large number of human cancers…”
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The pyrido[b]indole MDM2 inhibitor SP-141 exerts potent therapeutic effects in breast cancer models by Wang, Wei, Qin, Jiang-Jiang, Voruganti, Sukesh, Srivenugopal, Kalkunte S., Nag, Subhasree, Patil, Shivaputra, Sharma, Horrick, Wang, Ming-Hai, Wang, Hui, Buolamwini, John K, Zhang, Ruiwen

“…A requirement for Mouse Double Minute 2 (MDM2) oncogene activation has been suggested to be associated with cancer progression and metastasis, including breast…”
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Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors by Sharma, Horrick, Patil, Shivaputra, Sanchez, Tino W., Neamati, Nouri, Schinazi, Raymond F., Buolamwini, John K.

“…HIV-1 integrase is one of the three most important enzymes required for viral replication and is therefore an attractive target for anti retroviral therapy. We…”
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A novel RNA variant of human concentrative nucleoside transporter 1 (hCNT1) that is a potential cancer biomarker by Wang, Chunmei, Buolamwini, John K

“…The human concentrative nucleoside transporter 1 (hCNT1) a product of the  gene is one of the three concentrative nucleoside transporters, with a substrate…”
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Dipyridamole analogs as pharmacological inhibitors of equilibrative nucleoside transporters. Identification of novel potent and selective inhibitors of the adenosine transporter function of human equilibrative nucleoside transporter 4 (hENT4) by Wang, Chunmei, Lin, Wenwei, Playa, Hilaire, Sun, Shan, Cameron, Keyuna, Buolamwini, John K.

“…To identify needed human equilibrative nucleoside transporter 4 (hENT4) inhibitors, we cloned and stably expressed the recombinant protein in PK15NTD…”
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Inhibiting β-Catenin by β-Carboline-Type MDM2 Inhibitor for Pancreatic Cancer Therapy by Qin, Jiang-Jiang, Wang, Wei, Li, Xin, Deokar, Hemantkumar, Buolamwini, John K, Zhang, Ruiwen

“…The β-catenin and MDM2 oncoproteins are overexpressed and constitutively activated in human pancreatic cancer and contribute to its initiation, progression,…”
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JKA97, a novel benzylidene analog of harmine, exerts anti-cancer effects by inducing G1 arrest, apoptosis, and p53-independent up-regulation of p21 by Yang, Xinyi, Wang, Wei, Qin, Jiang-Jiang, Wang, Ming-Hai, Sharma, Horrick, Buolamwini, John K, Wang, Hui, Zhang, Ruiwen

“…JKA97, a benzylidene analog of harmine, has been found to be a promising drug candidate for human cancer therapy, although the underlying molecular mechanisms…”
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Synthesis and biological evaluation of novel 5( H)-phenanthridin-6-ones, 5( H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors by Patil, Shivaputra, Kamath, Shantaram, Sanchez, Tino, Neamati, Nouri, Schinazi, Raymond F., Buolamwini, John K.

“…Substitution of β-diketo acid moiety onto the phenanthridinone and analogous polycyclic aromatic systems provided new potent HIV integrase (IN) inhibitors. The…”
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Design, Synthesis, and Evaluation of 2-Diethanolamino-4,8-diheptamethyleneimino-2-(N-aminoethyl-N-ethanolamino)-6-(N,N-diethanolamino)pyrimido[5,4-d]pyrimidine-fluorescein Conjugate (8MDP-fluor), As a Novel Equilibrative Nucleoside Transporter Probe by Lin, Wenwei, Buolamwini, John K

“…Nucleoside transporters are integral membrane glycoproteins that play critical roles in physiological nucleoside and nucleobase fluxes, and influence the…”
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Targeted Brain Tumor Therapy by Inhibiting the MDM2 Oncogene: In Vitro and In Vivo Antitumor Activity and Mechanism of Action by Punganuru, Surendra R, Artula, Viswanath, Zhao, Wei, Rajaei, Mehrdad, Deokar, Hemantkumar, Zhang, Ruiwen, Buolamwini, John K, Srivenugopal, Kalkunte S, Wang, Wei

“…There is a desperate need for novel and efficacious chemotherapeutic strategies for human brain cancers. There are abundant molecular alterations along the p53…”
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Synthesis and biological evaluation of phloridzin analogs as human concentrative nucleoside transporter 3 (hCNT3) inhibitors by Gupte, Amol, Buolamwini, John K.

“…The synthesis and [ 3H]-uridine uptake investigation of the structure–activity relationship of new phloridzin analogs at the human concentrative nucleoside…”
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Anti-cancer Effects of JKA97 Are Associated with Its Induction of Cell Apoptosis via a Bax-dependent and p53-independent Pathway by Luo, Wenjing, Liu, Jinyi, Li, Jingxia, Zhang, Dongyun, Liu, Mingchao, Addo, James K., Patil, Shivaputra, Zhang, Lin, Yu, Jian, Buolamwini, John K., Chen, Jingyuan, Huang, Chuanshu

“…p53, one of the most commonly mutated genes in human cancers, is thought to be associated with cancer development. Hence, screening and identifying natural or…”
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Identification of the ENT1 Antagonists Dipyridamole and Dilazep as Amplifiers of Oncolytic Herpes Simplex Virus-1 Replication by PASSER, Brent J, CHEEMA, Tooba, QIANJUN LI, BUOLAMWINI, John K, YUN YEN, RABKIN, Samuel D, MARTUZA, Robert L, BINGSEN ZHOU, WAKIMOTO, Hiroaki, ZAUPA, Cecile, RAZMJOO, Mani, SARTE, Jason, SHULIN WU, WU, Chin-Lee, NOAH, James W

“…Oncolytic herpes simplex virus-1 (oHSV) vectors selectively replicate in tumor cells, where they kill through oncolysis while sparing normal cells. One of the…”
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Small Molecule Induces Time‐Dependent Inhibition of Stat3 Dimerization and DNA‐Binding Activity and Regresses Human Breast Tumor Xenografts by Yue, Peibin, Chen, Yue, Ogese, Monday O., Sun, Shan, Zhang, Xiaolei, Esan, Taiwo, Buolamwini, John K., Turkson, James

“…Aberrantly‐active signal transducer and activator of transcription (Stat)3 has a causal role in many human cancers and represents a validated anticancer drug…”
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SS-4 is a highly selective small molecule inhibitor of STAT3 tyrosine phosphorylation that potently inhibits GBM tumorigenesis in vitro and in vivo by Wang, Yinan, Yang, Chuanhe, Sims, Michelle M., Sacher, Joshua R., Raje, Mithun, Deokar, Hemantkumar, Yue, Peibin, Turkson, James, Buolamwini, John K., Pfeffer, Lawrence M.

“…Glioblastoma (GBM) is a highly aggressive cancer with a dismal prognosis. Constitutively active STAT3 has a causal role in GBM progression and is associated…”
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Targeting EGFR and HER-2 receptor tyrosine kinases for cancer drug discovery and development by Kamath, Shantaram, Buolamwini, John K.

“…Conventional anticancer therapy using cytotoxic drugs lacks selectivity and is prone to toxicity and drug resistance. Anticancer therapies targeting aberrant…”
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Identification of a New Class of MDM2 Inhibitor That Inhibits Growth of Orthotopic Pancreatic Tumors in Mice by Wang, Wei, Qin, Jiang-Jiang, Voruganti, Sukesh, Wang, Ming-Hai, Sharma, Horrick, Patil, Shivaputra, Zhou, Jianwei, Wang, Hui, Mukhopadhyay, Debabrata, Buolamwini, John K, Zhang, Ruiwen

“…Background & Aims The oncogene MDM2 , which encodes an E3 ubiquitin ligase, is overexpressed in pancreatic cancers and is therefore a therapeutic target…”
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QSAR studies of new pyrido[3,4-b]indole derivatives as inhibitors of colon and pancreatic cancer cell proliferation by Deokar, Hemantkumar, Deokar, Mrunalini, Wang, Wei, Zhang, Ruiwen, Buolamwini, John K.

“…We have discovered a new class of pyrido[ b ]bindole derivatives that show potent and broad spectrum anticancer activity with IC 50 values down to…”
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Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors by Sharma, Horrick, Sanchez, Tino W., Neamati, Nouri, Detorio, Mervi, Schinazi, Raymond F., Cheng, Xiaolin, Buolamwini, John K.

“…In the present study we report the synthesis of halogen-substituted phenanthrene β-diketo acids as new HIV-1 integrase inhibitors. The target phenanthrenes…”
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